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利多氟嗪在大鼠和犬肝脏匀浆中的体外代谢。

In vitro metabolism of lidoflazine by rat and dog liver fractions.

作者信息

Meuldermans W, Lauwers W, Knaeps A, Heykants J

出版信息

Arzneimittelforschung. 1977;27(4):828-32.

PMID:577461
Abstract

Lidoflazine was metabolized very rapidly by 16000 g supernatant fractions of rat and dog liver. The rate and the extent of metabolism were considerably superior for rat liver. Lidoflazine metabolites were purified by extraction and thin-layer chromatography and identified by mass spectrometry. The main pathways of the in vitro metabolism by rat and dog liver fractions were the same. Oxidative N-dealkylation was the most important. An incubation of major metabolite 1-[4,4-bis(4-fluorophenyl)-butyl]piperazine, with rat liver fraction was performed. A hydroxylated metabolite and a ketopiperazine metabolite were detected only in the dog experiments.

摘要

利多氟嗪在大鼠和犬肝脏的16000g上清液组分中代谢非常迅速。大鼠肝脏的代谢速率和程度明显更高。利多氟嗪代谢物通过萃取和薄层色谱法纯化,并通过质谱法鉴定。大鼠和犬肝脏组分体外代谢的主要途径相同。氧化N-去烷基化是最重要的。用大鼠肝脏组分对主要代谢物1-[4,4-双(4-氟苯基)-丁基]哌嗪进行了孵育。仅在犬实验中检测到一种羟基化代谢物和一种酮哌嗪代谢物。

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