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盐酸3-甲基-5,6,7,8-四氢喹啉-8-硫代甲酰胺(替喹酰胺)对胃肠道及自主神经系统的作用

The gastrointestinal and autonomic effects of 3-methyl-5,6,7,8-tetrahydroquinoline-8-thiocarboxamide hydrochloride (tiquinamide).

作者信息

Beattie D E, Dixon G T, Waterfall J F, Alps B J

出版信息

Arzneimittelforschung. 1979;29(10):1564-9.

PMID:583223
Abstract

3-Methyl-5,6,7,8-tetrahydroquinoline-8-thiocarboxamide hydrochloride (tiquinamide), a potent gastric anti-secretory compound, affords good protection against stress- and chemically-induced gastric and duodenal erosions. It causes a dose-related delay in gastric emptying and intestinal transit, and does not have a primary effect on gastric mucosal blood flow. The only actions of tiquinamide on the peripheral autonomic nervous system are weak, but apparently specific, histamine H2-receptor blocking activity, and non-competitive inhibition of acetylcholine and histamine responses at 10(-3) mol/l. Since no other effect on isolated tissues can be detected, it seems unlikely that the antisecretory action of tiquinamide involves a direct action on the peripheral autonomic nervous system.

摘要

3-甲基-5,6,7,8-四氢喹啉-8-硫代甲酰胺盐酸盐(替喹酰胺)是一种有效的胃抗分泌化合物,对应激和化学诱导的胃及十二指肠糜烂具有良好的保护作用。它会导致胃排空和肠道转运出现剂量相关的延迟,并且对胃黏膜血流没有主要影响。替喹酰胺对周围自主神经系统的唯一作用较弱,但显然具有特异性,即组胺H2受体阻断活性,以及在10(-3)mol/L时对乙酰胆碱和组胺反应的非竞争性抑制。由于在离体组织上未检测到其他作用,替喹酰胺的抗分泌作用似乎不太可能涉及对周围自主神经系统的直接作用。

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