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[中氮茚二脱氢-4-甲基-5-苯基-1,3,4-噻二唑烷-2-硫酮(LU 2443)的生物转化及药代动力学。大鼠体内生物转化研究]

[Biotransformation and pharmacokinetics of mesoionic didehydro-4-methyl-5-phenyl-1,3,4-thiadiazolidine-2-thione (LU 2443). Studies on its biotransformation in rats].

作者信息

Neidlein R, Eder T

出版信息

Arzneimittelforschung. 1982;32(10):1292-8.

PMID:6891230
Abstract

The metabolism of the antiepileptic mesoionic didehydro-4-methyl-5-phenyl-1,3,4-thiadiazolidine-2-thione (LU 2443) was investigated after p.o. application in rats. The main metabolite was benzoic acid, besides the unchanged material and hippuric acid the spasmodically compounds N-methyl-benzamide and mesionic didehydro-4-methyl-5-phenyl-1,3,4-thiadiazolidine-2-one were detectable. In-vitro experiments could be demonstrated that LU 2443 was not demethylated by biochemical oxidation, and LU 2443 was also very stable against metabolizing influences by enteric bacteria.

摘要

在大鼠口服抗癫痫的中氮茚二脱氢-4-甲基-5-苯基-1,3,4-噻二唑烷-2-硫酮(LU 2443)后,对其代谢情况进行了研究。主要代谢产物是苯甲酸,除了未变化的物质和马尿酸外,还可检测到痉挛性化合物N-甲基苯甲酰胺和中氮茚二脱氢-4-甲基-5-苯基-1,3,4-噻二唑烷-2-酮。体外实验表明,LU 2443不会通过生化氧化发生去甲基化,并且LU 2443对肠道细菌的代谢影响也非常稳定。

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