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大鼠肝微粒体对1,1 - 二氯 - 顺式 - 二苯环丙烷的代谢作用

Metabolism of 1,1-dichloro-cis-diphenylcyclopropane by rat liver microsomes.

作者信息

Caputo O, Grosa G, Ceruti M, Rocco F, Biglino G

机构信息

Istituto di Chimica Farmaceutica Applicata, Università di Torino, Italia.

出版信息

Drug Metab Dispos. 1990 Sep-Oct;18(5):771-8.

PMID:1981735
Abstract

The metabolic fate of the anti-estrogen 1,1-dichloro-cis-diphenylcyclopropane (Analog II), was studied in vitro with phenobarbital-induced rat liver microsomal fractions. The presence of five metabolites was directly or indirectly established. Biotransformation products were isolated by TLC and HPLC techniques and, when possible, the structures were confirmed through comparison with synthetic samples. The presence of an allyl chloride, highly reactive, metabolic intermediate was stated.

摘要

使用苯巴比妥诱导的大鼠肝微粒体组分在体外研究了抗雌激素1,1 - 二氯 - 顺式 - 二苯基环丙烷(类似物II)的代谢命运。直接或间接确定了五种代谢物的存在。通过薄层层析(TLC)和高效液相色谱(HPLC)技术分离生物转化产物,并在可能的情况下,通过与合成样品比较来确认结构。有报道称存在一种高反应性的烯丙基氯代谢中间体。

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