Identification of human cytochrome P450 2D6 as major enzyme involved in the O-demethylation of the designer drug P-methoxymethamphetamine

被引：27

作者：

Staack, RF ^{[1
]}

Theobald, DS ^{[1
]}

Paul, LD ^{[1
]}

Springer, D ^{[1
]}

Kraemer, T ^{[1
]}

Maurer, HH ^{[1
]}

机构：

[1] Univ Saarland, Dept Expt & Clin Toxicol, Inst Expt & Clin Pharmacol & Toxicol, D-66421 Homburg, Germany

来源：

DRUG METABOLISM AND DISPOSITION | 2004年 / 32卷 / 04期

关键词：

D O I：

10.1124/dmd.32.4.379

中图分类号：

R9 [药学];

学科分类号：

1007 [药学];

摘要：

p-Methoxymethamphetamine (PMMA) is a new designer drug, listed in many countries as a controlled substance. Several fatalities have been attributed to the abuse of this designer drug. Previous in vivo studies using Wistar rats had shown that PMMA was metabolized mainly by O-demethylation. The aim of the study presented here was to identify the human hepatic cytochrome P450 ( P450) enzymes involved in the biotransformation of PMMA to p-hydroxymethamphetamine. Baculovirus-infected insect cell microsomes, pooled human liver microsomes (pHLMs), and CYP2D6 poor-metabolizer genotype human liver microsomes (PM HLMs) were used for this purpose. Only CYP2D6 catalyzed O-demethylation.

引用

页码：379 / 381

页数：3

共 21 条

[1]

Involvement of CYP2D6 in the in vitro metabolism of amphetamine, two N-alkylamphetamines and their 4-methoxylated derivatives [J].