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新型取代嘧啶O 6553(盐酸2-甲氨基-4-N-甲基哌嗪基-5-硫代甲基-6-氯嘧啶)对胃肠道的促动力和止吐作用

Gastrointestinal prokinetic and antiemetic effects of a new substituted pyrimidinO 6553 (2-methylamino-4-N-methylpiperazino-5-thiomethyl-6-chloropyrimidine hydrochloride).

作者信息

Loiseau G, Millischer R, Donadieu A M, Marquet J P

出版信息

Arzneimittelforschung. 1977;27(3):606-11.

PMID:577427
Abstract

2-Methylamino-4-N-methylpiperazino-5-methylthio-6-chloropyrimidine hydrochloride (O 6553) is a new molecule showing an original pharmacological profile in the laboratory tests. It possesses at the same time potent gastro-intestinal prokinetic and central antiemetic properties, demonstrated on the one hand by the gastro-duodenal transit of barium meal in rats, and on the other hand by apomorphine-induced vomiting in dogs. The drug also has interesting anxiolytic and antiserotonin properties and, at doses which change gastro-intestinal behaviour, it is devoid of any untoward side effect. The acute and subacute toxicities of O 6553 show that the drug has a very good safety margin.

摘要

盐酸2-甲氨基-4-N-甲基哌嗪基-5-甲硫基-6-氯嘧啶(O 6553)是一种新分子,在实验室测试中显示出独特的药理学特性。它同时具有强大的胃肠促动力和中枢性止吐特性,一方面通过大鼠钡餐胃肠运输得到证明,另一方面通过阿扑吗啡诱导犬呕吐得到证明。该药物还具有有趣的抗焦虑和抗血清素特性,并且在改变胃肠行为的剂量下,没有任何不良副作用。O 6553的急性和亚急性毒性表明该药物具有非常好的安全范围。

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