Inhibitory metabolite complex formation of methylenedioxymethamphetamine with rat and human cytochrome P450. Particular involvement of CYP 2D

被引：39

作者：

Delaforge, M

Jaouen, M

Bouille, G

机构：

[1] CEA Saclay, DSV, DRM, SPI, F-99191 Gif Sur Yvette, France

[2] Univ Paris 05, Chim & Biochim Pharmacol & Toxicol Lab, CNRS, URA 400, F-75270 Paris 06, France

来源：

ENVIRONMENTAL TOXICOLOGY AND PHARMACOLOGY | 1999年 / 7卷 / 03期

关键词：

methylenedioxymethamphetamine; ecstasy inhibitory complex; cytochrome P450; metabolism; CYP 2D isozymes;

D O I：

10.1016/S1382-6689(99)00007-1

中图分类号：

X [环境科学、安全科学];

学科分类号：

08 ; 0830 ;

摘要：

Methylenedioxymethamphetamine (MDMA or ecstasy) is a common recreational drug used at rave parties. Unfortunately, MDMA may have neurological effects and in some cases causes hepatotoxicity. MDMA binds to cytochrome P450 in rat and human hepatic microsomal preparations. Upon metabolic transformation of either the methylenedioxy or the methylamino function, it forms an inhibitory P450-metabolite complex. This inhibitory complex is formed predominantly with the P450 2D isozymes. This complex formation may account for the clinical toxicity observed upon ingestion of MDMA, particularly with other compounds normally metabolized by P450 2D6. (C) 1999 Elsevier Science B.V. All rights reserved.

引用

页码：153 / 158

页数：6

共 34 条

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