亚甲二氧基甲基苯丙胺与大鼠和人细胞色素 P450 抑制性代谢产物复合物的形成。CYP 2D 的特殊参与。
Inhibitory metabolite complex formation of methylenedioxymethamphetamine with rat and human cytochrome P450. Particular involvement of CYP 2D.
机构信息
C.E.A Saclay, DSV/DRM/SPI, Bât. 136, 99191, Gif sur Yvette, Cedex, France; Université René Descartes, Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, CNRS URA 400, 45 rue des Saints-Pères, 75270, Paris, Cedex 06, France.
出版信息
Environ Toxicol Pharmacol. 1999 Jul;7(3):153-8. doi: 10.1016/s1382-6689(99)00007-1.
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.
亚甲二氧基甲基苯丙胺（MDMA 或摇头丸）是一种在锐舞派对中常用的常见消遣性药物。不幸的是，MDMA 可能会对神经系统产生影响，在某些情况下还会导致肝毒性。MDMA 与大鼠和人肝微粒体制剂中的细胞色素 P450 结合。无论是亚甲二氧基还是甲氨基功能发生代谢转化，都会形成一种抑制性 P450 代谢物复合物。这种抑制性复合物主要与 P450 2D 同工酶形成。这种复合物的形成可能解释了摄入 MDMA 后观察到的临床毒性，特别是与其他通常由 P450 2D6 代谢的化合物一起摄入时。
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