Flavin-containing monooxygenase 1-catalysed N,N-dimethylamphetamine N-oxidation
- Flavin-containing monooxygenase 1-catalysed N,N-dimethylamphetamine N-oxidation
- 이상규; 강민정; 진창배; 인문교; 김동현; 유혜현
- FMO; N,N-dimethylamphetamine (DMA); N-oxidation; avin-containing monooxygenase; N,N-dimethylamphetamine N-oxide (DMANO)
- Issue Date
- VOL 39, NO 9, 680-686
- N,N-dimethylamphetamine (DMA) is a methamphetamine analogue known to be a weaker central nerv-
ous system stimulant than methamphetamine. Although a major metabolite of DMA is known to be DMA
N-oxide (DMANO), which may be catalysed by avin-containing monooxygenase (FMO), the speci c
enzyme(s) involved in this biotransformation has not been identi ed. In this study, the speci c enzyme(s)
involved with DMA N-oxidation was characterized by several assays. When DMA was incubated with di er-
ent human recombinant drug-metabolizing enzymes, including FMOs and cytochrome P450s (CYPs), the
formation of DMANO by FMO1 was the most predominant. The Michaelis–Menten kinetic constants for
DMA N-oxidation by FMO1 were: Km of 44.5 μM, Vmax of 7.59 nmol min−1 mg−1 protein, and intrinsic clear-
ance of 171 μl min−1 mg−1 protein, which was about twelve-fold higher than that by FMO3. Imipramine,
an FMO1-speci c inhibitor, selectively inhibited DMA N-oxidation. The resulting data showed that DMA
N-oxidation is mainly mediated by FMO1.
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