Some Aspects of the Pharmacology of Clemizole Hydrochloride*

Murray Finkelstein, Clara M. Kromer, Sheila A. Sweeney, Charles S. Delahunt
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引用次数: 16

Abstract

Experiments have been described which demonstrate effective prolonged antihistaminic activity and other aspects of the pharmacology of clemizole HC1 (1-p-chloro-benzyl-2-pyrrolidyl-methyl-benzimidazole hydrochloride). A relatively high degree of antihistaminic specificity was observed in both in vitro and in vivo experiments. Clemizole was highly effective in antagonizing histamine aerosol bronchospasm. Spontaneous activity of isolated rabbit ileum and intestinal motility in anesthetized dogs were decreased. There was no significant effect on histamine-induced gastric secretion in chronic gastric fistula dogs. Enhanced responses to epinephrine appear to be due to a sensitization to this amine by the antihistamine.

Acute and chronic studies showed a relatively low order of toxicity.

盐酸克列咪唑的药理学研究*
已有实验证明克列咪唑HC1(1-对氯苄基-2-吡咯烷基-甲基-盐酸苯并咪唑)具有有效的长效抗组胺活性和其他药理学方面的作用。在体外和体内实验中均观察到较高程度的抗组胺特异性。克列咪唑对组胺雾化支气管痉挛的拮抗效果显著。兔离体回肠的自发活动和麻醉犬的肠蠕动均下降。组胺对慢性胃瘘犬胃液分泌无显著影响。对肾上腺素的增强反应似乎是由于抗组胺药对这种胺的敏化。急性和慢性研究显示毒性相对较低。
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