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豚鼠和兔组织制剂对N,N-二甲基苯胺的体外代谢

The in vitro metabolism of N,N-dimethylaniline by guinea pig and rabbit tissue preparations.

作者信息

Gorrod J W, Gooderham N J

出版信息

Eur J Drug Metab Pharmacokinet. 1981;6(3):195-206. doi: 10.1007/BF03189489.

Abstract

A study of the in vitro metabolism of N,N-dimethylaniline using guinea pig and rabbit preparations and GLC techniques has confirmed N-demethylation and N-oxidation and established ring hydroxylation as metabolic routes. Whereas N-demethylation and N-oxidation are major routes of metabolism, ring hydroxylation is a comparatively minor pathway. Like N-demethylase and N-oxidase, the 4-hydroxylase has been shown to be a microsomal enzyme. The major ring hydroxylated product of N,N-dimethylaniline is N,N-dimethyl-4-aminophenol; N-methyl-4-aminophenol is subsequently formed. The apparent Km and V max values for N-demethylation, N-oxidation and 4-hydroxylation, are presented for both the guinea pig and the rabbit.

摘要

一项利用豚鼠和兔制剂以及气相色谱技术对N,N-二甲基苯胺进行体外代谢研究,证实了N-去甲基化和N-氧化,并确定环羟基化是代谢途径。虽然N-去甲基化和N-氧化是主要代谢途径,但环羟基化是相对次要的途径。与N-去甲基酶和N-氧化酶一样,4-羟化酶已被证明是一种微粒体酶。N,N-二甲基苯胺的主要环羟基化产物是N,N-二甲基-4-氨基苯酚;随后形成N-甲基-4-氨基苯酚。给出了豚鼠和兔N-去甲基化、N-氧化和4-羟化的表观Km和Vmax值。

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