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1. Hatakeyama A, Fujii M, Hatakeyama R, Fukuoka Y, Satoh-Nakagawa T, Sasaki H: Azelastine hydrochloride on behavioral and psychological symptoms and activities of daily living in dementia patients. Geriatr Gerontol Int; 2008 Mar;8(1):59-61
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  • [Title] Azelastine hydrochloride on behavioral and psychological symptoms and activities of daily living in dementia patients.
  • [MeSH-major] Dementia / drug therapy. Histamine H1 Antagonists, Non-Sedating / therapeutic use. Phthalazines / therapeutic use

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  • (PMID = 18713191.001).
  • [ISSN] 1447-0594
  • [Journal-full-title] Geriatrics & gerontology international
  • [ISO-abbreviation] Geriatr Gerontol Int
  • [Language] eng
  • [Publication-type] Letter; Randomized Controlled Trial
  • [Publication-country] Japan
  • [Chemical-registry-number] 0 / Histamine H1 Antagonists, Non-Sedating; 0 / Phthalazines; ZQI909440X / azelastine
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2. Hashimoto T, Ishii N, Hamada T, Dainichi T, Karashima T, Nakama T, Yasumoto S: Effects of olopatadine hydrochloride, a histamine h(1) receptor antagonist, on histamine-induced skin responses. Dermatol Res Pract; 2010;2010
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  • [Title] Effects of olopatadine hydrochloride, a histamine h(1) receptor antagonist, on histamine-induced skin responses.
  • Effects of olopatadine hydrochloride, a histamine H(1) receptor antagonist, on histamine-induced skin responses were evaluated in 10 healthy subjects in comparison with placebo, fexofenadine hydrochloride, and bepotastine besilate.
  • Olopatadine significantly suppressed histamine-induced wheal, flare, and itch, starting 30 minutes after oral administration.
  • These results suggest that olopatadine can suppress skin symptoms caused by histamine soon after administration.

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  • (PMID = 20886023.001).
  • [ISSN] 1687-6113
  • [Journal-full-title] Dermatology research and practice
  • [ISO-abbreviation] Dermatol Res Pract
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Egypt
  • [Other-IDs] NLM/ PMC2945667
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3. Sugiura K, Hirai S, Suzuki T, Usuda T, Kondo T, Azumi T, Masaki S, Yokoi T, Nitta Y, Kamiya S, Ando K, Mori T, Tomita Y: Evaluation of cetirizine hydrochloride-based therapeutic strategy for chronic urticaria. Nagoya J Med Sci; 2008 Aug;70(3-4):97-106
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  • [Title] Evaluation of cetirizine hydrochloride-based therapeutic strategy for chronic urticaria.
  • [MeSH-major] Cetirizine / therapeutic use. Histamine H1 Antagonists, Non-Sedating / therapeutic use. Urticaria / drug therapy

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  • (PMID = 18954028.001).
  • [ISSN] 0027-7622
  • [Journal-full-title] Nagoya journal of medical science
  • [ISO-abbreviation] Nagoya J Med Sci
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] Japan
  • [Chemical-registry-number] 0 / Histamine H1 Antagonists, Non-Sedating; YO7261ME24 / Cetirizine
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4. Lee JS, Lee JE, Kim N, Oum BS: Comparison of the conjunctival toxicity of topical ocular antiallergic agents. J Ocul Pharmacol Ther; 2008 Dec;24(6):557-62
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  • PURPOSE: The aim of this study was to investigate the cytotoxic effect of topical ocular allergic agents with H1-receptor antagonism and inhibition of histamine release from mast cells on the cultured conjunctival cells of rabbit in vitro.
  • METHODS: Cell damage by the topical ocular antiallergic agents (azelastine hydrochloride, ketotifen fumarate, and olopatadine hydrochloride) was determined by using the lactate dehydrogenase (LDH) leakage assay with the rate of dilution of 10, 20, and 30%, respectively, for a period of 0 and 30 min and 4, 12, and 24 h, and compared with the balanced salt solution-treated group.
  • [MeSH-minor] Animals. Cells, Cultured. Dibenzoxepins / toxicity. Hydrogen-Ion Concentration. Ketotifen / toxicity. L-Lactate Dehydrogenase / analysis. Microscopy, Electron. Microscopy, Phase-Contrast. Olopatadine Hydrochloride. Phthalazines / toxicity. Rabbits

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  • (PMID = 19049267.001).
  • [ISSN] 1557-7732
  • [Journal-full-title] Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics
  • [ISO-abbreviation] J Ocul Pharmacol Ther
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Anti-Allergic Agents; 0 / Dibenzoxepins; 0 / Phthalazines; 2XG66W44KF / Olopatadine Hydrochloride; EC 1.1.1.27 / L-Lactate Dehydrogenase; X49220T18G / Ketotifen; ZQI909440X / azelastine
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5. Mizuguchi H, Hatano M, Matsushita C, Umehara H, Kuroda W, Kitamura Y, Takeda N, Fukui H: Repeated pre-treatment with antihistamines suppresses [corrected] transcriptional up-regulations of histamine H(1) receptor and interleukin-4 genes in toluene-2,4-diisocyanate-sensitized rats. J Pharmacol Sci; 2008 Dec;108(4):480-6
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  • [Title] Repeated pre-treatment with antihistamines suppresses [corrected] transcriptional up-regulations of histamine H(1) receptor and interleukin-4 genes in toluene-2,4-diisocyanate-sensitized rats.
  • To determine the reason for the effectiveness of prophylactic treatment with antihistamines, the effects of repeated pre-treatment with antihistamines before provocation with toluene 2,4-diisocyanate (TDI) on their nasal allergy-like behavior and up-regulations of histamine H(1) receptors (H1R) and interleukin (IL)-4 mRNAs in their nasal mucosa were examined.
  • [MeSH-major] Histamine H1 Antagonists / pharmacology. Interleukin-4 / metabolism. Receptors, Histamine H1 / drug effects. Up-Regulation / drug effects
  • [MeSH-minor] Animals. Chlorpheniramine / administration & dosage. Chlorpheniramine / pharmacology. Dibenzazepines / administration & dosage. Dibenzazepines / pharmacology. Dibenzoxepins / administration & dosage. Dibenzoxepins / pharmacology. Drug Administration Schedule. Imidazoles / administration & dosage. Imidazoles / pharmacology. Male. Nasal Mucosa / drug effects. Nasal Mucosa / metabolism. Olopatadine Hydrochloride. RNA, Messenger / drug effects. RNA, Messenger / metabolism. Rats. Rats, Inbred BN. Sneezing / drug effects. Time Factors. Toluene 2,4-Diisocyanate. Transcription, Genetic

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  • [ErratumIn] J Pharmacol Sci.2009 Feb;109(2):324
  • (PMID = 19075512.001).
  • [ISSN] 1347-8613
  • [Journal-full-title] Journal of pharmacological sciences
  • [ISO-abbreviation] J. Pharmacol. Sci.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] Japan
  • [Chemical-registry-number] 0 / Dibenzazepines; 0 / Dibenzoxepins; 0 / Histamine H1 Antagonists; 0 / Imidazoles; 0 / RNA, Messenger; 0 / Receptors, Histamine H1; 17X7AFZ1GH / Toluene 2,4-Diisocyanate; 207137-56-2 / Interleukin-4; 2XG66W44KF / Olopatadine Hydrochloride; 3U6IO1965U / Chlorpheniramine; Q13WX941EF / epinastine
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6. Ali AH, Yanoff LB, Stern EA, Akomeah A, Courville A, Kozlosky M, Brady SM, Calis KA, Reynolds JC, Crocker MK, Barak N, Yanovski JA: Acute effects of betahistine hydrochloride on food intake and appetite in obese women: a randomized, placebo-controlled trial. Am J Clin Nutr; 2010 Dec;92(6):1290-7
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  • [Title] Acute effects of betahistine hydrochloride on food intake and appetite in obese women: a randomized, placebo-controlled trial.
  • In animal models, histamine receptor 1 (HRH1) agonists and histamine receptor 3 (HRH3) antagonists decrease food intake.
  • OBJECTIVE: The objective of this study was to examine the acute effects of betahistine hydrochloride (an HRH1 agonist and HRH3 antagonist) on food intakes and appetites.

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  • (PMID = 20881066.001).
  • [ISSN] 1938-3207
  • [Journal-full-title] The American journal of clinical nutrition
  • [ISO-abbreviation] Am. J. Clin. Nutr.
  • [Language] eng
  • [Databank-accession-numbers] ClinicalTrials.gov/ NCT00459992
  • [Grant] United States / NICHD NIH HHS / HD / Z01-HD-00641
  • [Publication-type] Journal Article; Randomized Controlled Trial; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] X32KK4201D / Betahistine
  • [Other-IDs] NLM/ PMC2980955
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7. Dong Y, Ishikawa H, Wu Y, Yoshitomi T: Vasodilatory mechanism of levobunolol on vascular smooth muscle cells. Exp Eye Res; 2007 Jun;84(6):1039-46
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  • Topical application of levobunolol hydrochloride, a beta-adrenergic antagonist used for treatment of glaucoma, is reported to increase ocular blood flow.
  • Levobunolol relaxed ciliary artery rings that were pre-contracted with either high-K solution, 1microM histamine, 10microM phenylephrine, or 100nM endothelin-1.
  • Histamine-induced contractions were inhibited by the histamine H(1) antagonist pyrilamine.
  • Further, histamine induced transient contraction in Ca(2+)-free solution, and levobunolol inhibited this contraction by 74.6+/-11.0%.
  • In cultured smooth muscle cells in the presence of extracellular Ca(2+), levobunolol significantly inhibited the histamine-induced elevation of [Ca(2+)](i).
  • However, it did not inhibit the increase of [Ca(2+)](i) in histamine-stimulated cells incubated in Ca(2+)-free solution.

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  • (PMID = 17459374.001).
  • [ISSN] 0014-4835
  • [Journal-full-title] Experimental eye research
  • [ISO-abbreviation] Exp. Eye Res.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Adrenergic beta-Antagonists; 0 / Vasoconstrictor Agents; 0 / Vasodilator Agents; 1WS297W6MV / Phenylephrine; EE92BBP03H / Diltiazem; G6317AOI7K / Levobunolol; SY7Q814VUP / Calcium
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8. Ozadali K, Ozkannli F, Erol D, Doğan AE, Erol K: Synthesis and biological activities of some thiazolidin-4-ones. Arzneimittelforschung; 2006;56(10):678-81
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  • Compound 15 (3-[3-(2-methyl-piperidine-1-yl)propyl]-2-(4-methyl-phenyl)thiazolidin-4-one hydrochloride) showed the highest inhibition (53 %).
  • [MeSH-major] Cholinergic Antagonists / chemical synthesis. Cholinergic Antagonists / pharmacology. Histamine Antagonists / chemical synthesis. Histamine Antagonists / pharmacology. Thiazolidines / chemical synthesis. Thiazolidines / pharmacology

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  • (PMID = 17225562.001).
  • [ISSN] 0004-4172
  • [Journal-full-title] Arzneimittel-Forschung
  • [ISO-abbreviation] Arzneimittelforschung
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Chemical-registry-number] 0 / Cholinergic Antagonists; 0 / Histamine Antagonists; 0 / Indicators and Reagents; 0 / Schiff Bases; 0 / Thiazolidines; 0 / Vasodilator Agents; N9YNS0M02X / Acetylcholine
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9. Mochizuki Y, Furuta A, Furuya A, Kanai K, Asano K, Suzaki H: Suppressive activity of epinastine hydrochloride on eosinophil activation in vitro. In Vivo; 2008 Jan-Feb;22(1):13-20
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  • [Title] Suppressive activity of epinastine hydrochloride on eosinophil activation in vitro.
  • The influence of a histamine H1 receptor antagonist, epinastine hydrochloride (EP), on eosinophil functions was examined in vitro and in vivo.
  • [MeSH-major] Dibenzazepines / pharmacology. Eosinophils / drug effects. Histamine H1 Antagonists / pharmacology. Imidazoles / pharmacology. Platelet Aggregation Inhibitors / pharmacology

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  • (PMID = 18396776.001).
  • [ISSN] 0258-851X
  • [Journal-full-title] In vivo (Athens, Greece)
  • [ISO-abbreviation] In Vivo
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] Greece
  • [Chemical-registry-number] 0 / Ccl5 protein, mouse; 0 / Chemokine CCL4; 0 / Chemokine CCL5; 0 / Dibenzazepines; 0 / Drug Combinations; 0 / Histamine H1 Antagonists; 0 / Imidazoles; 0 / Platelet Aggregation Inhibitors; 0 / Stem Cell Factor; 2CU6TT9V48 / Leukotriene C4; 37341-29-0 / Immunoglobulin E; Q13WX941EF / epinastine
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10. Ohmura T, Kawasaki T: [Pharmacological and clinical profile of epinastine hydrochloride (Alesion Dry Syrup 1%)]. Nihon Yakurigaku Zasshi; 2006 Jan;127(1):37-46
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] [Pharmacological and clinical profile of epinastine hydrochloride (Alesion Dry Syrup 1%)].
  • [MeSH-major] Dibenzazepines / pharmacology. Dibenzazepines / therapeutic use. Histamine H1 Antagonists / pharmacology. Histamine H1 Antagonists / therapeutic use. Imidazoles / pharmacology. Imidazoles / therapeutic use

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  • (PMID = 16508222.001).
  • [ISSN] 0015-5691
  • [Journal-full-title] Nihon yakurigaku zasshi. Folia pharmacologica Japonica
  • [ISO-abbreviation] Nippon Yakurigaku Zasshi
  • [Language] jpn
  • [Publication-type] Journal Article; Review
  • [Publication-country] Japan
  • [Chemical-registry-number] 0 / Dibenzazepines; 0 / Histamine H1 Antagonists; 0 / Imidazoles; Q13WX941EF / epinastine
  • [Number-of-references] 43
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11. Roland PS, Marple BF, Wall GM: Olopatadine nasal spray for the treatment of allergic rhinitis. Expert Rev Clin Immunol; 2010 Mar;6(2):197-204
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  • Olopatadine hydrochloride nasal spray (Patanase Nasal Spray, Alcon Laboratories, TX, USA) was approved by the US FDA in 2008, and is indicated for the relief of symptoms of seasonal allergic rhinitis (SAR), also referred to as allergic rhinosinusitis.
  • [MeSH-major] Dibenzoxepins / therapeutic use. Histamine H1 Antagonists, Non-Sedating / therapeutic use. Rhinitis, Allergic, Seasonal / drug therapy
  • [MeSH-minor] Activities of Daily Living. Administration, Intranasal. Clinical Trials as Topic. Drug Approval. Epistaxis / etiology. Nasal Obstruction. Olopatadine Hydrochloride. Quality of Life

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  • (PMID = 20402382.001).
  • [ISSN] 1744-666X
  • [Journal-full-title] Expert review of clinical immunology
  • [ISO-abbreviation] Expert Rev Clin Immunol
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Dibenzoxepins; 0 / Histamine H1 Antagonists, Non-Sedating; 2XG66W44KF / Olopatadine Hydrochloride
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12. Zhou HY, Chen XG, Liu CS, Meng XH, Yu LJ, Liu XY, Liu N: Chitosan/cellulose acetate microspheres preparation and ranitidine release in vitro. Pharm Dev Technol; 2005;10(2):219-25
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  • Ranitidine hydrochloride, as a model drug, was investigated for its release properties in vitro.
  • [MeSH-major] Cellulose / analogs & derivatives. Cellulose / chemistry. Chitosan / chemistry. Excipients / chemistry. Histamine H2 Antagonists / administration & dosage. Ranitidine / administration & dosage

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  • (PMID = 15926670.001).
  • [ISSN] 1083-7450
  • [Journal-full-title] Pharmaceutical development and technology
  • [ISO-abbreviation] Pharm Dev Technol
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Delayed-Action Preparations; 0 / Excipients; 0 / Histamine H2 Antagonists; 3J2P07GVB6 / acetylcellulose; 884KT10YB7 / Ranitidine; 9004-34-6 / Cellulose; 9012-76-4 / Chitosan
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13. Tashiro M, Kato M, Miyake M, Watanuki S, Funaki Y, Ishikawa Y, Iwata R, Yanai K: Dose dependency of brain histamine H(1) receptor occupancy following oral administration of cetirizine hydrochloride measured using PET with [11C]doxepin. Hum Psychopharmacol; 2009 Oct;24(7):540-8
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  • [Title] Dose dependency of brain histamine H(1) receptor occupancy following oral administration of cetirizine hydrochloride measured using PET with [11C]doxepin.
  • The purpose of the present study is to measure histamine H(1) receptor (H(1)R) occupancy following oral administration of cetirizine (10 and 20 mg) in order to examine dose dependency.
  • [MeSH-major] Brain. Cetirizine / administration & dosage. Cetirizine / pharmacology. Doxepin. Histamine Antagonists. Histamine H1 Antagonists, Non-Sedating / pharmacology. Receptors, Histamine H1 / metabolism

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  • (PMID = 19697300.001).
  • [ISSN] 1099-1077
  • [Journal-full-title] Human psychopharmacology
  • [ISO-abbreviation] Hum Psychopharmacol
  • [Language] eng
  • [Publication-type] Clinical Trial; Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Carbon Isotopes; 0 / Histamine Antagonists; 0 / Histamine H1 Antagonists, Non-Sedating; 0 / Receptors, Histamine H1; 1668-19-5 / Doxepin; 30S50YM8OG / Hydroxyzine; YO7261ME24 / Cetirizine
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14. Tamura T, Amano T, Ohmori K, Manabe H: The effects of olopatadine hydrochloride on the number of scratching induced by repeated application of oxazolone in mice. Eur J Pharmacol; 2005 Nov 7;524(1-3):149-54
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  • [Title] The effects of olopatadine hydrochloride on the number of scratching induced by repeated application of oxazolone in mice.
  • It is suggested that atopic dermatitis is a skin disease associated with itching as subjective symptoms, and histamine H(1) receptor antagonists are used in order to prevent the itching, and the deterioration for scratch by itching.
  • Histamine H(1) receptor selective anti-histamine olopatadine hydrochloride (olopatadine; Allelock shows consistent efficacy and safety in the treatment of allergic disorders.
  • These results indicate that olopatadine inhibited not only the increased production of cytokines but also NGF and substance P unlike other histamine H(1) receptor antagonists.
  • Therefore, olopatadine appears to exert additional biological effects besides its blockade of a histamine H(1) receptor.
  • [MeSH-major] Dibenzoxepins / therapeutic use. Histamine H1 Antagonists / therapeutic use. Pruritus / prevention & control
  • [MeSH-minor] Animals. Anti-Inflammatory Agents / therapeutic use. Antipruritics / therapeutic use. Chlorpheniramine / therapeutic use. Cytokines / metabolism. Dermatitis, Contact / etiology. Dermatitis, Contact / metabolism. Dermatitis, Contact / prevention & control. Dose-Response Relationship, Drug. Ear / pathology. Immunoglobulin E / blood. Male. Mice. Mice, Inbred BALB C. Nerve Growth Factor / metabolism. Olopatadine Hydrochloride. Oxazolone / administration & dosage. Oxazolone / toxicity. Prednisolone / therapeutic use. Severity of Illness Index

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  • (PMID = 16259975.001).
  • [ISSN] 0014-2999
  • [Journal-full-title] European journal of pharmacology
  • [ISO-abbreviation] Eur. J. Pharmacol.
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / Anti-Inflammatory Agents; 0 / Antipruritics; 0 / Cytokines; 0 / Dibenzoxepins; 0 / Histamine H1 Antagonists; 15646-46-5 / Oxazolone; 2XG66W44KF / Olopatadine Hydrochloride; 37341-29-0 / Immunoglobulin E; 3U6IO1965U / Chlorpheniramine; 9061-61-4 / Nerve Growth Factor; 9PHQ9Y1OLM / Prednisolone
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15. Zarrindast MR, Taheri S, Rezayof A: The effects of histaminergic agents in the nucleus accumbens of rats in the elevated plus-maze test of anxiety. Iran J Psychiatry; 2010;5(1):11-7
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  • There are reports indicating that central histamine systems are involved in many physiological behavioral processes, including anxiety.
  • METHODS: Rats were anesthetized with intra-peritoneal injection of ketamine hydrochloride, plus xylazine and then were placed in a stereotaxic apparatus.
  • RESULTS: Intra-NAc administration of histamine (0.01, 0.1 and 1 µg/rat) increased the percentage of open arm time (%OAT) and open arm entries (%OAE), but not locomotor activity, indicating an anxiolytic response.
  • However, both histamine and histamine receptor antagonists showed an anxiolytic-like effect; the antagonists (1 µg/rat) also decreased the histamine response.
  • CONCLUSION: The results may indicate a modulatory effect for the H(1) and H(2) histamine receptors of nucleus accumbens in the anxiety behavior of rats.

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  • (PMID = 22952484.001).
  • [ISSN] 1735-4587
  • [Journal-full-title] Iranian journal of psychiatry
  • [ISO-abbreviation] Iran J Psychiatry
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Iran
  • [Other-IDs] NLM/ PMC3430404
  • [Keywords] NOTNLM ; Anxiety / Histamine / Maze learning / Pyrilamine / Ranitidine / Rats
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16. Lekhanont K, Park CY, Combs JC, Suwan-Apichon O, Rangsin R, Chuck RS: Effect of topical olopatadine and epinastine in the botulinum toxin B-induced mouse model of dry eye. J Ocul Pharmacol Ther; 2007 Feb;23(1):83-8
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  • [MeSH-major] Dibenzazepines / therapeutic use. Dibenzoxepins / therapeutic use. Disease Models, Animal. Histamine H1 Antagonists / therapeutic use. Imidazoles / therapeutic use. Keratoconjunctivitis Sicca / drug therapy
  • [MeSH-minor] Administration, Topical. Animals. Botulinum Toxins / toxicity. Botulinum Toxins, Type A. Female. Mice. Mice, Inbred CBA. Olopatadine Hydrochloride. Tears / secretion

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  • (PMID = 17341156.001).
  • [ISSN] 1080-7683
  • [Journal-full-title] Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics
  • [ISO-abbreviation] J Ocul Pharmacol Ther
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Dibenzazepines; 0 / Dibenzoxepins; 0 / Histamine H1 Antagonists; 0 / Imidazoles; 0Y70779M1F / rimabotulinumtoxinB; 2XG66W44KF / Olopatadine Hydrochloride; EC 3.4.24.69 / Botulinum Toxins; EC 3.4.24.69 / Botulinum Toxins, Type A; Q13WX941EF / epinastine
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17. Watase F, Watanabe S, Kanai K, Yamada N, Sakaue S, Asano K, Hisamitsu T, Suzaki H: Modulation of eosinophil survival by epinastine hydrochloride, an H1 receptor antagonist, in vitro. In Vivo; 2008 Nov-Dec;22(6):687-91
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  • [Title] Modulation of eosinophil survival by epinastine hydrochloride, an H1 receptor antagonist, in vitro.
  • The influence of epinastine hydrochloride (EP) on eosinophil survival was examined by an in vitro cell culture technique.
  • [MeSH-major] Cell Survival / drug effects. Dibenzazepines / pharmacology. Eosinophils / cytology. Histamine H1 Antagonists / pharmacology. Imidazoles / pharmacology

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  • (PMID = 19180992.001).
  • [ISSN] 0258-851X
  • [Journal-full-title] In vivo (Athens, Greece)
  • [ISO-abbreviation] In Vivo
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] Greece
  • [Chemical-registry-number] 0 / Dibenzazepines; 0 / Histamine H1 Antagonists; 0 / Imidazoles; 0 / Tumor Necrosis Factor-alpha; 83869-56-1 / Granulocyte-Macrophage Colony-Stimulating Factor; Q13WX941EF / epinastine
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18. Kishimoto K, Kaneko S, Ohmori K, Tamura T, Hasegawa K: Olopatadine suppresses the migration of THP-1 monocytes induced by S100A12 protein. Mediators Inflamm; 2006;2006(1):42726
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  • Olopatadine hydrochloride (olopatadine) is an antiallergic drug with histamine H(1) receptor antagonistic activity.
  • However, ketotifen, another histamine H(1) receptor antagonist, had little effect on the activity of S100A12.
  • These results suggest that olopatadine has a new mechanism of action, that is, suppression of the function of S100A12, in addition to histamine H(1) receptor antagonistic activity.
  • [MeSH-major] Dibenzoxepins / pharmacology. Gene Expression Regulation. Histamine H1 Antagonists, Non-Sedating / pharmacology. Monocytes / cytology. S100 Proteins / physiology
  • [MeSH-minor] Aminopyridines / pharmacology. Cell Culture Techniques / methods. Cell Movement. Histamine H1 Antagonists / pharmacology. Humans. Inflammation. Ketotifen / pharmacology. Olopatadine Hydrochloride. Receptors, Histamine H1 / metabolism. S100A12 Protein

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  • (PMID = 16864903.001).
  • [ISSN] 0962-9351
  • [Journal-full-title] Mediators of inflammation
  • [ISO-abbreviation] Mediators Inflamm.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Aminopyridines; 0 / Dibenzoxepins; 0 / Histamine H1 Antagonists; 0 / Histamine H1 Antagonists, Non-Sedating; 0 / Receptors, Histamine H1; 0 / S100 Proteins; 0 / S100A12 Protein; 0 / S100A12 protein, human; 2XG66W44KF / Olopatadine Hydrochloride; BRL1C2459K / amlexanox; X49220T18G / Ketotifen
  • [Other-IDs] NLM/ PMC1570388
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19. Wüstenberg EG, Zahnert T, Hüttenbrink KB, Hummel T: Comparison of optical rhinometry and active anterior rhinomanometry using nasal provocation testing. Arch Otolaryngol Head Neck Surg; 2007 Apr;133(4):344-9
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  • Changes in nasal congestion were induced by nasal provocation with histamine, allergens, solvent, and xylometazoline hydrochloride, 0.1%.
  • INTERVENTIONS: Nasal provocation tests with allergens, histamine, control solution, or xylometazoline were performed.

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  • (PMID = 17438248.001).
  • [ISSN] 0886-4470
  • [Journal-full-title] Archives of otolaryngology--head & neck surgery
  • [ISO-abbreviation] Arch. Otolaryngol. Head Neck Surg.
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article
  • [Publication-country] United States
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20. Kurai J, Chikumi H, Kodani M, Sako T, Watanabe M, Miyata M, Makino H, Touge H, Hitsuda Y, Shimizu E: Acute eosinophilic pneumonia caused by calcium stearate, an additive agent for an oral antihistaminic medication. Intern Med; 2006;45(17):1011-6
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  • A 70-year-old man was admitted to our hospital because of dyspnea after taking an antihistaminic agent (homochlorcyclizine hydrochloride) for itching.
  • A drug lymphocyte stimulation test was positive only for calcium stearate, an additive contained in the homochlorcyclizine hydrochloride tablet.
  • [MeSH-major] Histamine H1 Antagonists / adverse effects. Pulmonary Eosinophilia / chemically induced. Stearic Acids / adverse effects

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  • (PMID = 17016002.001).
  • [ISSN] 1349-7235
  • [Journal-full-title] Internal medicine (Tokyo, Japan)
  • [ISO-abbreviation] Intern. Med.
  • [Language] eng
  • [Publication-type] Case Reports; Journal Article
  • [Publication-country] Japan
  • [Chemical-registry-number] 0 / Histamine H1 Antagonists; 0 / Stearic Acids; 0 / Tablets; 4ELV7Z65AP / stearic acid; N5MVC31W2N / homochlorocyclizine; QRW9FCR9P2 / Cyclizine
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21. Kamijo Y, Hayashi I, Ide A, Yoshimura K, Soma K, Majima M: Effects of inhaled monoethanolamine on bronchoconstriction. J Appl Toxicol; 2009 Jan;29(1):15-9
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  • MEA-induced bronchoconstriction was significantly suppressed by premedication with intravenously injected atropine sulfate (3 mg kg(-1)), a muscarinic receptor antagonist, or diphenhydramine hydrochloride (10 mg kg(-1)), a histamine-H(1) receptor antagonist.
  • When bronchoconstriction was induced by MEA, histamine concentrations in bronchoalveolar lavage fluid (BALF) were not significantly greater than in BALF after KOH-induced bronchoconstriction or in BALF after inhalation of physiologic saline.
  • In vitro, contraction of trachea denuded of epithelium during superfusion with MEA (10 mm) was suppressed by premedication with pyrilamine maleate, a histamine-H(1) receptor antagonist, at 10 and 100 microm.
  • These results suggest that asthma-like symptoms may result partly from agonistic MEA effects at histamine-H(1) receptors and muscarinic receptors.
  • [MeSH-minor] Aerosols. Airway Resistance / drug effects. Animals. Atropine / pharmacology. Bronchoalveolar Lavage Fluid / chemistry. Bronchodilator Agents / pharmacology. Diphenhydramine / pharmacology. Disease Models, Animal. Dose-Response Relationship, Drug. Drug Interactions. Guinea Pigs. Histamine / analysis. Inhalation Exposure. Intubation, Intratracheal. Male. Neostigmine / pharmacology. Organ Culture Techniques. Trachea / drug effects. Trachea / physiopathology

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  • [Copyright] Copyright (c) 2008 John Wiley & Sons, Ltd.
  • (PMID = 18651722.001).
  • [ISSN] 0260-437X
  • [Journal-full-title] Journal of applied toxicology : JAT
  • [ISO-abbreviation] J Appl Toxicol
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Aerosols; 0 / Air Pollutants, Occupational; 0 / Bronchodilator Agents; 3982TWQ96G / Neostigmine; 5KV86114PT / Ethanolamine; 7C0697DR9I / Atropine; 820484N8I3 / Histamine; 8GTS82S83M / Diphenhydramine
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22. Tsunematsu M, Yamaji T, Kozutsumi D, Murakami R, Kimura S, Kino K: Establishment of an allergic rhinitis model in mice for the evaluation of nasal symptoms. Life Sci; 2007 Mar 20;80(15):1388-94
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  • Five weeks after the final sensitization, we challenged the mice by instilling Cry j 1 intranasally from the day after intranasal histamine pretreatment.
  • In addition, we confirmed the effects of ketotifen fumarate and dexamethasone hydrochloride on these animals.
  • In Cry j 1-sensitized B10.S mice, sneezes, eosinophil peroxidase (EPO) activity in nasal tissues, and Cry j 1-specific IgE clearly increased after intranasal histamine pretreatment and 5 days of continuous intranasal Cry j 1 challenge.
  • [MeSH-minor] Animals. Anti-Allergic Agents / pharmacology. Anti-Inflammatory Agents / pharmacology. Antigens / immunology. Cryptomeria. Dexamethasone / pharmacology. Disease Models, Animal. Eosinophils / enzymology. Eosinophils / pathology. Female. Histamine / pharmacology. Immunization. Immunoglobulin E / immunology. Ketotifen / pharmacology. Mice. Peroxidases / metabolism. Pollen / immunology. Sneezing / drug effects

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  • (PMID = 17300813.001).
  • [ISSN] 0024-3205
  • [Journal-full-title] Life sciences
  • [ISO-abbreviation] Life Sci.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Anti-Allergic Agents; 0 / Anti-Inflammatory Agents; 0 / Antigens; 37341-29-0 / Immunoglobulin E; 7S5I7G3JQL / Dexamethasone; 820484N8I3 / Histamine; EC 1.11.1.- / Peroxidases; X49220T18G / Ketotifen
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23. Takahashi H, Zhang Y, Morita E: Evaluation of the antihistamine effects of olopatadine, cetirizine and fexofenadine during a 24 h period: a double-blind, randomized, crossover, placebo-controlled comparison in skin responses induced by histamine iontophoresis. Arch Dermatol Res; 2008 Jul;300(6):291-5
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  • [Title] Evaluation of the antihistamine effects of olopatadine, cetirizine and fexofenadine during a 24 h period: a double-blind, randomized, crossover, placebo-controlled comparison in skin responses induced by histamine iontophoresis.
  • The test was designed in a double-blind, randomized, crossover, placebo-controlled study of ten healthy volunteers on histamine-induced flare and wheal response using an iontophoresis technique.
  • The suppressive effect of olopatadine on the wheals induced by a 0.1-mA histamine iontophoresis lasted for 24 h after dosing.
  • Olopatadine completely suppressed even the wheal response induced by a 0.2-mA histamine iontophoresis, although fexofenadine and cetirizine were less effective on the wheals induced by the same histamine challenge.
  • [MeSH-major] Cetirizine / administration & dosage. Dibenzoxepins / administration & dosage. Histamine Antagonists / administration & dosage. Skin / drug effects. Terfenadine / analogs & derivatives
  • [MeSH-minor] Adult. Cross-Over Studies. Dose-Response Relationship, Drug. Double-Blind Method. Drug Administration Schedule. Female. Humans. Iontophoresis / adverse effects. Male. Olopatadine Hydrochloride. Urticaria / chemically induced. Urticaria / immunology

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  • (PMID = 18305947.001).
  • [ISSN] 1432-069X
  • [Journal-full-title] Archives of dermatological research
  • [ISO-abbreviation] Arch. Dermatol. Res.
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article; Randomized Controlled Trial
  • [Publication-country] Germany
  • [Chemical-registry-number] 0 / Dibenzoxepins; 0 / Histamine Antagonists; 2XG66W44KF / Olopatadine Hydrochloride; 7BA5G9Y06Q / Terfenadine; E6582LOH6V / fexofenadine; YO7261ME24 / Cetirizine
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24. Tamura T, Masaki S, Ohmori K, Karasawa A: Effect of olopatadine and other histamine H1 receptor antagonists on the skin inflammation induced by repeated topical application of oxazolone in mice. Pharmacology; 2005 Dec;75(1):45-52
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  • [Title] Effect of olopatadine and other histamine H1 receptor antagonists on the skin inflammation induced by repeated topical application of oxazolone in mice.
  • Histamine H1 receptor antagonists have long been prescribed for atopic dermatitis as an adjuvant therapy with topical therapy by local applied steroids.
  • Olopatadine is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders.
  • We investigated that the effect of olopatadine on oxazolone-induced chronic contact hypersensitivity response in BALB/c mice compared with other histamine H1 receptor antagonists loratadine, cetirizine and fexofenadine.
  • The chronic contact hypersensitivity induced by repeated application of oxazolone was treated with olopatadine and other histamine H1 receptor antagonists at the effective doses on histamine-induced paw edema in mice.
  • On the other hand, the other histamine H1 receptor antagonists did not significantly suppress the increase in ear thickness.
  • These results indicate that olopatadine appears to exert additional biological effects besides its blockade of the histamine H1 receptor.
  • [MeSH-major] Dibenzoxepins / pharmacology. Drug Eruptions / prevention & control. Edema / prevention & control. Histamine H1 Antagonists / pharmacology
  • [MeSH-minor] Animals. Cytokines / metabolism. Ear. Histamine. Immunoglobulin E / blood. Male. Mice. Mice, Inbred BALB C. Nerve Growth Factor / metabolism. Olopatadine Hydrochloride. Oxazolone / administration & dosage. Skin / drug effects. Skin / metabolism. Time Factors

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  • [Copyright] Copyright (c) 2005 S. Karger AG, Basel.
  • (PMID = 15942272.001).
  • [ISSN] 0031-7012
  • [Journal-full-title] Pharmacology
  • [ISO-abbreviation] Pharmacology
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article
  • [Publication-country] Switzerland
  • [Chemical-registry-number] 0 / Cytokines; 0 / Dibenzoxepins; 0 / Histamine H1 Antagonists; 15646-46-5 / Oxazolone; 2XG66W44KF / Olopatadine Hydrochloride; 37341-29-0 / Immunoglobulin E; 820484N8I3 / Histamine; 9061-61-4 / Nerve Growth Factor
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25. Zhang Y, Zhang L, Li B, Wang LP: [Effects of acupuncture preventive treatment on the quality of life in patients of no-aura migraine]. Zhongguo Zhen Jiu; 2009 Jun;29(6):431-5
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  • The observation group was treated with acupuncture combined with oral administration of Flunarizine Hydrochloride vacuity capsules, and Baihui (GV 20), Shenting (GV 24) and Benshen (GB 13) were selected as main points.
  • The control group was treated with oral administration of Flunarizine Hydrochloride capsules combined with acupuncture at placebo-points, thrice each week, for 4 weeks.
  • There is no significant difference in improving the physical and psychological health of the migraine patients between acupuncture and Flunarizine Hydrochloride, and acupuncture is more effective in reducing the migraine attack days.
  • [MeSH-minor] Acupuncture Points. Adult. Double-Blind Method. Female. Flunarizine / administration & dosage. Flunarizine / therapeutic use. Histamine H1 Antagonists / administration & dosage. Histamine H1 Antagonists / therapeutic use. Humans. Male. Middle Aged. Surveys and Questionnaires. Treatment Outcome. Young Adult

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  • (PMID = 19563186.001).
  • [ISSN] 0255-2930
  • [Journal-full-title] Zhongguo zhen jiu = Chinese acupuncture & moxibustion
  • [ISO-abbreviation] Zhongguo Zhen Jiu
  • [Language] chi
  • [Publication-type] English Abstract; Journal Article; Randomized Controlled Trial
  • [Publication-country] China
  • [Chemical-registry-number] 0 / Histamine H1 Antagonists; R7PLA2DM0J / Flunarizine
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26. Tashiro M, Mochizuki H, Sakurada Y, Ishii K, Oda K, Kimura Y, Sasaki T, Ishiwata K, Yanai K: Brain histamine H receptor occupancy of orally administered antihistamines measured by positron emission tomography with (11)C-doxepin in a placebo-controlled crossover study design in healthy subjects: a comparison of olopatadine and ketotifen. Br J Clin Pharmacol; 2006 Jan;61(1):16-26
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  • [Title] Brain histamine H receptor occupancy of orally administered antihistamines measured by positron emission tomography with (11)C-doxepin in a placebo-controlled crossover study design in healthy subjects: a comparison of olopatadine and ketotifen.
  • The purpose of the present study is to measure histamine H(1) receptor (H(1)R) occupancy due to olopatadine, a new second-generation antihistamine and to compare it with that of ketotifen.
  • Abbreviations histamine H(1) receptor (H(1)R), histamine H(1) receptor occupancy (H(1)RO), dopamine D(2) receptor (D(2)R), positron emission tomography (PET), blood-brain barrier (BBB), binding potential ratio (BPR), distribution volume (DV).
  • [MeSH-major] Brain / metabolism. Dibenzoxepins / administration & dosage. Histamine H1 Antagonists / administration & dosage. Ketotifen / administration & dosage. Receptors, Histamine H1 / metabolism
  • [MeSH-minor] Administration, Oral. Adult. Area Under Curve. Cross-Over Studies. Doxepin. Histamine Antagonists. Humans. Male. Olopatadine Hydrochloride. Positron-Emission Tomography / methods

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  • (PMID = 16390347.001).
  • [ISSN] 0306-5251
  • [Journal-full-title] British journal of clinical pharmacology
  • [ISO-abbreviation] Br J Clin Pharmacol
  • [Language] eng
  • [Publication-type] Clinical Trial; Comparative Study; Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Dibenzoxepins; 0 / Histamine Antagonists; 0 / Histamine H1 Antagonists; 0 / Receptors, Histamine H1; 1668-19-5 / Doxepin; 2XG66W44KF / Olopatadine Hydrochloride; X49220T18G / Ketotifen
  • [Other-IDs] NLM/ PMC1884984
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27. Niide M, Okubo Y, Irisawa R, Tsuboi R: [Clinical effects of olopatadine hydrochloride on pruritus in skin diseases]. Arerugi; 2006 Oct;55(10):1327-36
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  • [Title] [Clinical effects of olopatadine hydrochloride on pruritus in skin diseases].
  • METHODS: Five mg of olopatadine hydrochloride (Allerock) was administered to the subjects twice daily.
  • These results suggest that second generation antihistamines like olopatadine hydrochloride, which showed a prompt response to histamine, are effective against pruritus in urticaria, and that continuous use of these antihistamines is effective against pruritus in other forms of skin disease, such as asteatotic dermatitis and atopic dermatitis in which other chemical mediators besides histamine may be the triggers for pruritus.
  • [MeSH-minor] Adult. Dermatitis, Atopic / drug therapy. Dermatitis, Atopic / physiopathology. Drug Administration Schedule. Female. Humans. Male. Middle Aged. Olopatadine Hydrochloride

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  • (PMID = 17072113.001).
  • [ISSN] 0021-4884
  • [Journal-full-title] Arerugī = [Allergy]
  • [ISO-abbreviation] Arerugi
  • [Language] jpn
  • [Publication-type] English Abstract; Journal Article
  • [Publication-country] Japan
  • [Chemical-registry-number] 0 / Antipruritics; 0 / Dibenzoxepins; 2XG66W44KF / Olopatadine Hydrochloride
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28. Danarti R, Waskito F, Indrastuti N: Onset and duration of action of topical antihistamine: a study of histamine skin test response. Int J Dermatol; 2008 Aug;47(8):861-3
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  • [Title] Onset and duration of action of topical antihistamine: a study of histamine skin test response.
  • In this study, we aimed to determine the onset and duration of action of single topical AH application by observing histamine-STR suppression over time.
  • The topical AH tested was a single application of 5% doxepin hydrochloride cream, while 10 mg/ml histamine dihydrochloride was used to test the skin responses.
  • Histamine wheal response was suppressed starting on minute 90 and the wheal width were back to >/= 7 mm(2 )on minute 270.
  • Significant histamine reactivity difference between genders (P = 0.201) and atopic status (P = 1.000), which could be a source of bias in histamine STR, was not found among our subjects.
  • [MeSH-major] Doxepin / therapeutic use. Histamine H1 Antagonists / therapeutic use. Pruritus / prevention & control. Skin Tests / adverse effects

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  • (PMID = 18717873.001).
  • [ISSN] 1365-4632
  • [Journal-full-title] International journal of dermatology
  • [ISO-abbreviation] Int. J. Dermatol.
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article; Randomized Controlled Trial
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Allergens; 0 / Histamine H1 Antagonists; 1668-19-5 / Doxepin
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29. Pathak A, Rajput SJ: Simultaneous determination of a ternary mixture of doxylamine succinate, pyridoxine hydrochloride, and folic acid by the ratio spectra-zero-crossing, double divisor-ratio spectra derivative, and column high-performance liquid chromatographic methods. J AOAC Int; 2008 Sep-Oct;91(5):1059-69
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  • [Title] Simultaneous determination of a ternary mixture of doxylamine succinate, pyridoxine hydrochloride, and folic acid by the ratio spectra-zero-crossing, double divisor-ratio spectra derivative, and column high-performance liquid chromatographic methods.
  • Three simple, rapid, and accurate methods, i.e., the derivative ratio spectra-zero-crossing method (method I), double divisor-ratio spectra derivative method (method II), and column reversed-phase high-performance liquid chromatographic (RP-HPLC) method (method III) were developed for the simultaneous determination of doxylamine succinate (DOX), pyridoxine hydrochloride (PYR), and folic acid (FA) in their ternary mixtures and in tablets.
  • [MeSH-major] Doxylamine / analogs & derivatives. Folic Acid / analysis. Histamine H1 Antagonists / analysis. Pyridoxine / analysis. Vitamins / analysis

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  • (PMID = 18980119.001).
  • [ISSN] 1060-3271
  • [Journal-full-title] Journal of AOAC International
  • [ISO-abbreviation] J AOAC Int
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Histamine H1 Antagonists; 0 / Indicators and Reagents; 0 / Solutions; 0 / Tablets; 0 / Vitamins; 935E97BOY8 / Folic Acid; 95QB77JKPL / Doxylamine; KV2JZ1BI6Z / Pyridoxine; V9BI9B5YI2 / doxylamine succinate
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30. Hori M, Iwama T, Asakura Y, Kawanishi M, Kamon J, Hoshino A, Takahashi S, Takahashi K, Nakaike S, Tsuruzoe N: NT-702 (parogrelil hydrochloride, NM-702), a novel and potent phosphodiesterase 3 inhibitor, suppress the asthmatic response in guinea pigs, with both bronchodilating and anti-inflammatory effects. Eur J Pharmacol; 2009 Sep 15;618(1-3):63-9
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  • [Title] NT-702 (parogrelil hydrochloride, NM-702), a novel and potent phosphodiesterase 3 inhibitor, suppress the asthmatic response in guinea pigs, with both bronchodilating and anti-inflammatory effects.
  • We evaluated the effects of NT-702 (parogrelil hydrochloride, NM-702, 4-bromo-6-[3-(4-chlorophenyl) propoxy]-5-[(pyridine-3-ylmethyl) amino] pyridazin-3(2H)-one hydrochloride), a selective phosphodiesterase 3 inhibitor, on the asthmatic response in guinea pigs.
  • Leukotriene (LT) D(4)- and histamine-induced contraction of isolated guinea pig tracheal strips was inhibited by NT-702, with EC(50) values of 3.2 x 10(-7) and 2.5 x 10(-7)M, respectively.
  • [MeSH-minor] Animals. Antigens / immunology. Bronchoconstriction / drug effects. Bronchoconstriction / immunology. Cell Movement / drug effects. Cyclic AMP / metabolism. Dinoprostone / pharmacology. Guinea Pigs. Histamine / pharmacology. In Vitro Techniques. Leukotriene D4 / pharmacology. Lung / drug effects. Lung / pathology. Male. Muscle Contraction / drug effects. Muscle, Smooth / drug effects. Muscle, Smooth / physiopathology. Trachea / drug effects

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  • (PMID = 19616537.001).
  • [ISSN] 1879-0712
  • [Journal-full-title] European journal of pharmacology
  • [ISO-abbreviation] Eur. J. Pharmacol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / 4-bromo-6-(3-(4-chlorophenyl)propoxy)-5-(3-pyridylmethylamino)-3(2H)-pyridazinone hydrochloride; 0 / Anti-Inflammatory Agents; 0 / Antigens; 0 / Bronchodilator Agents; 0 / Enzyme Inhibitors; 0 / Phosphodiesterase 3 Inhibitors; 0 / Pyridazines; 73836-78-9 / Leukotriene D4; 820484N8I3 / Histamine; E0399OZS9N / Cyclic AMP; K7Q1JQR04M / Dinoprostone
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31. Shen J, Tanida M, Yao JF, Niijima A, Nagai K: Biphasic effects of orexin-A on autonomic nerve activity and lipolysis. Neurosci Lett; 2008 Oct 24;444(2):166-71
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  • The effect of the high dose of orexin-A (1 microg/rat) was eliminated by pretreatment with diphenhydramine hydrochloride, a histamine H(1) receptor antagonist.
  • In contrast, the effect of the low dose of orexin-A (10 ng/rat) was suppressed by thioperamide maleate salt, a histamine H(3) receptor antagonist.
  • The effect of 1 microg/rat of orexin-A on plasma FFA was eliminated by propranolol hydrochloride, a beta-adrenergic receptor blocker, and also by diphenhydramine.
  • Our results suggest that high doses of orexin-A may regulate the lipolytic processes in adipose tissue through facilitation of the sympathetic nervous system, which is driven by histamine neurons through the H(1) receptor, and that the beta(3)-receptor may be involved in this enhanced lipolytic response.
  • [MeSH-minor] Adrenergic beta-3 Receptor Antagonists. Amino Acid Sequence. Animals. Atropine / pharmacology. Diphenhydramine / pharmacology. Histamine Antagonists / pharmacology. Injections, Intraventricular. Male. Molecular Sequence Data. Muscarinic Antagonists / pharmacology. Orexins. Piperidines / pharmacology. Rats. Rats, Wistar. Receptors, Adrenergic, beta-3 / physiology. Receptors, Histamine H1 / physiology. Receptors, Histamine H3 / physiology. Receptors, Muscarinic / physiology

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  • (PMID = 18755242.001).
  • [ISSN] 0304-3940
  • [Journal-full-title] Neuroscience letters
  • [ISO-abbreviation] Neurosci. Lett.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Ireland
  • [Chemical-registry-number] 0 / Adrenergic beta-3 Receptor Antagonists; 0 / Histamine Antagonists; 0 / Intracellular Signaling Peptides and Proteins; 0 / Muscarinic Antagonists; 0 / Neuropeptides; 0 / Orexins; 0 / Piperidines; 0 / Receptors, Adrenergic, beta-3; 0 / Receptors, Histamine H1; 0 / Receptors, Histamine H3; 0 / Receptors, Muscarinic; 106243-16-7 / thioperamide; 7C0697DR9I / Atropine; 8GTS82S83M / Diphenhydramine
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32. She X, Wu L, Wei H, Liu W, Chen Y: Determination of oxatomide in human plasma by high-performance liquid chromatography-electrospray ionization mass spectrometry. Biomed Chromatogr; 2008 Jul;22(7):746-52
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  • Flunarizine hydrochloride was employed as the internal standard (IS).
  • [MeSH-minor] Administration, Oral. Anti-Allergic Agents / blood. Anti-Allergic Agents / chemistry. Anti-Allergic Agents / pharmacokinetics. Flunarizine / blood. Histamine H1 Antagonists / blood. Histamine H1 Antagonists / chemistry. Histamine H1 Antagonists / pharmacokinetics. Humans. Linear Models. Male. Sensitivity and Specificity

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  • (PMID = 18348338.001).
  • [ISSN] 0269-3879
  • [Journal-full-title] Biomedical chromatography : BMC
  • [ISO-abbreviation] Biomed. Chromatogr.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't; Validation Studies
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Anti-Allergic Agents; 0 / Histamine H1 Antagonists; 0 / Piperazines; J31IL9Z2EE / oxatomide; R7PLA2DM0J / Flunarizine
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33. Bendas ER, Ayres JW: Leaky enteric coating on ranitidine hydrochloride beads: dissolution and prediction of plasma data. Eur J Pharm Biopharm; 2008 Aug;69(3):977-85
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  • [Title] Leaky enteric coating on ranitidine hydrochloride beads: dissolution and prediction of plasma data.
  • The present research is based on the hypothesis that leaky enteric-coated pellets formulations are able to provide sustained input for drugs that have an absorption window, such as ranitidine hydrochloride, without jeopardizing their bioavailability.
  • Predictions of plasma concentration-time profiles of the model drug ranitidine hydrochloride from leaky enteric-coated pellets in fasted conditions and from immediate-release formulations were performed using computer simulations.
  • [MeSH-major] Histamine H2 Antagonists / administration & dosage. Ranitidine / administration & dosage

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  • (PMID = 18424095.001).
  • [ISSN] 0939-6411
  • [Journal-full-title] European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e.V
  • [ISO-abbreviation] Eur J Pharm Biopharm
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / Excipients; 0 / Histamine H2 Antagonists; 0 / Tablets, Enteric-Coated; 30IQX730WE / Polyethylene Glycols; 884KT10YB7 / Ranitidine; J2B2A4N98G / Lactose
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34. Chieng N, Aaltonen J, Saville D, Rades T: Physical characterization and stability of amorphous indomethacin and ranitidine hydrochloride binary systems prepared by mechanical activation. Eur J Pharm Biopharm; 2009 Jan;71(1):47-54
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  • [Title] Physical characterization and stability of amorphous indomethacin and ranitidine hydrochloride binary systems prepared by mechanical activation.
  • Co-milling of gamma-indomethacin and ranitidine hydrochloride form 2 at various weight ratios (1:2, 1:1 and 2:1) was investigated with a particular interest in the physicochemical properties and the stability of the milled mixed amorphous form.
  • Results showed that both indomethacin and ranitidine hydrochloride were fully converted into the amorphous state after 60 min of co-milling.
  • During co-milling, the XRPD characteristic peaks of indomethacin were found to decrease faster than those of ranitidine hydrochloride.
  • DRIFTS spectra of the co-milled amorphous samples showed peaks at 1610, 1679 and 1723 cm(-1), that were not present in the individually milled samples and that are indicative of an interaction at the carboxylic acid carbonyl (HO-C=O) and benzonyl amide (N=CO) of the indomethacin molecule with the aci-nitro (C=N) of ranitidine hydrochloride.
  • Although XRPD, DSC and DRIFTS suggested an interaction between the two drugs, co-crystal formation was not observed between indomethacin and ranitidine hydrochloride.
  • [MeSH-major] Anti-Inflammatory Agents, Non-Steroidal / chemistry. Histamine H2 Antagonists / chemistry. Indomethacin / chemistry. Ranitidine / chemistry

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  • (PMID = 18644443.001).
  • [ISSN] 1873-3441
  • [Journal-full-title] European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e.V
  • [ISO-abbreviation] Eur J Pharm Biopharm
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / Anti-Inflammatory Agents, Non-Steroidal; 0 / Histamine H2 Antagonists; 884KT10YB7 / Ranitidine; XXE1CET956 / Indomethacin
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35. Gulati A, Tiwary AK, Jain S, Moudgil P, Gupta A: Intrasperm Ca2+ modulation and human ejaculated sperm viability: influence of miconazole, clotrimazole and loperamide. J Pharm Pharmacol; 2006 Aug;58(8):1145-51
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  • Miconazole nitrate, clotrimazole and loperamide hydrochloride produced a dose- and time-dependent decrease in viability, each requiring respectively 0.5, 1.0 and 1.0 mM for producing death of all sperm cells immediately upon addition to ejaculated human semen samples.
  • Synergism of spermicidal activity and intrasperm Ca(2+) elevation by miconazole or clotrimazole was observed when Ca(2+) efflux from sperm cells was simultaneously inhibited by 2',4'-dichlorobenzamil hydrochloride, a Na(+)-Ca(2+) exchange inhibitor.
  • [MeSH-minor] Adult. Amiloride / analogs & derivatives. Amiloride / pharmacology. Drug Compounding. Drug Synergism. Histamine / pharmacology. Humans. In Vitro Techniques. Male. Pharmaceutical Solutions. Sperm Motility / drug effects

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  • (PMID = 16872563.001).
  • [ISSN] 0022-3573
  • [Journal-full-title] The Journal of pharmacy and pharmacology
  • [ISO-abbreviation] J. Pharm. Pharmacol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Antidiarrheals; 0 / Antifungal Agents; 0 / Pharmaceutical Solutions; 0 / Spermatocidal Agents; 1166-01-4 / 3',4'-dichlorobenzamil; 6X9OC3H4II / Loperamide; 7DZO8EB0Z3 / Amiloride; 7NNO0D7S5M / Miconazole; 820484N8I3 / Histamine; G07GZ97H65 / Clotrimazole; SY7Q814VUP / Calcium
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36. Izu K, Tokura Y: The various effects of four H1-antagonists on serum substance P levels in patients with atopic dermatitis. J Dermatol; 2005 Oct;32(10):776-81
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  • [MeSH-major] Anti-Allergic Agents / therapeutic use. Dermatitis, Atopic / blood. Histamine H1 Antagonists / therapeutic use. Substance P / blood
  • [MeSH-minor] Adult. Cetirizine / therapeutic use. Dibenzazepines / therapeutic use. Dibenzoxepins / therapeutic use. E-Selectin / blood. Female. Humans. Imidazoles / therapeutic use. Intercellular Adhesion Molecule-1 / blood. Male. Olopatadine Hydrochloride. Terfenadine / analogs & derivatives. Terfenadine / therapeutic use. Vascular Cell Adhesion Molecule-1 / blood

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  • (PMID = 16361727.001).
  • [ISSN] 0385-2407
  • [Journal-full-title] The Journal of dermatology
  • [ISO-abbreviation] J. Dermatol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Japan
  • [Chemical-registry-number] 0 / Anti-Allergic Agents; 0 / Dibenzazepines; 0 / Dibenzoxepins; 0 / E-Selectin; 0 / Histamine H1 Antagonists; 0 / Imidazoles; 0 / Vascular Cell Adhesion Molecule-1; 126547-89-5 / Intercellular Adhesion Molecule-1; 2XG66W44KF / Olopatadine Hydrochloride; 33507-63-0 / Substance P; 7BA5G9Y06Q / Terfenadine; E6582LOH6V / fexofenadine; Q13WX941EF / epinastine; YO7261ME24 / Cetirizine
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37. Bhise K, Shaikh S, Bora D: Taste mask, design and evaluation of an oral formulation using ion exchange resin as drug carrier. AAPS PharmSciTech; 2008;9(2):557-62
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  • The purpose of this research was to mask the bitter taste of Diphenhydramine Hydrochloride (DPH) using cation exchange resins.
  • [MeSH-major] Cation Exchange Resins / administration & dosage. Diphenhydramine / administration & dosage. Drug Carriers. Histamine H1 Antagonists / administration & dosage. Perceptual Masking. Taste / drug effects

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  • [Cites] Int J Pharm. 2000 Apr 20;199(2):151-8 [10802408.001]
  • [Cites] Int J Pharm. 2001 Mar 23;216(1-2):67-76 [11274808.001]
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  • (PMID = 18491233.001).
  • [ISSN] 1530-9932
  • [Journal-full-title] AAPS PharmSciTech
  • [ISO-abbreviation] AAPS PharmSciTech
  • [Language] eng
  • [Publication-type] Evaluation Studies; Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Cation Exchange Resins; 0 / Drug Carriers; 0 / Histamine H1 Antagonists; 0 / Tablets; 8GTS82S83M / Diphenhydramine
  • [Other-IDs] NLM/ PMC2976952
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38. Shimizu M, Fuse K, Okudaira K, Nishigaki R, Maeda K, Kusuhara H, Sugiyama Y: Contribution of OATP (organic anion-transporting polypeptide) family transporters to the hepatic uptake of fexofenadine in humans. Drug Metab Dispos; 2005 Oct;33(10):1477-81
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  • Fexofenadine hydrochloride (FEX), a second generation H(1)-receptor antagonist, is mainly eliminated from the liver into bile in unchanged form.
  • [MeSH-major] Histamine H1 Antagonists / pharmacology. Organic Anion Transport Protein 1 / metabolism. Terfenadine / analogs & derivatives

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  • (PMID = 16014768.001).
  • [ISSN] 0090-9556
  • [Journal-full-title] Drug metabolism and disposition: the biological fate of chemicals
  • [ISO-abbreviation] Drug Metab. Dispos.
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Histamine H1 Antagonists; 0 / Organic Anion Transport Polypeptide C; 0 / Organic Anion Transport Protein 1; 1806-98-0 / estradiol-17 beta-glucuronide; 2DI9HA706A / Estrone; 4TI98Z838E / Estradiol; 7BA5G9Y06Q / Terfenadine; E6582LOH6V / fexofenadine; M03GIQ7Z6P / Sincalide; QTL48N278K / estrone sulfate
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39. Yamaguchi J, Aihara M, Kobayashi Y, Kambara T, Ikezawa Z: Quantitative analysis of nerve growth factor (NGF) in the atopic dermatitis and psoriasis horny layer and effect of treatment on NGF in atopic dermatitis. J Dermatol Sci; 2009 Jan;53(1):48-54
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  • The NGF level decreased significantly at 2 and 4 weeks of treatment with olopatadine, a histamine H(1) receptor antagonist, and/or topical steroid.
  • [MeSH-major] Dermatitis, Atopic / drug therapy. Dermatitis, Atopic / metabolism. Dibenzoxepins / therapeutic use. Histamine H1 Antagonists, Non-Sedating / therapeutic use. Nerve Growth Factor / metabolism. Psoriasis / metabolism
  • [MeSH-minor] Adult. Case-Control Studies. Epidermis / drug effects. Epidermis / metabolism. Epidermis / pathology. Female. Humans. Immunoglobulin E / blood. L-Lactate Dehydrogenase / blood. Male. Olopatadine Hydrochloride. Pruritus / etiology. Pruritus / metabolism. Pruritus / pathology. Severity of Illness Index. Treatment Outcome

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  • (PMID = 18922683.001).
  • [ISSN] 0923-1811
  • [Journal-full-title] Journal of dermatological science
  • [ISO-abbreviation] J. Dermatol. Sci.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / Dibenzoxepins; 0 / Histamine H1 Antagonists, Non-Sedating; 2XG66W44KF / Olopatadine Hydrochloride; 37341-29-0 / Immunoglobulin E; 9061-61-4 / Nerve Growth Factor; EC 1.1.1.27 / L-Lactate Dehydrogenase
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40. Arayne MS, Sultana N, Mirza AZ, Siddiqui FA: Simultaneous determination of gliquidone, fexofenadine, buclizine, and levocetirizine in dosage formulation and human serum by RP-HPLC. J Chromatogr Sci; 2010 May-Jun;48(5):382-5
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  • In the present paper, a simultaneous method has been developed and validated for estimation of gliquidone in the presence of H(1)-receptor antagonists (fexofenadine hydrochloride, buclizine hydrochloride, and levocetirizine dihydrochloride) using reversed-phase high-performance liquid chromatographic technique.
  • The linearity of the calibration curves for gliquidone, fexofenadine hydrochloride, buclizine hydrochloride, and levocetirizine dihydrochloride were found to be 0.338-50 microg/mL (r = 0.9964), 5-50 microg/mL (r = 0.9956), 0.325-50 microg/mL (r = 0.9967), and 0.553-50 microg/mL (r = 0.9950), respectively.
  • [MeSH-major] Cetirizine / blood. Chromatography, High Pressure Liquid / methods. Histamine H1 Antagonists / blood. Piperazines / blood. Sulfonylurea Compounds / blood. Terfenadine / analogs & derivatives

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  • (PMID = 20515533.001).
  • [ISSN] 1945-239X
  • [Journal-full-title] Journal of chromatographic science
  • [ISO-abbreviation] J Chromatogr Sci
  • [Language] eng
  • [Publication-type] Evaluation Studies; Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Dosage Forms; 0 / Histamine H1 Antagonists; 0 / Piperazines; 0 / Sulfonylurea Compounds; 0C94V6X681 / buclizine; 6U5EA9RT2O / levocetirizine; 7BA5G9Y06Q / Terfenadine; C7C2QDD75P / gliquidone; E6582LOH6V / fexofenadine; YO7261ME24 / Cetirizine
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41. Karakuş S, Küçükgüzel I, Küçükgüzel SG: Development and validation of a rapid RP-HPLC method for the determination of cetirizine or fexofenadine with pseudoephedrine in binary pharmaceutical dosage forms. J Pharm Biomed Anal; 2008 Jan 22;46(2):295-302
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  • The objective of the current study was to develop a simple, accurate, precise and rapid reversed-phase HPLC method and subsequent validation using ICH suggested approach for the determination of antihistaminic-decongestant pharmaceutical dosage forms containing binary mixtures of pseudoephedrine hydrochloride (PSE) with fexofenadine hydrochloride (FEX) or cetirizine dihydrochloride (CET).
  • [MeSH-major] Cetirizine / analysis. Chromatography, High Pressure Liquid / methods. Histamine H1 Antagonists / analysis. Pharmaceutical Preparations / chemistry. Pseudoephedrine / analysis. Terfenadine / analogs & derivatives

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  • (PMID = 18054459.001).
  • [ISSN] 0731-7085
  • [Journal-full-title] Journal of pharmaceutical and biomedical analysis
  • [ISO-abbreviation] J Pharm Biomed Anal
  • [Language] eng
  • [Publication-type] Journal Article; Validation Studies
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Dosage Forms; 0 / Histamine H1 Antagonists; 0 / Pharmaceutical Preparations; 7BA5G9Y06Q / Terfenadine; 7CUC9DDI9F / Pseudoephedrine; E6582LOH6V / fexofenadine; YO7261ME24 / Cetirizine
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42. Lapa GB, Mathews TA, Harp J, Budygin EA, Jones SR: Diphenylpyraline, a histamine H1 receptor antagonist, has psychostimulant properties. Eur J Pharmacol; 2005 Jan 4;506(3):237-40
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  • [Title] Diphenylpyraline, a histamine H1 receptor antagonist, has psychostimulant properties.
  • Diphenylpyraline hydrochloride (DPP) is used clinically as an antihistamine drug, but its neurobiological effects are not completely understood.
  • [MeSH-major] Histamine H1 Antagonists / pharmacology. Motor Activity / drug effects. Piperidines / pharmacology. Receptors, Histamine H1 / physiology

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  • (PMID = 15627433.001).
  • [ISSN] 0014-2999
  • [Journal-full-title] European journal of pharmacology
  • [ISO-abbreviation] Eur. J. Pharmacol.
  • [Language] eng
  • [Grant] United States / NIAAA NIH HHS / AA / AA014091; United States / NIMHD NIH HHS / MD / MD00232
  • [Publication-type] Comparative Study; Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / Central Nervous System Stimulants; 0 / Histamine H1 Antagonists; 0 / Piperidines; 0 / Receptors, Histamine H1; 33361OE3AV / diphenylpyraline
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43. Enomoto T, Ide T, Ogino S: Construction of an environmental exposure unit and investigation of the effects of cetirizine hydrochloride on symptoms of cedar pollinosis in Japan. J Investig Allergol Clin Immunol; 2007;17(3):173-81
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  • [Title] Construction of an environmental exposure unit and investigation of the effects of cetirizine hydrochloride on symptoms of cedar pollinosis in Japan.
  • In the clinical study, 20 volunteers with known cedar pollinosis were exposed to pollen for 5 hours, randomly allocated to receive either cetirizine hydrochloride or placebo 30 minutes after exposure.
  • Test drugs were administered 30 minutes after exposure, and 1 hour later patients in the cetirizine hydrochloride group experienced a significant decrease in sneezing, nose-blowing frequency, and nasal congestion compared with the placebo group.
  • [MeSH-major] Cetirizine / therapeutic use. Environmental Exposure. Histamine H1 Antagonists, Non-Sedating / therapeutic use. Hypersensitivity, Immediate / drug therapy. Immunologic Tests / methods

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  • (PMID = 17583105.001).
  • [ISSN] 1018-9068
  • [Journal-full-title] Journal of investigational allergology & clinical immunology
  • [ISO-abbreviation] J Investig Allergol Clin Immunol
  • [Language] eng
  • [Publication-type] Clinical Trial; Journal Article; Randomized Controlled Trial
  • [Publication-country] Spain
  • [Chemical-registry-number] 0 / Histamine H1 Antagonists, Non-Sedating; YO7261ME24 / Cetirizine
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44. Kaliner MA, Oppenheimer J, Farrar JR: Comprehensive review of olopatadine: the molecule and its clinical entities. Allergy Asthma Proc; 2010 Mar-Apr;31(2):112-9
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  • [Title] Comprehensive review of olopatadine: the molecule and its clinical entities.
  • Olopatadine is a tricyclic compound with antihistaminic, mast cell-stabilizing, and anti-inflammatory properties.
  • In the United States olopatadine is approved as a b.i.d. ophthalmic solution, Patanol (Alcon Laboratories, Inc., Fort Worth, TX) to treat all signs and symptoms of allergic conjunctivitis and as a q.d. formulation, Pataday (Alcon Laboratories, Inc.
  • ), to treat itching associated with allergic conjunctivitis.
  • A nasal spray, Patanase (Alcon Laboratories, Inc.
  • ), was approved in 2008 for treatment of the symptoms of seasonal allergic rhinitis.
  • The available data on olopatadine was assessed with regard to future uses through a comprehensive literature review and a Roundtable Discussion held at the 2009 meeting of the American Academy of Allergy Asthma and Immunology.
  • The unique mechanisms of action of olopatadine still under study include mast cell stabilization, potent H(1)-anthistaminic activity, and anti-inflammatory effects.
  • Data support consideration of nasal olopatadine for as-needed use for episodic symptoms of allergic rhinitis, for treatment of nonallergic rhinitis, and for use in combination with topical steroids for patients with moderate-to-severe allergy symptoms.

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  • (PMID = 20406593.001).
  • [ISSN] 1539-6304
  • [Journal-full-title] Allergy and asthma proceedings
  • [ISO-abbreviation] Allergy Asthma Proc
  • [Language] ENG
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't; Review
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Anti-Inflammatory Agents; 0 / Dibenzoxepins; 0 / Dosage Forms; 0 / Histamine H1 Antagonists, Non-Sedating; 2XG66W44KF / Olopatadine Hydrochloride
  • [Number-of-references] 47
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45. Morita E, Matsuo H, Zhang Y: Double-blind, crossover comparison of olopatadine and cetirizine versus placebo: suppressive effects on skin response to histamine iontophoresis. J Dermatol; 2005 Jan;32(1):58-61
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  • [Title] Double-blind, crossover comparison of olopatadine and cetirizine versus placebo: suppressive effects on skin response to histamine iontophoresis.
  • Olopathadine, a newly developed histamine H1-receptor antagonist, was compared with cetirizine in its suppressive effects on histamine-induced wheal and flare reaction using an iontophoresis technique in a double-blind, crossover, placebo-controlled fashion.
  • [MeSH-major] Cetirizine / administration & dosage. Dibenzoxepins / administration & dosage. Histamine H1 Antagonists / administration & dosage. Hypersensitivity, Immediate / drug therapy
  • [MeSH-minor] Administration, Oral. Adult. Cross-Over Studies. Double-Blind Method. Female. Histamine. Humans. Iontophoresis. Male. Olopatadine Hydrochloride. Time Factors. Treatment Outcome

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  • (PMID = 15841664.001).
  • [ISSN] 0385-2407
  • [Journal-full-title] The Journal of dermatology
  • [ISO-abbreviation] J. Dermatol.
  • [Language] eng
  • [Publication-type] Clinical Trial; Comparative Study; Journal Article; Randomized Controlled Trial
  • [Publication-country] Japan
  • [Chemical-registry-number] 0 / Dibenzoxepins; 0 / Histamine H1 Antagonists; 2XG66W44KF / Olopatadine Hydrochloride; 820484N8I3 / Histamine; YO7261ME24 / Cetirizine
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46. Darwish IA, Hussein SA, Mahmoud AM, Hassan AI: A sensitive spectrophotometric method for the determination of H2-receptor antagonists by means of N-bromosuccinimide and p-aminophenol. Acta Pharm; 2008 Mar;58(1):87-97
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  • A simple, accurate and sensitive spectrophotometric method for determination of H2-receptor antagonists: cimetidine (CIM), famotidine (FAM), nizatidine (NIZ), and ranitidine hydrochloride (RAN) has been fully developed and validated.
  • [MeSH-major] Aminophenols. Bromosuccinimide. Histamine H2 Antagonists / analysis. Spectrophotometry / methods

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  • (PMID = 18337210.001).
  • [ISSN] 1846-9558
  • [Journal-full-title] Acta pharmaceutica (Zagreb, Croatia)
  • [ISO-abbreviation] Acta Pharm
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Croatia
  • [Chemical-registry-number] 0 / Aminophenols; 0 / Dosage Forms; 0 / Histamine H2 Antagonists; K8G1F2UCJF / Bromosuccinimide; R7P8FRP05V / 4-aminophenol
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47. Tamura T, Matsubara M, Hasegawa K, Ohmori K, Karasawa A: Olopatadine hydrochloride suppresses the rebound phenomenon after discontinuation of treatment with a topical steroid in mice with chronic contact hypersensitivity. Clin Exp Allergy; 2005 Jan;35(1):97-103
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  • [Title] Olopatadine hydrochloride suppresses the rebound phenomenon after discontinuation of treatment with a topical steroid in mice with chronic contact hypersensitivity.
  • BACKGROUND: Olopatadine hydrochloride (olopatadine; Allelock) is one of the second-generation antihistamines that are treated for allergic disorders such as rhinitis, urticaria and eczema dermatitis.
  • The effects of olopatadine were quantified by measurements of ear-swelling, and levels of cytokines and histamine in the lesioned ear.
  • Results Topical prednisolone (0.05 mg/ear/day) significantly inhibited the increases in ear swelling and production of IL-1beta, IL-4, IL-18, granulocyte-macrophage colony-stimulating factor (GM-CSF) and histamine.
  • The sequential treatment with olopatadine (10 mg/kg/day) after discontinuation of the treatment with topical prednisolone alone, or topical prednisolone with olopatadine, significantly inhibited the increases in ear swelling and levels of IL-1beta, IL-4, IL-18, GM-CSF, nerve growth factor and histamine.
  • [MeSH-major] Dermatitis, Contact / drug therapy. Dibenzoxepins / therapeutic use. Histamine H1 Antagonists / therapeutic use. Substance Withdrawal Syndrome / drug therapy
  • [MeSH-minor] Animals. Chronic Disease. Glucocorticoids / therapeutic use. Interleukin-4 / immunology. Male. Mice. Mice, Inbred BALB C. Models, Animal. Olopatadine Hydrochloride. Prednisolone / therapeutic use. Recurrence

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  • (PMID = 15649273.001).
  • [ISSN] 0954-7894
  • [Journal-full-title] Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology
  • [ISO-abbreviation] Clin. Exp. Allergy
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Dibenzoxepins; 0 / Glucocorticoids; 0 / Histamine H1 Antagonists; 207137-56-2 / Interleukin-4; 2XG66W44KF / Olopatadine Hydrochloride; 9PHQ9Y1OLM / Prednisolone
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48. Medhurst SJ, Collins SD, Billinton A, Bingham S, Dalziel RG, Brass A, Roberts JC, Medhurst AD, Chessell IP: Novel histamine H3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and virally-induced rat models of neuropathic pain. Pain; 2008 Aug 15;138(1):61-9
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  • [Title] Novel histamine H3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and virally-induced rat models of neuropathic pain.
  • Several studies have implicated a potential role for histamine H(3) receptors in pain processing, although the data are somewhat conflicting.
  • In the present study we investigated the effects of the novel potent and highly selective H(3) receptor antagonists GSK189254 (6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide hydrochloride) and GSK334429 (1-(1-methylethyl)-4-([1-[6-(trifluoromethyl)-3-pyridinyl]-4-piperidinyl]carbonyl)hexahydro-1H-1,4-diazepine) in two rat models of neuropathic pain, namely the chronic constriction injury (CCI) model and the varicella-zoster virus (VZV) model.
  • [MeSH-major] Azepines / administration & dosage. Benzazepines / administration & dosage. Disease Models, Animal. Histamine H3 Antagonists / administration & dosage. Neuralgia / drug therapy. Neuralgia / metabolism. Niacinamide / analogs & derivatives. Pain Measurement / drug effects. Pyridines / administration & dosage. Receptors, Histamine H3 / metabolism. Spinal Cord / metabolism

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  • (PMID = 18164820.001).
  • [ISSN] 1872-6623
  • [Journal-full-title] Pain
  • [ISO-abbreviation] Pain
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / 1-(1-methylethyl)-4-((1-(6-(trifluoromethyl)-3-pyridinyl)-4-piperidinyl)carbonyl)hexahydro-1H-1,4-diazepine; 0 / 6-((3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy)-N-methyl-3-pyridinecarboxamide; 0 / Azepines; 0 / Benzazepines; 0 / Histamine H3 Antagonists; 0 / Pyridines; 0 / Receptors, Histamine H3; 25X51I8RD4 / Niacinamide
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49. Schoch C: Effect of ketotifen fumarate, olopatadine, and levocabastine on ocular active anaphylaxis in the guinea pig and ocular immediate hypersensitivity in the albino rat. Ocul Immunol Inflamm; 2005 Feb;13(1):39-44
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  • [MeSH-major] Anaphylaxis / drug therapy. Conjunctivitis, Allergic / drug therapy. Dibenzoxepins / therapeutic use. Histamine H1 Antagonists / therapeutic use. Ketotifen / therapeutic use. Piperidines / therapeutic use
  • [MeSH-minor] Animals. Capillary Permeability / drug effects. Disease Models, Animal. Edema / drug therapy. Eyelids / blood supply. Guinea Pigs. Male. Olopatadine Hydrochloride. Ophthalmic Solutions / therapeutic use. Ovalbumin. Rats

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  • (PMID = 15804768.001).
  • [ISSN] 0927-3948
  • [Journal-full-title] Ocular immunology and inflammation
  • [ISO-abbreviation] Ocul. Immunol. Inflamm.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / Dibenzoxepins; 0 / Histamine H1 Antagonists; 0 / Ophthalmic Solutions; 0 / Piperidines; 2XG66W44KF / Olopatadine Hydrochloride; 9006-59-1 / Ovalbumin; H68BP06S81 / levocabastine; X49220T18G / Ketotifen
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50. Darwish IA, Hussein SA, Mahmoud AM, Hassan AI: Spectrophotometric determination of H(2)-receptor antagonists via their oxidation with cerium(IV). Spectrochim Acta A Mol Biomol Spectrosc; 2008 Jan;69(1):33-40
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  • A simple, accurate and sensitive spectrophotometric method has been developed and validated for determination of H(2)-receptor antagonists: cimetidine, famotidine, nizatidine and ranitidine hydrochloride.
  • [MeSH-major] Cerium / metabolism. Histamine H2 Antagonists / analysis. Histamine H2 Antagonists / metabolism

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  • (PMID = 17442613.001).
  • [ISSN] 1386-1425
  • [Journal-full-title] Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy
  • [ISO-abbreviation] Spectrochim Acta A Mol Biomol Spectrosc
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Aminobenzoates; 0 / Dosage Forms; 0 / Excipients; 0 / Histamine H2 Antagonists; 0 / Solvents; 30K4522N6T / Cerium; 5QZO15J2Z8 / Famotidine; 80061L1WGD / Cimetidine; 884KT10YB7 / Ranitidine; P41PML4GHR / Nizatidine
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51. Oliveira DC, Weigch A, Rolim CM: Simple and reliable HPLC analysis of fexofenadine hydrochloride in tablets and its application to dissolution studies. Pharmazie; 2007 Feb;62(2):96-100
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  • [Title] Simple and reliable HPLC analysis of fexofenadine hydrochloride in tablets and its application to dissolution studies.
  • A simple RP-HPLC method using a PDA detector was developed and validated for the analysis and dissolution studies of fexofenadine hydrochloride (FEX) in dosage forms.
  • [MeSH-major] Histamine H1 Antagonists / analysis. Terfenadine / analogs & derivatives

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  • (PMID = 17341026.001).
  • [ISSN] 0031-7144
  • [Journal-full-title] Die Pharmazie
  • [ISO-abbreviation] Pharmazie
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Chemical-registry-number] 0 / Histamine H1 Antagonists; 0 / Tablets; 7BA5G9Y06Q / Terfenadine; E6582LOH6V / fexofenadine
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52. Suuronen T, Nuutinen T, Huuskonen J, Ojala J, Thornell A, Salminen A: Anti-inflammatory effect of selective estrogen receptor modulators (SERMs) in microglial cells. Inflamm Res; 2005 May;54(5):194-203
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [MeSH-minor] Animals. Astrocytes / cytology. Blotting, Northern. Cell Proliferation. Cells, Cultured. CpG Islands. DNA / metabolism. Dose-Response Relationship, Drug. Down-Regulation. Enzyme-Linked Immunosorbent Assay. Estradiol / analogs & derivatives. Estradiol / metabolism. Estradiol / pharmacology. Hippocampus / cytology. Histone Deacetylase Inhibitors. Histone Deacetylases / metabolism. Humans. Interleukin-6 / blood. Interleukin-6 / metabolism. L-Lactate Dehydrogenase / metabolism. Lipopolysaccharides / metabolism. Mice. Nitric Oxide / metabolism. Oligonucleotides / metabolism. Protein Binding. RNA, Messenger / metabolism. Raloxifene Hydrochloride / pharmacology. Rats. Rats, Wistar. Tamoxifen / pharmacology. Time Factors

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  • (PMID = 15953991.001).
  • [ISSN] 1023-3830
  • [Journal-full-title] Inflammation research : official journal of the European Histamine Research Society ... [et al.]
  • [ISO-abbreviation] Inflamm. Res.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] Switzerland
  • [Chemical-registry-number] 0 / Anti-Inflammatory Agents; 0 / Histone Deacetylase Inhibitors; 0 / Interleukin-6; 0 / Lipopolysaccharides; 0 / Oligonucleotides; 0 / RNA, Messenger; 0 / Selective Estrogen Receptor Modulators; 094ZI81Y45 / Tamoxifen; 22X328QOC4 / fulvestrant; 31C4KY9ESH / Nitric Oxide; 4F86W47BR6 / Raloxifene Hydrochloride; 4TI98Z838E / Estradiol; 9007-49-2 / DNA; EC 1.1.1.27 / L-Lactate Dehydrogenase; EC 3.5.1.98 / Histone Deacetylases
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53. Watanabe C, Orito T, Watanabe H, Mizoguchi H, Yonezawa A, Yanai K, Mobarakeh JI, Onodera K, Sakurada T, Sakurada S: Intrathecal high-dose histamine induces spinally-mediated nociceptive behavioral responses through a polyamine site of NMDA receptors. Eur J Pharmacol; 2008 Feb 26;581(1-2):54-63
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  • [Title] Intrathecal high-dose histamine induces spinally-mediated nociceptive behavioral responses through a polyamine site of NMDA receptors.
  • Previous research has demonstrated that a high dose of histamine (1600 pmol) injected i.t. in mice can evoke nociceptive behaviors consisting of biting/licking along with occasional scratching.
  • The present study was undertaken to examine the involvement of spinal N-methyl-d-aspartate (NMDA) and histamine H(1) and H(2) receptors in the nociceptive behaviors evoked by high-dose histamine.
  • Co-administration of the histamine H(1) receptor antagonists, d-chlorpheniramine and pyrilamine, or the histamine H(2) receptor antagonists, ranitidine and zolantidine, failed to suppress the histamine-evoked nociceptive behaviors.
  • Moreover, following histamine administration, nociceptive behaviors in histamine H(1) receptor-knockout and histamine H(2) receptor-knockout mice were indistinguishable from those in wild-type mice, suggesting that histamine-induced nociceptive behaviors are not mediated through histamine H(1) and H(2) receptors in the spinal cord.
  • The histamine-induced nociceptive behaviors were inhibited by co-administration of the competitive NMDA receptor antagonists, d-(-)-2-amino-5-phosphonovaleric acid (D-APV) and 3-((+)-2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid (CPPA), and the ion channel blocker, (5R,10S)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5,10-imine maleate (MK-801).
  • Co-administration of ifenprodil, an antagonist for both the polyamine site and the NR2B subunit of NMDA receptors, also inhibited the histamine-induced nociceptive behaviors. (R-[R, S])-alpha-(4-hydroxyphenyl)-beta-methyl-4-(phenylmethyl)-1-piperidinepropanol hydrochloride (Ro25-6981), an antagonist of the NMDA receptor subtype containing the NR2B subunit, did not inhibit histamine-induced nociceptive behaviors, whereas these behaviors were attenuated by pretreatment with an antisense oligodeoxynucleotide against the mRNA for the NR1 subunit of the NMDA receptor.
  • Moreover, agmatine and arcaine, antagonists for a polyamine site on the NMDA receptor, inhibited nociceptive behaviors induced by histamine.
  • These results suggest that a polyamine site on spinal NMDA receptors is involved in eliciting the nociceptive behavioral episode following intrathecal injection of histamine.
  • [MeSH-major] Histamine / administration & dosage. Pain / physiopathology. Receptors, N-Methyl-D-Aspartate / physiology. Spinal Cord / drug effects
  • [MeSH-minor] Animals. Excitatory Amino Acid Antagonists / pharmacology. Injections, Spinal. Male. Mice. Mice, Inbred C57BL. Mice, Knockout. Polyamines. Receptors, Histamine H1 / physiology. Receptors, Histamine H2 / physiology. Receptors, Neurokinin-1 / physiology. Receptors, Neurokinin-2 / physiology

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  • (PMID = 18155693.001).
  • [ISSN] 0014-2999
  • [Journal-full-title] European journal of pharmacology
  • [ISO-abbreviation] Eur. J. Pharmacol.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / Excitatory Amino Acid Antagonists; 0 / Polyamines; 0 / Receptors, Histamine H1; 0 / Receptors, Histamine H2; 0 / Receptors, N-Methyl-D-Aspartate; 0 / Receptors, Neurokinin-1; 0 / Receptors, Neurokinin-2; 820484N8I3 / Histamine
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54. Axelrod D, Bielory L: Fexofenadine hydrochloride in the treatment of allergic disease: a review. J Asthma Allergy; 2008;1:19-29
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  • [Title] Fexofenadine hydrochloride in the treatment of allergic disease: a review.
  • Fexofenadine has been shown to have an impact on inflammatory mediators, other than histamine, such as decreasing the production of LTC(4), LTD(4), LTE(4), PGE(2), and PGF(2α); inhibiting cyclo-oxygenase 2, thromboxane; limiting iNOS generation of NO; decreasing cytokine levels (ICAM-1, ELAM-1, VCAM-1, RANTES, I-TAC, MDC, TARC, MMP-2, MMP-9, tryptase); and diminishing eosinophil adherence, chemotaxis, and opsonization of particles.

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  • (PMID = 21436982.001).
  • [ISSN] 1178-6965
  • [Journal-full-title] Journal of asthma and allergy
  • [ISO-abbreviation] J Asthma Allergy
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] New Zealand
  • [Other-IDs] NLM/ PMC3121339
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55. Kaye AD, Hoover JM, Ibrahim IN, Phelps J, Baluch A, Fields A, Huffman S: Analysis of the effects of fentanyl in the feline pulmonary vascular bed. Am J Ther; 2006 Nov-Dec;13(6):478-84
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  • In separate experiments, the effects of diphenhydramine (histamine receptor blocker), glibenclamide (ATP-sensitive K+ channel blocker), L-N5-(1-Iminoethyl) ornithine hydrochloride (L-NIO) (nitric oxide synthase inhibitor), nimesulide (selective cyclooxygenase [COX]-2 inhibitor), and naloxone (opiate receptor antagonist) were investigated on pulmonary arterial responses to fentanyl and other agonists in the pulmonary vascular bed of the cat.
  • [MeSH-minor] Analgesics, Opioid / pharmacology. Animals. Blood Pressure / drug effects. Bradykinin / metabolism. Cats. Cyclooxygenase 2 / metabolism. Diphenhydramine / pharmacology. Dose-Response Relationship, Drug. Histamine / metabolism. Histamine H1 Antagonists / pharmacology. Naloxone / pharmacology. Narcotic Antagonists / pharmacology. Nitric Oxide / metabolism. Norepinephrine / metabolism. Pulmonary Circulation / drug effects

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  • (PMID = 17122527.001).
  • [ISSN] 1075-2765
  • [Journal-full-title] American journal of therapeutics
  • [ISO-abbreviation] Am J Ther
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Analgesics, Opioid; 0 / Histamine H1 Antagonists; 0 / Narcotic Antagonists; 0 / Receptors, Opioid; 0 / Vasodilator Agents; 31C4KY9ESH / Nitric Oxide; 36B82AMQ7N / Naloxone; 820484N8I3 / Histamine; 8GTS82S83M / Diphenhydramine; EC 1.14.99.1 / Cyclooxygenase 2; S8TIM42R2W / Bradykinin; UF599785JZ / Fentanyl; X4W3ENH1CV / Norepinephrine
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56. Spector SL, Shikiar R, Harding G, Meeves S, Leahy MJ: The effect of fexofenadine hydrochloride on productivity and quality of life in patients with chronic idiopathic urticaria. Cutis; 2007 Feb;79(2):157-62
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  • [Title] The effect of fexofenadine hydrochloride on productivity and quality of life in patients with chronic idiopathic urticaria.
  • The present study examined the impact of once-daily fexofenadine hydrochloride (HCl) 180 mg on health-related quality of life (HRQL) in subjects with chronic idiopathic urticaria (CIU).
  • [MeSH-major] Efficiency. Histamine H1 Antagonists, Non-Sedating / therapeutic use. Quality of Life. Terfenadine / analogs & derivatives. Urticaria / drug therapy

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  • (PMID = 17388220.001).
  • [ISSN] 0011-4162
  • [Journal-full-title] Cutis
  • [ISO-abbreviation] Cutis
  • [Language] eng
  • [Publication-type] Journal Article; Multicenter Study; Randomized Controlled Trial; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Histamine H1 Antagonists, Non-Sedating; 7BA5G9Y06Q / Terfenadine; E6582LOH6V / fexofenadine
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57. Ashenager MS, Grgela T, Aragane Y, Kawada A: Inhibition of cytokine-induced expression of T-cell cytokines by antihistamines. J Investig Allergol Clin Immunol; 2007;17(1):20-6
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  • [MeSH-major] Histamine H1 Antagonists, Non-Sedating / pharmacology. Interferon-gamma / antagonists & inhibitors. Interleukin-5 / antagonists & inhibitors. T-Lymphocytes / drug effects
  • [MeSH-minor] Cells, Cultured. Cetirizine / pharmacology. Dibenzoxepins / pharmacology. Humans. Immunosuppressive Agents / pharmacology. Interleukin-12. Interleukin-4. Loratadine / pharmacology. Olopatadine Hydrochloride. RNA, Messenger / biosynthesis. Terfenadine / analogs & derivatives. Terfenadine / pharmacology

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  • (PMID = 17323859.001).
  • [ISSN] 1018-9068
  • [Journal-full-title] Journal of investigational allergology & clinical immunology
  • [ISO-abbreviation] J Investig Allergol Clin Immunol
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Spain
  • [Chemical-registry-number] 0 / Dibenzoxepins; 0 / Histamine H1 Antagonists, Non-Sedating; 0 / Immunosuppressive Agents; 0 / Interleukin-5; 0 / RNA, Messenger; 187348-17-0 / Interleukin-12; 207137-56-2 / Interleukin-4; 2XG66W44KF / Olopatadine Hydrochloride; 7AJO3BO7QN / Loratadine; 7BA5G9Y06Q / Terfenadine; 82115-62-6 / Interferon-gamma; E6582LOH6V / fexofenadine; YO7261ME24 / Cetirizine
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58. Ohashi Y, Nakai Y, Murata K: Effect of pretreatment with fexofenadine on the safety of immunotherapy in patients with allergic rhinitis. Ann Allergy Asthma Immunol; 2006 Apr;96(4):600-5
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  • METHODS: In this open-label, multicenter study, 134 patients receiving immunotherapy for allergic rhinitis were randomized 1:1 to a group receiving pretreatment with fexofenadine hydrochloride (60 mg) 2 hours before immunization injection (n = 67) or to a control group receiving no pretreatment (n = 67).
  • [MeSH-major] Desensitization, Immunologic. Histamine H1 Antagonists / administration & dosage. Rhinitis, Allergic, Perennial / therapy. Rhinitis, Allergic, Seasonal / therapy. Terfenadine / analogs & derivatives

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  • (PMID = 16680932.001).
  • [ISSN] 1081-1206
  • [Journal-full-title] Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology
  • [ISO-abbreviation] Ann. Allergy Asthma Immunol.
  • [Language] eng
  • [Publication-type] Journal Article; Randomized Controlled Trial
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Anti-Allergic Agents; 0 / Histamine H1 Antagonists; 7BA5G9Y06Q / Terfenadine; E6582LOH6V / fexofenadine
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59. Watanabe Y, Faraci FM, Heistad DD: Activation of Rho-associated kinase during augmented contraction of the basilar artery to serotonin after subarachnoid hemorrhage. Am J Physiol Heart Circ Physiol; 2005 Jun;288(6):H2653-8
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  • Contraction to histamine was similar in the two groups.
  • Fasudil hydrochloride (3 mumol/l), an inhibitor of Rho kinase, markedly attenuated serotonin-induced contraction.
  • Fasudil had little effect on contractions induced by histamine or phorbol 12,13-dibutyrate.
  • [MeSH-minor] Animals. Disease Models, Animal. Enzyme Activation. Histamine / pharmacology. Intracellular Signaling Peptides and Proteins. Male. Motor Activity / drug effects. Motor Activity / physiology. Rabbits. rho-Associated Kinases

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  • (PMID = 15665056.001).
  • [ISSN] 0363-6135
  • [Journal-full-title] American journal of physiology. Heart and circulatory physiology
  • [ISO-abbreviation] Am. J. Physiol. Heart Circ. Physiol.
  • [Language] eng
  • [Grant] United States / NHLBI NIH HHS / HL / HL-16066; United States / NHLBI NIH HHS / HL / HL-62984; United States / NINDS NIH HHS / NS / NS-24621
  • [Publication-type] Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, U.S. Gov't, P.H.S.
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Intracellular Signaling Peptides and Proteins; 103745-39-7 / fasudil; 333DO1RDJY / Serotonin; 820484N8I3 / Histamine; 84477-87-2 / 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; EC 2.7.11.1 / Protein-Serine-Threonine Kinases; EC 2.7.11.1 / rho-Associated Kinases
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60. Liu LL, Yang J, Lei GF, Wang GJ, Wang YW, Sun RP: Atomoxetine increases histamine release and improves learning deficits in an animal model of attention-deficit hyperactivity disorder: the spontaneously hypertensive rat. Basic Clin Pharmacol Toxicol; 2008 Jun;102(6):527-32
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  • [Title] Atomoxetine increases histamine release and improves learning deficits in an animal model of attention-deficit hyperactivity disorder: the spontaneously hypertensive rat.
  • It is known that central nervous system histamine is closely associated with cognition and it was recently shown that both atomoxetine and methylphenidate enhance cortical histamine release in rats.
  • To that end, the aim of our study was to investigate the effect of atomoxetine (2 mg/kg, intraperitoneally) on histamine release using the microdialysis technique in the spontaneously hypertensive rat (SHR), a suitable genetic model for ADHD.
  • Our data confirmed that atomoxetine increases extracellular levels of histamine in the prefrontal cortex, a brain region that is implicated in the pathophysiology of ADHD.
  • Given the tie between histamine neurotransmission and treatment of cognitive dysfunction, we also assessed the effects of atomoxetine on learning and memory as measured by the Morris water maze in SHR.
  • The results indicated that atomoxetine significantly ameliorated performance in the Morris water maze, consistent with its histamine-enhancing profile.
  • In conclusion, the current study provides further support for the notion that the therapeutic effect of atomoxetine could involve activation of histamine neurotransmission within the prefrontal cortex.
  • [MeSH-major] Adrenergic Uptake Inhibitors / therapeutic use. Attention Deficit Disorder with Hyperactivity / drug therapy. Behavior, Animal / drug effects. Disease Models, Animal. Histamine / metabolism. Learning / drug effects. Prefrontal Cortex / drug effects. Propylamines / therapeutic use
  • [MeSH-minor] Animals. Atomoxetine Hydrochloride. Injections, Intraperitoneal. Male. Maze Learning / drug effects. Memory / drug effects. Rats. Rats, Inbred SHR. Water

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  • (PMID = 18346050.001).
  • [ISSN] 1742-7843
  • [Journal-full-title] Basic & clinical pharmacology & toxicology
  • [ISO-abbreviation] Basic Clin. Pharmacol. Toxicol.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] Denmark
  • [Chemical-registry-number] 0 / Adrenergic Uptake Inhibitors; 0 / Propylamines; 059QF0KO0R / Water; 57WVB6I2W0 / Atomoxetine Hydrochloride; 820484N8I3 / Histamine
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61. Uzunović A, Vranić E: Effect of magnesium stearate concentration on dissolution properties of ranitidine hydrochloride coated tablets. Bosn J Basic Med Sci; 2007 Aug;7(3):279-83
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  • [Title] Effect of magnesium stearate concentration on dissolution properties of ranitidine hydrochloride coated tablets.
  • The objective of this study was to evaluate the effects of two different concentrations of magnesium stearate on dissolution properties of ranitidine hydrochloride coated tablet formulations labeled to contain 150 mg.
  • Fraction of ranitidine hydrochloride released in dissolution medium was calculated from calibration curves.
  • Application of f2 equation showed differences in time-course of ranitidine hydrochloride dissolution properties.
  • The obtained values indicate differences in drug release from analyzed ranitidine hydrochloride formulations and could cause differences in therapeutic response.

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  • (PMID = 17848158.001).
  • [ISSN] 1512-8601
  • [Journal-full-title] Bosnian journal of basic medical sciences
  • [ISO-abbreviation] Bosn J Basic Med Sci
  • [Language] ENG
  • [Publication-type] Journal Article
  • [Publication-country] Bosnia and Herzegovina
  • [Chemical-registry-number] 0 / Histamine H2 Antagonists; 0 / Pharmaceutical Preparations; 0 / Stearic Acids; 0 / Tablets; 0 / Tablets, Enteric-Coated; 4ELV7Z65AP / stearic acid; 884KT10YB7 / Ranitidine
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62. Ligneau X, Perrin D, Landais L, Camelin JC, Calmels TP, Berrebi-Bertrand I, Lecomte JM, Parmentier R, Anaclet C, Lin JS, Bertaina-Anglade V, la Rochelle CD, d'Aniello F, Rouleau A, Gbahou F, Arrang JM, Ganellin CR, Stark H, Schunack W, Schwartz JC: BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology. J Pharmacol Exp Ther; 2007 Jan;320(1):365-75
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  • [Title] BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology.
  • Histamine H3 receptor inverse agonists are known to enhance the activity of histaminergic neurons in brain and thereby promote vigilance and cognition.
  • 1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride (BF2.649) is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor.
  • [MeSH-major] Histamine Agonists / pharmacology. Histamine Antagonists / pharmacology. Piperidines / pharmacology. Receptors, Histamine H3 / drug effects
  • [MeSH-minor] Acetylcholine / secretion. Animals. Cats. Dopamine / secretion. Electroencephalography / drug effects. Guinea Pigs. Histamine Release / drug effects. Humans. Imidazoles / metabolism. Male. Methylhistamines / pharmacology. Mice. Mice, Inbred C57BL. Prefrontal Cortex / drug effects. Prefrontal Cortex / secretion. Scopolamine Hydrobromide / pharmacology

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  • (PMID = 17005916.001).
  • [ISSN] 0022-3565
  • [Journal-full-title] The Journal of pharmacology and experimental therapeutics
  • [ISO-abbreviation] J. Pharmacol. Exp. Ther.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Histamine Agonists; 0 / Histamine Antagonists; 0 / Imidazoles; 0 / Methylhistamines; 0 / Piperidines; 0 / Receptors, Histamine H3; 152028-96-1 / iodoproxyfan; 451IFR0GXB / Scopolamine Hydrobromide; 4BC83L4PIY / 1-(3-(3-(4-chlorophenyl)propoxy)propyl)piperidine; KCB81T4EOF / tele-methylhistamine; N9YNS0M02X / Acetylcholine; VTD58H1Z2X / Dopamine
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63. Marín A, Barbas C: Systematic comparison of different functionality columns for a classical pharmaceutical problem. J Pharm Biomed Anal; 2006 Feb 13;40(2):262-70
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  • They were systematically compared with a test mixture containing basic, neutral and acidic compounds of very different polarities, as well as different functional groups (acetaminophen, phenylephrine hydrochloride or phenylpropanolamine hydrochloride, chlorpheniramine maleate, 4-aminophenol, 4-chloracetanilide and 4-nitrophenol) at three pH levels (2.5, 4.6 and 7.0) and three proportions of buffer/acetonitrile (80:20, 50:50 and 20:80, v/v).
  • [MeSH-minor] Acetaminophen / analysis. Acetaminophen / chemistry. Acetonitriles / chemistry. Amides. Analgesics, Non-Narcotic / analysis. Analgesics, Non-Narcotic / chemistry. Chlorpheniramine / analysis. Chlorpheniramine / chemistry. Histamine H1 Antagonists / analysis. Histamine H1 Antagonists / chemistry. Hydrogen-Ion Concentration. Nasal Decongestants / analysis. Nasal Decongestants / chemistry. Phenylephrine / analysis. Phenylephrine / chemistry. Polyethylene Glycols

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  • (PMID = 16146679.001).
  • [ISSN] 0731-7085
  • [Journal-full-title] Journal of pharmaceutical and biomedical analysis
  • [ISO-abbreviation] J Pharm Biomed Anal
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Acetonitriles; 0 / Amides; 0 / Analgesics, Non-Narcotic; 0 / Fluorocarbons; 0 / Histamine H1 Antagonists; 0 / Nasal Decongestants; 0 / Pharmaceutical Preparations; 1WS297W6MV / Phenylephrine; 30IQX730WE / Polyethylene Glycols; 362O9ITL9D / Acetaminophen; 3U6IO1965U / Chlorpheniramine
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64. Murota H, Bae S, Hamasaki Y, Maruyama R, Katayama I: Emedastine difumarate inhibits histamine-induced collagen synthesis in dermal fibroblasts. J Investig Allergol Clin Immunol; 2008;18(4):245-52
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  • [Title] Emedastine difumarate inhibits histamine-induced collagen synthesis in dermal fibroblasts.
  • BACKGROUND: Mast cell-derived histamine is known to act on dermal fibroblasts and contribute to formation of an intractable chronic allergic dermatitis.
  • Although this fibrotic event may also occur in other organs such as the nasal mucosa, no direct evidence has been reported as to whether responsiveness to histamine by fibroblasts derived from different organs is of the same intensity.
  • Furthermore, while type 1 histamine receptor (H1R) blockers have been shown to be effective for alleviation of the symptoms of allergic diseases, their ability to affect histamine-induced tissue remodeling has not yet been clarified.
  • OBJECTIVE: Our aim was to study the effect of H1R-blockers on histamine-induced tissue remodeling.
  • METHODS: A macroarray assay was used for a comprehensive analysis of histamine-induced gene expression by normal human fibroblasts.
  • Fibroblasts derived from skin or nasal mucosa were cultured in the presence of various concentrations of histamine, and the synthesis of type 1 collagen was measured by means of semi-quantitative reverse-transcriptase polymerase chain reaction and enzyme-linked immunosorbent assay.
  • To determine the effect of H1R blockers, diphenhydramine hydrochloride and emedastine difumarate were investigated in this assay.
  • RESULTS: Histamine induced expression of various kinds of fibrogenic molecules in fibroblasts.
  • Increased type 1 collagen expression was observed in fibroblasts treated with high-dose (0.1 mM to 1 microM) and low-dose (1 pM) histamine.
  • This histamine-induced type 1 collagen synthesis was effectively diminished by emedastine difumarate.
  • While organ specificity seems to be involved, emedastine difumarate is considered to be an effective drug for reversal of such histamine-induced remodeling in the skin.
  • CONCLUSIONS: We found that the expression of fibroblast-derived genes is differentially regulated by different concentrations of histamine and that the robustness of the inhibitory action of H1R blockers is different for skin-derived and nasal mucosa-derived fibroblasts.
  • We believe that our findings may contribute to a better understanding of the mechanisms of histamine-induced tissue remodeling and provide information useful for the management of refractory allergic dermatitis.
  • [MeSH-major] Benzimidazoles / pharmacology. Collagen Type I / biosynthesis. Dermatitis, Atopic / metabolism. Fibroblasts / metabolism. Histamine H1 Antagonists / pharmacology
  • [MeSH-minor] Cells, Cultured. Diphenhydramine / pharmacology. Gene Expression. Gene Expression Profiling. Histamine / pharmacology. Humans. Mast Cells / cytology. Mast Cells / physiology. Nasal Mucosa / cytology. Oligonucleotide Array Sequence Analysis. Skin / cytology

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  • [ErratumIn] J Investig Allergol Clin Immunol. 2009;19(2):166. Dosage error in article text
  • (PMID = 18714531.001).
  • [ISSN] 1018-9068
  • [Journal-full-title] Journal of investigational allergology & clinical immunology
  • [ISO-abbreviation] J Investig Allergol Clin Immunol
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Spain
  • [Chemical-registry-number] 0 / Benzimidazoles; 0 / Collagen Type I; 0 / Histamine H1 Antagonists; 820484N8I3 / Histamine; 8GTS82S83M / Diphenhydramine; 9J1H7Y9OJV / emedastine
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65. Kim JH, Choi GS, Ye YM, Nahm DH, Park HS: Acute urticaria caused by the injection of goat-derived hyaluronidase. Allergy Asthma Immunol Res; 2009 Oct;1(1):48-50
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  • To relieve her pain, she had been given epidural injections consisting of mepivacaine hydrochloride, triamcinolone acetonide, and morphine sulfate biweekly for one year.
  • Skin prick testing showed a positive response to 1,500 IU/mL of hyaluronidase extract, as compared to histamine.

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  • (PMID = 20224671.001).
  • [ISSN] 2092-7363
  • [Journal-full-title] Allergy, asthma & immunology research
  • [ISO-abbreviation] Allergy Asthma Immunol Res
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Korea (South)
  • [Other-IDs] NLM/ PMC2831570
  • [Keywords] NOTNLM ; IgE-mediated hypersensitivity / hyaluronidase / urticaria
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66. Lu-Suguro JF, Hua J, Sakamoto K, Nagaoka I: Inhibitory action of glucosamine on platelet activation in guinea pigs. Inflamm Res; 2005 Dec;54(12):493-9
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  • MATERIALS AND METHODS: Glucosamine hydrochloride solution (0.5%, 5 mg/ml) was administered orally to guinea pigs ad libitum for 22 days, and platelet rich plasma was collected to evaluate platelet functions in vitro.

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  • (PMID = 16389570.001).
  • [ISSN] 1023-3830
  • [Journal-full-title] Inflammation research : official journal of the European Histamine Research Society ... [et al.]
  • [ISO-abbreviation] Inflamm. Res.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] Switzerland
  • [Chemical-registry-number] 0 / Receptors, Purinergic P2; 57576-52-0 / Thromboxane A2; 61D2G4IYVH / Adenosine Diphosphate; 8L70Q75FXE / Adenosine Triphosphate; N08U5BOQ1K / Glucosamine
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67. Hampel FC, Kittner B, van Bavel JH: Safety and tolerability of fexofenadine hydrochloride, 15 and 30 mg, twice daily in children aged 6 months to 2 years with allergic rhinitis. Ann Allergy Asthma Immunol; 2007 Dec;99(6):549-54
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  • [Title] Safety and tolerability of fexofenadine hydrochloride, 15 and 30 mg, twice daily in children aged 6 months to 2 years with allergic rhinitis.
  • OBJECTIVE: To establish the safety and tolerability of fexofenadine hydrochloride in children aged 6 months to 2 years in 2 studies (T/3001 and T/3002).
  • Subjects were randomized (T/3001, n = 174; and T/3002, n = 219) to twice-daily fexofenadine hydrochloride, 15 or 30 mg, or placebo mixed with a standard vehicle.
  • RESULTS: In the combined population, the incidence of treatment-emergent adverse events (TEAEs) was comparable between groups (placebo, 48.2% [96/199]; fexofenadine hydrochloride, 15 mg, 40.0% [34/85]; and fexofenadine hydrochloride, 30 mg, 35.2% [38/108]).
  • Vomiting was the most common TEAE (placebo, 13.6%; fexofenadine hydrochloride, 15 mg, 14.1%; and fexofenadine hydrochloride, 30 mg, 5.6%).
  • CONCLUSION: Fexofenadine hydrochloride, 15 or 30 mg, given for a mean duration of 8 days is well tolerated, with a good safety profile, in children aged 6 months to 2 years.
  • [MeSH-major] Histamine H1 Antagonists, Non-Sedating / administration & dosage. Rhinitis, Allergic, Perennial / drug therapy. Terfenadine / analogs & derivatives

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  • (PMID = 18219837.001).
  • [ISSN] 1081-1206
  • [Journal-full-title] Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology
  • [ISO-abbreviation] Ann. Allergy Asthma Immunol.
  • [Language] eng
  • [Publication-type] Journal Article; Multicenter Study; Randomized Controlled Trial; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Histamine H1 Antagonists, Non-Sedating; 7BA5G9Y06Q / Terfenadine; E6582LOH6V / fexofenadine
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68. Selmeczy Z, Csóka B, Pacher P, Vizi ES, Haskó G: The adenosine A2A receptor agonist CGS 21680 fails to ameliorate the course of dextran sulphate-induced colitis in mice. Inflamm Res; 2007 May;56(5):204-9
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  • OBJECTIVE: In this study we investigated the effect of CGS 21680 (2-p-(2-Carboxyethyl)phenethylamino-5-N-ethylcarboxamidoadenosine hydrochloride), an adenosine A2A receptor agonist, in a model of dextran sulphate sodium (DSS)-induced colitis.

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  • (PMID = 17588136.001).
  • [ISSN] 1023-3830
  • [Journal-full-title] Inflammation research : official journal of the European Histamine Research Society ... [et al.]
  • [ISO-abbreviation] Inflamm. Res.
  • [Language] eng
  • [Grant] United States / NIGMS NIH HHS / GM / GM66189; United States / NIGMS NIH HHS / GM / R01 GM066189-02; United States / Intramural NIH HHS / / Z01 AA000375-02; United States / NIGMS NIH HHS / GM / R01 GM066189-01; United States / NIGMS NIH HHS / GM / R01 GM066189
  • [Publication-type] Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
  • [Publication-country] Switzerland
  • [Chemical-registry-number] 0 / Adenosine A2 Receptor Agonists; 0 / Antihypertensive Agents; 0 / Chemokine CCL3; 0 / Chemokine CCL4; 0 / Chemokine CXCL2; 0 / Chemokines; 0 / Cxcl2 protein, mouse; 0 / Interleukin-1beta; 0 / Macrophage Inflammatory Proteins; 0 / Phenethylamines; 120225-54-9 / 2-(4-(2-carboxyethyl)phenethylamino)-5'-N-ethylcarboxamidoadenosine; 9042-14-2 / Dextran Sulfate; K72T3FS567 / Adenosine; N9YNS0M02X / Acetylcholine
  • [Other-IDs] NLM/ NIHMS38108; NLM/ PMC2225471
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69. Gillard M, Chatelain P: Changes in pH differently affect the binding properties of histamine H1 receptor antagonists. Eur J Pharmacol; 2006 Jan 20;530(3):205-14
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  • [Title] Changes in pH differently affect the binding properties of histamine H1 receptor antagonists.
  • We investigated the effect of acidic pH, a condition that can be encountered during inflammation accompanying allergic reaction, on the binding properties of histamine H1 receptor antagonists, including levocetirizine ((2-(4-[(R)-(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl)ethoxy)acetic acid; Xyzal ), fexofenadine (rac-2-[4-[1-Hydroxy-4-[4-(hydroxydiphenylmethyl) piperidin-1-yl]butyl]phenyl]-2-methylpropionic acid hydrochloride; Allegra) and desloratadine (8-Chloro-6,11-dihydro-11-(4-piperidylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine; Clarinex ).
  • Lowering the pH from 7.4 to 5.8 decreased the affinity of [3H]mepyramine for histamine H1 receptors from 1.7 to 7.5 nM while the opposite was observed with [3H]levocetirizine, whose affinity increased from 4.1 to 1.5 nM.
  • Competition curves with [3H]mepyramine indicated that decreasing the pH from 7.4 to 5.8 led to a 2- to 5-fold increase in the affinity of fexofenadine and levocetirizine, no change in affinity for desloratadine and a 5- to 10-fold decrease in affinity for mepyramine and histamine.
  • [MeSH-major] Histamine H1 Antagonists / metabolism. Receptors, Histamine H1 / metabolism

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  • (PMID = 16388798.001).
  • [ISSN] 0014-2999
  • [Journal-full-title] European journal of pharmacology
  • [ISO-abbreviation] Eur. J. Pharmacol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / Histamine H1 Antagonists; 0 / Receptors, Histamine H1
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70. Oshima KZ, Asano K, Kanai K, Suzuki M, Suzaki H: Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cells in vitro and in vivo. Mediators Inflamm; 2009;2009:738038
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  • [Title] Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cells in vitro and in vivo.
  • The aim of the present study was to examine the effect of epinastine hydrochloride (EP), the most notable histamine H(1) receptor antagonists in Japan, on Dermatophagoides farinae (Der f)-pulsed mouse bone marrow-derived DCs in vitro and in vivo.
  • [MeSH-major] Allergens / immunology. Bone Marrow Cells / cytology. Dendritic Cells / drug effects. Dendritic Cells / immunology. Dermatophagoides farinae / immunology. Dibenzazepines / pharmacology. Histamine H1 Antagonists / pharmacology. Imidazoles / pharmacology

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  • (PMID = 19381339.001).
  • [ISSN] 1466-1861
  • [Journal-full-title] Mediators of inflammation
  • [ISO-abbreviation] Mediators Inflamm.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Allergens; 0 / Cytokines; 0 / Dibenzazepines; 0 / Histamine H1 Antagonists; 0 / Imidazoles; Q13WX941EF / epinastine
  • [Other-IDs] NLM/ PMC2667935
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71. Chimona TS, Panayiotides JG, Papadakis CE, Helidonis ES, Velegrakis GA: Antihistamine effects on experimental middle ear inflammatory model. Eur Arch Otorhinolaryngol; 2008 Aug;265(8):899-905
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  • The purpose of this study was to determine the histopathologic effects of H1 histamine receptor antagonists in an experimental histamine-induced middle ear inflammation model.
  • In group A (20 rabbits), histamine challenge followed a 3-day intramuscular pretreatment with a single dose of 0.1 ml hydroxyzine hydrochloride (50 mg/ml) per day.
  • In group B (20 rabbits), histamine challenge followed a 3-day pretreatment with a single dose 1.2 mg desloratadine per day orally.
  • In group C (20 rabbits), histamine challenge followed a 3-day pretreatment with a single dose 1.2 mg levocetirizine per day orally.
  • On the fourth day after baseline otomicroscopy 0.5 ml histamine 20 mg/ml was injected transtympanically on the right.
  • Oldest H1 antagonists can be replaced by the newest agents who counteract successfully histamine effects, without any interactions or adverse effects from central nervous system.
  • [MeSH-major] Cetirizine / pharmacology. Disease Models, Animal. Ear, Middle / drug effects. Histamine H1 Antagonists, Non-Sedating / pharmacology. Loratadine / analogs & derivatives. Otitis Media with Effusion / pathology

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  • (PMID = 18175139.001).
  • [ISSN] 0937-4477
  • [Journal-full-title] European archives of oto-rhino-laryngology : official journal of the European Federation of Oto-Rhino-Laryngological Societies (EUFOS) : affiliated with the German Society for Oto-Rhino-Laryngology - Head and Neck Surgery
  • [ISO-abbreviation] Eur Arch Otorhinolaryngol
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Chemical-registry-number] 0 / Histamine H1 Antagonists, Non-Sedating; 6U5EA9RT2O / levocetirizine; 7AJO3BO7QN / Loratadine; FVF865388R / desloratadine; YO7261ME24 / Cetirizine
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72. Gocmen JS, Buyukkocak U, Caglayan O: In vitro antibacterial activity of some systemic and topical antihistaminic preparations. Clin Invest Med; 2009;32(6):E232
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  • METHODS: Four topical and 3 systemic preparations containing pheniramine maleate, chlorophenoxamine hydrochloride, and diphenhydramine hydrochloride were studied.
  • Chlorophenoxamine hydrochloride-topical and chlorophenoxamine hydrochloride-systemic were the most effective (P < 0.05).
  • Despite the same active substrate content, diphenhydramine hydrochloride-topical-1 and diphenhydramine hydrochloride-topical-2 yielded different results when they were compared with each other or with the other preparations.
  • Diphenhydramine hydrochloride-topical-2 had a relatively higher rate of activity than diphenhydramine hydrochloride-topical-1.
  • [MeSH-major] Anti-Bacterial Agents / pharmacology. Histamine Antagonists / pharmacology. Microbial Sensitivity Tests. Staphylococcus aureus / drug effects. Staphylococcus epidermidis / drug effects

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  • (PMID = 20003827.001).
  • [ISSN] 1488-2353
  • [Journal-full-title] Clinical and investigative medicine. Médecine clinique et experimentale
  • [ISO-abbreviation] Clin Invest Med
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Canada
  • [Chemical-registry-number] 0 / Anti-Bacterial Agents; 0 / Ethylamines; 0 / Histamine Antagonists; 134FM9ZZ6M / Pheniramine; 3UVD77BP8R / chlorphenoxamine; 8GTS82S83M / Diphenhydramine
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73. Shen J, Yao JF, Tanida M, Nagai K: Regulation of sympathetic nerve activity by L-carnosine in mammalian white adipose tissue. Neurosci Lett; 2008 Aug 15;441(1):100-4
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  • The effect of lower dose of L-carnosine (100 ng/rat) was eliminated by pretreatment with diphenhydramine hydrochloride, a histamine H(1) receptor antagonist.
  • In contrast, the effect of higher dose of L-carnosine (10 microg/rat) was suppressed by thioperamide maleate salt, a histamine H(3) receptor antagonist.
  • The changes of plasma FFAs resulting from the exposure to 100 ng and 10 microg of L-carnosine were diminished by the beta-adrenergic receptor blocker propranolol hydrochloride and the muscarinic receptor blocker atropine sulfate, respectively; and eliminated by the corresponding histamine receptor antagonists, which eliminated the changes in SNA-WAT.
  • Our results suggest that low doses of L-carnosine may regulate the lipolytic processes in adipose tissue through facilitation of the sympathetic nervous system, which is driven by histamine neurons through the H(1) receptor, and that the beta(3)-receptor may be involved in this enhanced lipolytic response.
  • [MeSH-minor] Adrenergic beta-Antagonists / pharmacology. Animals. Atropine / pharmacology. Diphenhydramine / pharmacology. Dose-Response Relationship, Drug. Drug Interactions. Fatty Acids / blood. Histamine H1 Antagonists / pharmacology. Histamine H3 Antagonists / pharmacology. Male. Muscarinic Antagonists / pharmacology. Piperidines / pharmacology. Propranolol / pharmacology. Rats. Rats, Wistar

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  • (PMID = 18599216.001).
  • [ISSN] 0304-3940
  • [Journal-full-title] Neuroscience letters
  • [ISO-abbreviation] Neurosci. Lett.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Ireland
  • [Chemical-registry-number] 0 / Adrenergic beta-Antagonists; 0 / Fatty Acids; 0 / Histamine H1 Antagonists; 0 / Histamine H3 Antagonists; 0 / Muscarinic Antagonists; 0 / Piperidines; 106243-16-7 / thioperamide; 7C0697DR9I / Atropine; 8GTS82S83M / Diphenhydramine; 8HO6PVN24W / Carnosine; 9Y8NXQ24VQ / Propranolol
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74. Sakairi T, Suzuki K, Makita S, Wajima T, Shakuto S, Yoshida Y, Yaguchi M: Effects of fexofenadine hydrochloride in a guinea pig model of antigen-induced rhinitis. Pharmacology; 2005 Oct;75(2):76-86
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  • [Title] Effects of fexofenadine hydrochloride in a guinea pig model of antigen-induced rhinitis.
  • Allergic rhinitis is an inflammatory disease of the nasal mucosa, induced by histamine, leukotrienes, and other substances released from mast cells.
  • Fexofenadine hydrochloride, the active metabolite of terfenadine, is a novel, nonsedating antiallergic drug having H1 receptor antagonistic activity.
  • Fexofenadine hydrochloride (20 mg/kg) and terfenadine (20 mg/kg) administered orally 70 min prior to the challenge significantly inhibited (fexofenadine, p < 0.001, terfenadine, p < 0.05) the increase in nasal airway resistance.

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  • [Copyright] Copyright 2005 S. Karger AG, Basel.
  • (PMID = 16037679.001).
  • [ISSN] 0031-7012
  • [Journal-full-title] Pharmacology
  • [ISO-abbreviation] Pharmacology
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Switzerland
  • [Chemical-registry-number] 0 / Anti-Allergic Agents; 0 / Carbazoles; 0 / Leukotrienes; 0 / Sulfonamides; 0 / Thromboxanes; 0 / Tosyl Compounds; 107753-78-6 / zafirlukast; 7BA5G9Y06Q / Terfenadine; 9006-59-1 / Ovalbumin; E6582LOH6V / fexofenadine; HPE317O9TL / Pyrilamine; P1ALI72U6C / ramatroban
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75. Pipkorn P, Costantini C, Reynolds C, Wall M, Drake M, Sanico A, Proud D, Togias A: The effects of the nasal antihistamines olopatadine and azelastine in nasal allergen provocation. Ann Allergy Asthma Immunol; 2008 Jul;101(1):82-9
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  • Efficacy variables were the allergen-induced sneezes, other clinical symptoms, and the levels of histamine, tryptase, albumin, lysozyme, and cysteinyl-leukotrienes (third study only) in nasal lavage fluids.
  • Olopatadine, 0.1%, inhibited lysozyme levels, but olopatadine, 0.2%, inhibited histamine, albumin, and lysozyme.
  • [MeSH-major] Allergens / immunology. Conjunctivitis, Allergic / drug therapy. Dibenzoxepins / therapeutic use. Histamine H1 Antagonists / therapeutic use. Phthalazines / therapeutic use. Rhinitis, Allergic, Seasonal / drug therapy
  • [MeSH-minor] Adult. Anti-Allergic Agents / administration & dosage. Anti-Allergic Agents / therapeutic use. Cross-Over Studies. Double-Blind Method. Female. Humans. Male. Middle Aged. Nasal Provocation Tests. Olopatadine Hydrochloride

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  • (PMID = 18681089.001).
  • [ISSN] 1081-1206
  • [Journal-full-title] Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology
  • [ISO-abbreviation] Ann. Allergy Asthma Immunol.
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article; Randomized Controlled Trial; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Allergens; 0 / Anti-Allergic Agents; 0 / Dibenzoxepins; 0 / Histamine H1 Antagonists; 0 / Phthalazines; 2XG66W44KF / Olopatadine Hydrochloride; ZQI909440X / azelastine
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76. Kortejärvi H, Yliperttula M, Dressman JB, Junginger HE, Midha KK, Shah VP, Barends DM: Biowaiver monographs for immediate release solid oral dosage forms: ranitidine hydrochloride. J Pharm Sci; 2005 Aug;94(8):1617-25
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  • [Title] Biowaiver monographs for immediate release solid oral dosage forms: ranitidine hydrochloride.
  • Literature and experimental data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the approval of immediate release (IR) solid oral dosage forms containing ranitidine hydrochloride are reviewed.
  • According to the current Biopharmaceutics Classification System (BCS), ranitidine hydrochloride should be assigned to Class III.
  • [MeSH-major] Histamine H2 Antagonists / pharmacokinetics. Ranitidine / pharmacokinetics

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  • [Copyright] (c) 2005 Wiley-Liss, Inc. and the American Pharmacists Association
  • (PMID = 15959881.001).
  • [ISSN] 0022-3549
  • [Journal-full-title] Journal of pharmaceutical sciences
  • [ISO-abbreviation] J Pharm Sci
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Dosage Forms; 0 / Excipients; 0 / Histamine H2 Antagonists; 884KT10YB7 / Ranitidine
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77. Mimami K: [Recent evidences in the pharmacological mechanisms of the tramadol]. Masui; 2005 Nov;54(11):1224-33
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  • Tramadol [(1R, 2R) and (1S, 2S)-2-dimethyl-amino-methyl-1-(3-methoxyphenyl) -cyclohexanol hydrochloride] has been used clinically.
  • [MeSH-minor] Animals. Humans. Ion Channels / drug effects. Norepinephrine Plasma Membrane Transport Proteins / drug effects. Rats. Receptors, G-Protein-Coupled / drug effects. Receptors, Histamine / radiation effects. Receptors, Muscarinic / drug effects

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  • (PMID = 16296359.001).
  • [ISSN] 0021-4892
  • [Journal-full-title] Masui. The Japanese journal of anesthesiology
  • [ISO-abbreviation] Masui
  • [Language] jpn
  • [Publication-type] English Abstract; Journal Article; Review
  • [Publication-country] Japan
  • [Chemical-registry-number] 0 / Analgesics, Opioid; 0 / Ion Channels; 0 / Narcotics; 0 / Norepinephrine Plasma Membrane Transport Proteins; 0 / Receptors, G-Protein-Coupled; 0 / Receptors, Histamine; 0 / Receptors, Muscarinic; 39J1LGJ30J / Tramadol
  • [Number-of-references] 33
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78. Galatowicz G, Ajayi Y, Stern ME, Calder VL: Ocular anti-allergic compounds selectively inhibit human mast cell cytokines in vitro and conjunctival cell infiltration in vivo. Clin Exp Allergy; 2007 Nov;37(11):1648-56
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  • BACKGROUND: Conjunctival mast cells (MCs) are important effector cells in seasonal allergic conjunctivitis, via histamine and cytokine secretion.
  • Several new anti-allergic eye drops stabilize MCs and block histamine receptors, but their anti-inflammatory effects are unclear.
  • METHODS: Human cord blood stem cell-derived (CBMC) and conjunctival biopsy-derived MCs were stimulated via FcepsilonRI, degranulation and histamine release were assayed at 1 h and cytokine secretion at 24 h using multiplex arrays.
  • RESULTS: After a 1 h stimulation, 80% of the CBMC had degranulated and secreted histamine (27.9+/-4.7 ng/10(6) cells; P<0.05).
  • Pre-treatment by all drugs significantly reduced histamine and TNF-alpha, whereas IL-5, IL-8, IL-10 and TNF-beta profiles were differentially decreased.
  • For conjunctival biopsy-derived cultures (n=11), FcepsilonR1 stimulation increased histamine, TNF-alpha, TNF-beta, IL-5 and IL-8 levels and the production of IL-5, IL-6 (P<0.05), histamine and IL-8 (P<0.01) was inhibited by epinastine.
  • The anti-allergic drugs have anti-histamine and mast-cell stabilizing properties but might differ in clinical improvement depending on the individual and the cytokines involved.
  • [MeSH-minor] Animals. Cell Differentiation / drug effects. Cells, Cultured. Conjunctiva / cytology. Dibenzazepines / pharmacology. Dibenzazepines / therapeutic use. Dibenzoxepins / pharmacology. Dibenzoxepins / therapeutic use. Eosinophilia / prevention & control. Female. Fetal Blood / cytology. Histamine Release / drug effects. Humans. Imidazoles / pharmacology. Imidazoles / therapeutic use. Mice. Mice, Inbred BALB C. Nedocromil / pharmacology. Nedocromil / therapeutic use. Neutrophils / pathology. Olopatadine Hydrochloride. Pollen / immunology. Proto-Oncogene Proteins c-kit / analysis. Receptors, IgE / agonists. Stem Cells / cytology. Stem Cells / drug effects. Stem Cells / metabolism

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  • (PMID = 17877767.001).
  • [ISSN] 0954-7894
  • [Journal-full-title] Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology
  • [ISO-abbreviation] Clin. Exp. Allergy
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Anti-Allergic Agents; 0 / Cytokines; 0 / Dibenzazepines; 0 / Dibenzoxepins; 0 / Imidazoles; 0 / Receptors, IgE; 0B535E0BN0 / Nedocromil; 2XG66W44KF / Olopatadine Hydrochloride; EC 2.7.10.1 / Proto-Oncogene Proteins c-kit; Q13WX941EF / epinastine
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79. Dake Y, Enomoto T, Cheng L, Enomoto K, Shibano A, Ikeda H, Yoda S, Yajin S, Sakota T, Yamanishi E: Effect of antihistamine eye drops on the conjunctival provocation test with Japanese cedar pollen allergen. Allergol Int; 2006 Dec;55(4):373-8
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  • 2) Levocabastine hydrochloride ophthalmic suspension and ketotifen fumarate ophthalmic solution were respectively instilled in the left and right eyes, which were then challenged with the allergen.
  • [MeSH-major] Allergens. Conjunctivitis, Allergic / diagnosis. Cryptomeria / immunology. Histamine H1 Antagonists / therapeutic use. Histamine H1 Antagonists, Non-Sedating / therapeutic use. Ketotifen / therapeutic use. Piperidines / therapeutic use. Plant Proteins. Pollen / immunology. Premedication

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  • (PMID = 17130679.001).
  • [ISSN] 1323-8930
  • [Journal-full-title] Allergology international : official journal of the Japanese Society of Allergology
  • [ISO-abbreviation] Allergol Int
  • [Language] eng
  • [Publication-type] Clinical Trial; Comparative Study; Journal Article
  • [Publication-country] Japan
  • [Chemical-registry-number] 0 / Allergens; 0 / Antigens, Plant; 0 / Cry j I protein, Cryptomeria japonica; 0 / Histamine H1 Antagonists; 0 / Histamine H1 Antagonists, Non-Sedating; 0 / Ophthalmic Solutions; 0 / Piperidines; 0 / Plant Proteins; H68BP06S81 / levocabastine; X49220T18G / Ketotifen
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80. Yoshida Y, Kumagai H, Ohkubo Y, Tsuchiya R, Morita M, Miyakawa H, Kudo Y: Effects of bifemelane on the calcium level and ATP release of the human origin astrocyte clonal cell. J Pharmacol Sci; 2006 Sep;102(1):121-8
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  • The effect of bifemelane hydrochloride (bifemelane) was examined on human origin astrocyte clonal cells (Kings-1).
  • Bifemelane caused a dose-dependent ATP release, but histamine and carbachol, which induced a large increase in [Ca(2+)](i), had no effects on the ATP release.
  • [MeSH-minor] Boron Compounds / pharmacology. Calcium Channels. Carbachol / pharmacology. Cell Line. Cholinergic Agonists / pharmacology. Clone Cells. Dose-Response Relationship, Drug. Histamine / metabolism. Humans. Inositol 1,4,5-Trisphosphate Receptors. Purinergic P2 Receptor Antagonists. Pyridoxal Phosphate / analogs & derivatives. Pyridoxal Phosphate / pharmacology. Receptors, Cytoplasmic and Nuclear / antagonists & inhibitors

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  • (PMID = 16974067.001).
  • [ISSN] 1347-8613
  • [Journal-full-title] Journal of pharmacological sciences
  • [ISO-abbreviation] J. Pharmacol. Sci.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] Japan
  • [Chemical-registry-number] 0 / 2-aminoethoxydiphenyl borate; 0 / Benzhydryl Compounds; 0 / Boron Compounds; 0 / Calcium Channels; 0 / Cholinergic Agonists; 0 / ITPR1 protein, human; 0 / Inositol 1,4,5-Trisphosphate Receptors; 0 / Nootropic Agents; 0 / Purinergic P2 Receptor Antagonists; 0 / Receptors, Cytoplasmic and Nuclear; 149017-66-3 / pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid; 5V5IOJ8338 / Pyridoxal Phosphate; 820484N8I3 / Histamine; 8L70Q75FXE / Adenosine Triphosphate; 8Y164V895Y / Carbachol; SY7Q814VUP / Calcium; Z4501GN13G / bifemelane
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81. Kumar P, Singh S, Mishra B: Floating osmotic drug delivery system of ranitidine hydrochloride: development and evaluation--a technical note. AAPS PharmSciTech; 2008;9(2):480-5
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  • [Title] Floating osmotic drug delivery system of ranitidine hydrochloride: development and evaluation--a technical note.
  • [MeSH-major] Drug Carriers. Excipients / chemistry. Histamine H2 Antagonists / chemistry. Ranitidine / chemistry

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  • (PMID = 18431658.001).
  • [ISSN] 1530-9932
  • [Journal-full-title] AAPS PharmSciTech
  • [ISO-abbreviation] AAPS PharmSciTech
  • [Language] eng
  • [Publication-type] Evaluation Studies; Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Delayed-Action Preparations; 0 / Drug Carriers; 0 / Excipients; 0 / Histamine H2 Antagonists; 0 / Tablets; 142M471B3J / Carbon Dioxide; 884KT10YB7 / Ranitidine
  • [Other-IDs] NLM/ PMC2976918
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82. Chu NN, Chen WL, Xu HR, Li XN: Pharmacokinetics of orally administered single- and multiple-dose olopatadine in healthy Chinese subjects: an open-label study. Clin Drug Investig; 2009;29(7):451-7
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  • BACKGROUND AND OBJECTIVES: Olopatadine is a new selective histamine H(1) receptor antagonist with anti-inflammatory and anti-allergic effects.
  • [MeSH-minor] Administration, Oral. Area Under Curve. Asian Continental Ancestry Group. Chromatography, Liquid. Dose-Response Relationship, Drug. Drug Administration Schedule. Female. Half-Life. Humans. Male. Olopatadine Hydrochloride. Sex Factors. Tandem Mass Spectrometry. Young Adult

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  • (PMID = 19499962.001).
  • [ISSN] 1173-2563
  • [Journal-full-title] Clinical drug investigation
  • [ISO-abbreviation] Clin Drug Investig
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] New Zealand
  • [Chemical-registry-number] 0 / Anti-Inflammatory Agents, Non-Steroidal; 0 / Dibenzoxepins; 2XG66W44KF / Olopatadine Hydrochloride
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83. Thumma S, Zhang SQ, Repka MA: Development and validation of a HPLC method for the analysis of promethazine hydrochloride in hot-melt extruded dosage forms. Pharmazie; 2008 Aug;63(8):562-7
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  • [Title] Development and validation of a HPLC method for the analysis of promethazine hydrochloride in hot-melt extruded dosage forms.
  • A simple and rapid stability-indicating HPLC method was developed for determination of promethazine hydrochloride (PMZ) in hot-melt extruded (HME) films and sustained release tablets.
  • [MeSH-major] Histamine H1 Antagonists / analysis. Promethazine / analysis

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  • (PMID = 18771002.001).
  • [ISSN] 0031-7144
  • [Journal-full-title] Die Pharmazie
  • [ISO-abbreviation] Pharmazie
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Chemical-registry-number] 0 / Dosage Forms; 0 / Histamine H1 Antagonists; FF28EJQ494 / Promethazine
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84. Kanai K, Asano K, Hisamitsu T, Suzaki H: Suppressive activity of epinastine hydrochloride on TARC production from human peripheral blood CD4+ T cells in-vitro. J Pharm Pharmacol; 2005 Aug;57(8):1027-36
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  • [Title] Suppressive activity of epinastine hydrochloride on TARC production from human peripheral blood CD4+ T cells in-vitro.
  • The aim of this study is to examine the influence of epinastine hydrochloride, an H1-receptor antagonist, on TARC production from human peripheral blood CD4+ T cells using an in-vitro cell culture technique.
  • [MeSH-major] CD4-Positive T-Lymphocytes / drug effects. Chemokines, CC / antagonists & inhibitors. Dibenzazepines / pharmacology. Histamine H1 Antagonists / pharmacology. Imidazoles / pharmacology. T-Lymphocyte Subsets / drug effects

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  • (PMID = 16102259.001).
  • [ISSN] 0022-3573
  • [Journal-full-title] The Journal of pharmacy and pharmacology
  • [ISO-abbreviation] J. Pharm. Pharmacol.
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / CCL17 protein, human; 0 / Chemokine CCL17; 0 / Chemokines, CC; 0 / Dibenzazepines; 0 / Histamine H1 Antagonists; 0 / Imidazoles; 0 / Muromonab-CD3; 0 / NF-kappa B; 207137-56-2 / Interleukin-4; Q13WX941EF / epinastine
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85. Jones JD, Temino VM, Dworski R, Anderson CK, Fahrenholz JM, An AQ: Use of olopatadine ophthalmic solution and reactivity of histamine skin testing. Allergy Asthma Proc; 2008 Nov-Dec;29(6):636-9
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  • [Title] Use of olopatadine ophthalmic solution and reactivity of histamine skin testing.
  • However, the very drugs used to treat allergic symptoms have been found to suppress histamine-induced skin testing, making the diagnosis very challenging.
  • This study was performed to evaluate whether olopatadine hydrochloride 0.2% ophthalmic solution suppressed histamine-induced wheals and flares on skin-prick testing.
  • A randomized, double-blinded, placebo-controlled, single-center, cross-over pilot study was performed that compared histamine-induced wheal and flare areas after 7-10 days of treatment with both olopatadine 0.2% ophthalmic solution and artificial tears, allowing for a 7- to 10-day washout period between medications.

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  • (PMID = 19173791.001).
  • [ISSN] 1088-5412
  • [Journal-full-title] Allergy and asthma proceedings
  • [ISO-abbreviation] Allergy Asthma Proc
  • [Language] ENG
  • [Grant] United States / NCRR NIH HHS / RR / UL1 RR 024975
  • [Publication-type] Journal Article; Randomized Controlled Trial; Research Support, N.I.H., Extramural
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Dibenzoxepins; 0 / Histamine H1 Antagonists, Non-Sedating; 0 / Ophthalmic Solutions; 2XG66W44KF / Olopatadine Hydrochloride; 820484N8I3 / Histamine
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86. Abelson MB, Gomes PJ, Vogelson CT, Pasquine TA, Turner FD, Wells DT, Robertson SM: Effects of a new formulation of olopatadine ophthalmic solution on nasal symptoms relative to placebo in two studies involving subjects with allergic conjunctivitis or rhinoconjunctivitis. Curr Med Res Opin; 2005 May;21(5):683-91
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  • BACKGROUND: A new formulation of olopatadine hydrochloride ophthalmic solution (olopatadine 0.2%) was evaluated in two separate, randomized, placebo-controlled, double-masked, hybrid environmental studies intended to determine efficacy and safety in subjects with histories of seasonal allergic conjunctivitis or rhinoconjunctivitis.
  • [MeSH-major] Conjunctivitis, Allergic / drug therapy. Dibenzoxepins / therapeutic use. Histamine H1 Antagonists / therapeutic use. Rhinitis, Allergic, Perennial / drug therapy
  • [MeSH-minor] Adolescent. Adult. Child. Female. Humans. Male. Middle Aged. Olopatadine Hydrochloride. Ophthalmic Solutions. Placebos

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  • (PMID = 15969867.001).
  • [ISSN] 0300-7995
  • [Journal-full-title] Current medical research and opinion
  • [ISO-abbreviation] Curr Med Res Opin
  • [Language] eng
  • [Publication-type] Clinical Trial; Journal Article; Randomized Controlled Trial; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Dibenzoxepins; 0 / Histamine H1 Antagonists; 0 / Ophthalmic Solutions; 0 / Placebos; 2XG66W44KF / Olopatadine Hydrochloride
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87. Horner WE, Johnson DE, Schmidt AW, Rollema H: Methylphenidate and atomoxetine increase histamine release in rat prefrontal cortex. Eur J Pharmacol; 2007 Mar 8;558(1-3):96-7
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  • [Title] Methylphenidate and atomoxetine increase histamine release in rat prefrontal cortex.
  • Using microdialysis in rat prefrontal cortex, we found that 1 mg/kg of the stimulant methylphenidate and the non-stimulant atomoxetine, two widely used treatments for Attention Deficit/Hyperactivity Disorder (ADHD), produce robust increases in the extracellular levels of histamine, which plays a key role in attention, learning and memory.
  • While the clinical response to ADHD drugs is typically attributed to modulation of norepinephrine and dopamine, this finding suggests enhanced histamine release may contribute to their efficacy as ADHD treatments.
  • [MeSH-major] Histamine Release / drug effects. Methylphenidate / pharmacology. Prefrontal Cortex / drug effects. Propylamines / pharmacology
  • [MeSH-minor] Animals. Atomoxetine Hydrochloride. Attention Deficit Disorder with Hyperactivity / drug therapy. Male. Rats. Rats, Sprague-Dawley

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  • (PMID = 17198700.001).
  • [ISSN] 0014-2999
  • [Journal-full-title] European journal of pharmacology
  • [ISO-abbreviation] Eur. J. Pharmacol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / Propylamines; 207ZZ9QZ49 / Methylphenidate; 57WVB6I2W0 / Atomoxetine Hydrochloride
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88. Apostu M, Dorneanu V: [Analytical application of phosphotungstic acid complexes. Fabrication and characterisation of membrane selective electrodes for some H2 antihistaminics]. Rev Med Chir Soc Med Nat Iasi; 2008 Jul-Sep;112(3):856-9
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  • All these electrodes were applied for the direct quantitative potentiometric determination of ranitidine hydrochloride, nizatidine and famotidine in pharmaceutical formulations.
  • [MeSH-major] Anti-Ulcer Agents / chemistry. Famotidine / chemistry. Histamine H2 Antagonists / chemistry. Membranes, Artificial. Nizatidine / chemistry. Phosphotungstic Acid / chemistry. Ranitidine / chemistry

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  • (PMID = 20201281.001).
  • [ISSN] 0048-7848
  • [Journal-full-title] Revista medico-chirurgicală̆ a Societă̆ţ̜ii de Medici ş̧i Naturaliş̧ti din Iaş̧i
  • [ISO-abbreviation] Rev Med Chir Soc Med Nat Iasi
  • [Language] rum
  • [Publication-type] English Abstract; Journal Article
  • [Publication-country] Romania
  • [Chemical-registry-number] 0 / Anti-Ulcer Agents; 0 / Histamine H2 Antagonists; 0 / Membranes, Artificial; 0 / Pharmaceutical Preparations; 12067-99-1 / Phosphotungstic Acid; 5QZO15J2Z8 / Famotidine; 884KT10YB7 / Ranitidine; P41PML4GHR / Nizatidine
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89. Liu X, Liu L, Chen H, Chen X: Separation and determination of four active components in medicinal preparations by flow injection-capillary electrophoresis. J Pharm Biomed Anal; 2007 Apr 11;43(5):1700-5
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  • A simple, rapid and accurate method for the separation and determination of paracetamol (Par), pseudoephedrine hydrochloride (Pse), dextromethorphan hydrobromide (Dex) and chlorphenamine hydrogen maleate (Chl) was developed by combination of flow injection and capillary zone electrophoresis for the first time.
  • [MeSH-minor] Analgesics, Non-Narcotic / analysis. Analgesics, Non-Narcotic / chemistry. Analgesics, Non-Narcotic / isolation & purification. Analgesics, Non-Narcotic / pharmacology. Antitussive Agents / analysis. Antitussive Agents / chemistry. Antitussive Agents / isolation & purification. Antitussive Agents / pharmacology. Bronchodilator Agents / analysis. Bronchodilator Agents / chemistry. Bronchodilator Agents / isolation & purification. Bronchodilator Agents / pharmacology. Buffers. Common Cold / drug therapy. Flow Injection Analysis / methods. Histamine H1 Antagonists / analysis. Histamine H1 Antagonists / chemistry. Histamine H1 Antagonists / isolation & purification. Histamine H1 Antagonists / pharmacology. Hydrogen-Ion Concentration. Maleates / isolation & purification. Reproducibility of Results. Time Factors

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  • (PMID = 17337151.001).
  • [ISSN] 0731-7085
  • [Journal-full-title] Journal of pharmaceutical and biomedical analysis
  • [ISO-abbreviation] J Pharm Biomed Anal
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Analgesics, Non-Narcotic; 0 / Antitussive Agents; 0 / Bronchodilator Agents; 0 / Buffers; 0 / Histamine H1 Antagonists; 0 / Maleates; 362O9ITL9D / Acetaminophen; 3U6IO1965U / Chlorpheniramine; 7355X3ROTS / Dextromethorphan; GN83C131XS / Ephedrine
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90. Le S, Gruner JA, Mathiasen JR, Marino MJ, Schaffhauser H: Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H3 receptor antagonists. J Pharmacol Exp Ther; 2008 Jun;325(3):902-9
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  • The histamine H3 receptor (H3R) modulates the release of neurotransmitters that are involved in vigilance, cognition, and sleep-wake regulation.
  • The H3R antagonists ciproxifan, thioperamide, GSK189254 (6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide hydrochloride), and ABT-239 ([4-(2-{2-[(2R)-2-methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile) produced wake-promoting activity in vivo and a dose-dependent inhibition of H3R binding ex vivo.
  • [MeSH-major] Histamine H3 Antagonists / pharmacology. Receptors, Histamine H3 / metabolism. Wakefulness / drug effects

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  • (PMID = 18305012.001).
  • [ISSN] 1521-0103
  • [Journal-full-title] The Journal of pharmacology and experimental therapeutics
  • [ISO-abbreviation] J. Pharmacol. Exp. Ther.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Histamine H3 Antagonists; 0 / Receptors, Histamine H3
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91. Kaye AD, Hoover JM, Kaye AJ, Ibrahim IN, Fox C, Bajwa A, Anwar M, Fields AM, Baluch A, Huffman S, Chilian W: Morphine, opioids, and the feline pulmonary vascular bed. Acta Anaesthesiol Scand; 2008 Aug;52(7):931-7
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  • Additionally, the effects of L-N(5)-(1-iminoethyl) ornithine hydrochloride (L-NIO) (nitric oxide synthase inhibitor), nimesulide [selective cyclooxygenase (COX)-2 inhibitor], glibenclamide (ATP-sensitive K+ channel blocker), naloxone (non-selective opioid receptor antagonist), and diphenhydramine (histamine H(1)-receptor antagonist) were investigated on pulmonary arterial responses to morphine and other selected agonists in the feline pulmonary vascular bed.
  • Morphine-induced vasodilatory responses appeared to be mediated or modulated by both opioid receptor and histamine-receptor-sensitive pathways.

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  • Hazardous Substances Data Bank. FENTANYL .
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  • (PMID = 18477088.001).
  • [ISSN] 1399-6576
  • [Journal-full-title] Acta anaesthesiologica Scandinavica
  • [ISO-abbreviation] Acta Anaesthesiol Scand
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Analgesics, Opioid; 0 / Piperidines; 0 / Sulfonamides; 0 / Vasodilator Agents; 36889-13-1 / N(G)-iminoethylornithine; 36B82AMQ7N / Naloxone; 76I7G6D29C / Morphine; 8GTS82S83M / Diphenhydramine; 9E338QE28F / Meperidine; AFE2YW0IIZ / Sufentanil; E524N2IXA3 / Ornithine; P10582JYYK / remifentanil; SX6K58TVWC / Glyburide; UF599785JZ / Fentanyl; V4TKW1454M / nimesulide
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92. Lichtenstein SJ, Abelson MB: Pharmacology, clinical efficacy and safety of olopatadine hydrochloride. Expert Rev Clin Immunol; 2006 May;2(3):341-51
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  • [Title] Pharmacology, clinical efficacy and safety of olopatadine hydrochloride.
  • Studies in human conjunctival mast cells clearly demonstrate, in the relevant tissue and species, olopatadine's inhibition of histamine release, which was subsequently confirmed in allergen-challenged subjects.
  • Its comfort and tolerability may be related to the absence of perturbation of cell membranes, in contrast to many anti-allergics, whose disruption of membranes lead to histamine release even at therapeutically relevant concentrations.

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  • (PMID = 20476906.001).
  • [ISSN] 1744-8409
  • [Journal-full-title] Expert review of clinical immunology
  • [ISO-abbreviation] Expert Rev Clin Immunol
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
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93. Roy P, Shahiwala A: Statistical optimization of ranitidine HCl floating pulsatile delivery system for chronotherapy of nocturnal acid breakthrough. Eur J Pharm Sci; 2009 Jun 28;37(3-4):363-9
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  • This approach will be achieved by using a programmed delivery of ranitidine hydrochloride from a floating tablet with time-lagged coating.
  • The proposed mathematical model is found to be robust and accurate for optimization of time-lagged coating formulations for programmable pulsatile release of ranitidine hydrochloride, consistent with the demands of nocturnal acid breakthrough.
  • [MeSH-major] Histamine H2 Antagonists / administration & dosage. Histamine H2 Antagonists / chemistry. Ranitidine / administration & dosage. Ranitidine / chemistry

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  • (PMID = 19491027.001).
  • [ISSN] 1879-0720
  • [Journal-full-title] European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
  • [ISO-abbreviation] Eur J Pharm Sci
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / Delayed-Action Preparations; 0 / Excipients; 0 / Histamine H2 Antagonists; 0 / Tablets, Enteric-Coated; 3NXW29V3WO / Hypromellose Derivatives; 884KT10YB7 / Ranitidine; 9004-34-6 / Cellulose; 9004-57-3 / ethyl cellulose; 9004-67-5 / Methylcellulose
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94. Murota H, El-latif MA, Tamura T, Amano T, Katayama I: Olopatadine hydrochloride improves dermatitis score and inhibits scratch behavior in NC/Nga mice. Int Arch Allergy Immunol; 2010;153(2):121-32
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  • [Title] Olopatadine hydrochloride improves dermatitis score and inhibits scratch behavior in NC/Nga mice.
  • Itch is mediated by a variety of pruritogens, including histamine, and promoted by neurite outgrowth in the epidermis of AD patients, probably due to the release of nerve growth factor.
  • OBJECTIVES: We investigated the effects of orally administered olopatadine hydrochloride (olopatadine) on itching, itching mediators, and neuritogenic action in a mouse model.
  • RESULTS: Olopatadine significantly suppressed scratching, improved the dermatitis score, inhibited neurite outgrowth, and decreased the elevated inflammatory markers, growth factors and histamine content in the lesional skin, and serum concentration of Dfb-specific IgE.
  • [MeSH-major] Dermatitis, Atopic / drug therapy. Dibenzoxepins / therapeutic use. Histamine H1 Antagonists, Non-Sedating / therapeutic use. Pruritus / drug therapy
  • [MeSH-minor] Animals. Cytokines / analysis. Dermatophagoides farinae / immunology. Disease Models, Animal. Female. Immunoglobulin E / blood. Mice. Nerve Growth Factor / genetics. Neurites / drug effects. Neurites / physiology. Olopatadine Hydrochloride. Rats. Rats, Wistar. Semaphorin-3A / genetics. Th2 Cells / immunology

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  • [Copyright] Copyright © 2010 S. Karger AG, Basel.
  • (PMID = 20407268.001).
  • [ISSN] 1423-0097
  • [Journal-full-title] International archives of allergy and immunology
  • [ISO-abbreviation] Int. Arch. Allergy Immunol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Switzerland
  • [Chemical-registry-number] 0 / Cytokines; 0 / Dibenzoxepins; 0 / Histamine H1 Antagonists, Non-Sedating; 0 / Semaphorin-3A; 2XG66W44KF / Olopatadine Hydrochloride; 37341-29-0 / Immunoglobulin E; 9061-61-4 / Nerve Growth Factor
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95. El-Didamony AM: Extractive spectrophotometric methods for the determination of oxomemazine hydrochloride in bulk and pharmaceutical formulations using bromocresol green, bromocresol purple and bromophenol blue. Arch Pharm (Weinheim); 2005 Apr;338(4):190-7
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  • [Title] Extractive spectrophotometric methods for the determination of oxomemazine hydrochloride in bulk and pharmaceutical formulations using bromocresol green, bromocresol purple and bromophenol blue.
  • Three simple, sensitive and accurate spectrophotometric methods have been developed for the determination of oxomemazine hydrochloride in bulk and pharmaceutical formulations.
  • [MeSH-major] Cyclic S-Oxides / analysis. Histamine Antagonists / analysis. Phenothiazines / analysis

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  • Hazardous Substances Data Bank. Bromophenol Blue .
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  • (PMID = 15864789.001).
  • [ISSN] 0365-6233
  • [Journal-full-title] Archiv der Pharmazie
  • [ISO-abbreviation] Arch. Pharm. (Weinheim)
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Chemical-registry-number] 0 / Cyclic S-Oxides; 0 / Histamine Antagonists; 0 / Indicators and Reagents; 0 / Phenothiazines; 0 / Solvents; 0R2969YC90 / Bromphenol Blue; 201C22C3EC / Bromcresol Purple; 305MB38V1C / oxomemazine; 8YGN0Y942M / Bromcresol Green
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96. Gschwend MH, Guserle R, Erenmemişoglu A, Martin W, Tamur U, Kanzik I, Hincal AA: Pharmacokinetics and bioequivalence study of ranitidine film tablets in healthy male subjects. Arzneimittelforschung; 2007;57(6):315-9
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  • The aim of the present study was to compare the bioavailability of ranitidine (CAS 66357-35-5) from two different ranitidine hydrochloride (CAS 66357-59-3) film tablets (Ranitab 150 mg film tablets as test preparation and 150 mg film tablets of the originator product as reference preparation).
  • [MeSH-major] Histamine H2 Antagonists / pharmacokinetics. Ranitidine / pharmacokinetics

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  • (PMID = 17688076.001).
  • [ISSN] 0004-4172
  • [Journal-full-title] Arzneimittel-Forschung
  • [ISO-abbreviation] Arzneimittelforschung
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article; Randomized Controlled Trial
  • [Publication-country] Germany
  • [Chemical-registry-number] 0 / Histamine H2 Antagonists; 0 / Tablets; 884KT10YB7 / Ranitidine
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97. Amano T, Takeda T, Yano H, Tamura T: Olopatadine hydrochloride accelerates the recovery of skin barrier function in mice. Br J Dermatol; 2007 May;156(5):906-12
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  • [Title] Olopatadine hydrochloride accelerates the recovery of skin barrier function in mice.
  • Olopatadine hydrochloride (olopatadine; Allelock; Kyowa Hakko Kogyo Co., Ltd, Shizuoka, Japan) is an antiallergic drug with histamine H(1) receptor antagonistic action.
  • [MeSH-major] Dibenzoxepins / pharmacology. Histamine H1 Antagonists, Non-Sedating / pharmacology. Skin Physiological Phenomena / drug effects. Water Loss, Insensible / drug effects
  • [MeSH-minor] Animals. Betamethasone / adverse effects. Epidermis / pathology. Glucocorticoids / adverse effects. Histamine Release / drug effects. Hyperplasia / prevention & control. Male. Mice. Mice, Inbred ICR. Olopatadine Hydrochloride

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  • (PMID = 17355233.001).
  • [ISSN] 0007-0963
  • [Journal-full-title] The British journal of dermatology
  • [ISO-abbreviation] Br. J. Dermatol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Dibenzoxepins; 0 / Glucocorticoids; 0 / Histamine H1 Antagonists, Non-Sedating; 2XG66W44KF / Olopatadine Hydrochloride; 9842X06Q6M / Betamethasone
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98. Kiss B, Horváth A, Némethy Z, Schmidt E, Laszlovszky I, Bugovics G, Fazekas K, Hornok K, Orosz S, Gyertyán I, Agai-Csongor E, Domány G, Tihanyi K, Adham N, Szombathelyi Z: Cariprazine (RGH-188), a dopamine D(3) receptor-preferring, D(3)/D(2) dopamine receptor antagonist-partial agonist antipsychotic candidate: in vitro and neurochemical profile. J Pharmacol Exp Ther; 2010 Apr;333(1):328-40
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  • Cariprazine {RGH-188; trans-N-[4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]cyclohexyl]-N',N'-dimethylurea hydrochloride}, a novel candidate antipsychotic, demonstrated approximately 10-fold higher affinity for human D(3) versus human D(2L) and human D(2S) receptors (pKi 10.07, 9.16, and 9.31, respectively).
  • Moderate or low affinity for histamine H(1) and 5-HT(2C) receptors (pK(i) 7.63 and 6.87, respectively) suggest cariprazine's reduced propensity for adverse events related to these receptors.
  • [MeSH-minor] 4-Butyrolactone / pharmacology. Animals. Aripiprazole. Brain / drug effects. Brain / metabolism. Cell Line. Cricetinae. Cricetulus. Cyclic AMP / biosynthesis. Dopamine / metabolism. Drug Partial Agonism. Guinea Pigs. Humans. In Vitro Techniques. Inositol Phosphates / biosynthesis. Male. Mice. Quinolones / pharmacology. Radioligand Assay. Rats. Receptors, Histamine H1 / metabolism. Receptors, Serotonin / metabolism. Recombinant Proteins / agonists. Recombinant Proteins / antagonists & inhibitors. Reserpine / pharmacology. Serotonin / metabolism

  • Hazardous Substances Data Bank. RESERPINE .
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  • (PMID = 20093397.001).
  • [ISSN] 1521-0103
  • [Journal-full-title] The Journal of pharmacology and experimental therapeutics
  • [ISO-abbreviation] J. Pharmacol. Exp. Ther.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Antipsychotic Agents; 0 / Dopamine D2 Receptor Antagonists; 0 / Inositol Phosphates; 0 / Piperazines; 0 / Quinolones; 0 / Receptors, Dopamine D3; 0 / Receptors, Histamine H1; 0 / Receptors, Serotonin; 0 / Recombinant Proteins; 333DO1RDJY / Serotonin; 82VFR53I78 / Aripiprazole; 8B1QWR724A / Reserpine; E0399OZS9N / Cyclic AMP; F6RJL8B278 / cariprazine; OL659KIY4X / 4-Butyrolactone; VTD58H1Z2X / Dopamine
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99. Rossoni G, Manfredi B, Razzetti R, Civelli M, Bongrani S, Berti F: Positive interaction of the beta2-agonist CHF 4226.01 with budesonide in the control of bronchoconstriction induced by acetaldehyde in the guinea-pigs. Br J Pharmacol; 2005 Feb;144(3):422-9
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  • Pretreatment of anaesthetized guinea-pigs with either CHF 4226.01 (8-hydroxy-5-[(1R)-1-hydroxy-2-[N-[(1R)-2-(p-methoxyphenyl)-1-methylethyl]amino]ethyl] carbostyril hydrochloride), formoterol or budesonide reduced acetaldehyde (AcCHO)-evoked responses in the lungs with a rank order of potency CHF 4226.01 (ED(50) values, from 1.88 to 3.31 pmol) > formoterol (ED(50) values, from 3.03 to 5.51 pmol) >> budesonide (ED(50) values, from 335 to 458 nmol).
  • [MeSH-minor] Amphetamines. Animals. Capillary Permeability / drug effects. Dose-Response Relationship, Drug. Drug Synergism. Ethanolamines / pharmacology. Formoterol Fumarate. Guinea Pigs. Histamine / blood. Inosine Triphosphate / pharmacology. Male. Quinolones. Substance P / pharmacology

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  • (PMID = 15655502.001).
  • [ISSN] 0007-1188
  • [Journal-full-title] British journal of pharmacology
  • [ISO-abbreviation] Br. J. Pharmacol.
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Adrenergic beta-2 Receptor Agonists; 0 / Adrenergic beta-Agonists; 0 / Amphetamines; 0 / Bronchodilator Agents; 0 / Ethanolamines; 0 / Ethylamines; 0 / Hydroxyquinolines; 0 / Quinolones; 132-06-9 / Inosine Triphosphate; 33507-63-0 / Substance P; 51333-22-3 / Budesonide; 820484N8I3 / Histamine; 9810NUL4D1 / carmoterol; GO1N1ZPR3B / Acetaldehyde; W34SHF8J2K / Formoterol Fumarate
  • [Other-IDs] NLM/ PMC1576020
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100. Oliva A, Partemi S, Arena V, De Giorgio F, Colecchi C, Fucci N, Pascali VL: Fatal injection of ranitidine: a case report. J Med Case Rep; 2008;2:232
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  • INTRODUCTION: Ranitidine hydrochloride (Zantac), a histamine-2-receptor antagonist, is a widely used medication with an excellent safety record.

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  • (PMID = 18637187.001).
  • [ISSN] 1752-1947
  • [Journal-full-title] Journal of medical case reports
  • [ISO-abbreviation] J Med Case Rep
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Other-IDs] NLM/ PMC2488348
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