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Updated: May 30, 2026

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
Published on: March 28, 2017
Inhibitory metabolite complex formation of methylenedioxymethamphetamine with rat and human cytochrome P450.
M Delaforge1, M Jaouen, G Bouille
1C.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.
Abstract:
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.
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