Inhibitory effects of histamine H1 receptor blocking drugs on metabolic activations of neutrophils.
作者： Katsuhiko TANIGUCHI , Yasusuke MASUDA , Koichiro TAKANAKA
关键词: Chemistry 、 Pharmacology 、 Histamine H1 receptor 、 Clemastine 、 Arachidonic acid 、 Antiallergic agent 、 Oxatomide 、 Leukotriene 、 Homochlorcyclizine 、 Histamine
摘要: Inhibitory effects of various histamine receptor-blocking agents including antiallergic on metabolic activations neutrophils were examined by measuring leukotrienes (C4, D4 and E4) formation, arachidonic acid release superoxide generation. The stimulation calcium ionophore (A23187) causes the production concomitantly with from cells these effectively diminished a variety antihistaminic agents. Almost all H1 drugs studied here showed as inhibitors neutrophils, although degree was dependent drug concentrations. order potency inhibitory were: homochlorcyclizine, clemastine, azelastine (IC50 less than 20 microM) greater oxatomide 60 diphenylpyraline triprolidine, meclizine, diphenhydramine 100 microM). generation activated phorbol 12-myristate 13-acetate also inhibited agents, but generally lower concentrations required to obtain same degrees effects. These results indicated that some drugs, such clemastine may act formation at locus inflammation.
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