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Flavin-containing monooxygenase 1-catalysed N,N-dimethylamphetamine N-oxidation

Title
Flavin-containing monooxygenase 1-catalysed N,N-dimethylamphetamine N-oxidation
Author
유혜현
Keywords
N,N-dimethylamphetamine (DMA); flavin-containing monooxygenase; N-oxidation; N,N-dimethylamphetamine N-oxide (DMANO)
Issue Date
2009-09
Publisher
TAYLOR & FRANCIS LTD
Citation
XENOBIOTICA, v. 39, No. 9, Page. 680-686
Abstract
N,N-dimethylamphetamine (DMA) is a methamphetamine analogue known to be a weaker central nervous system stimulant than methamphetamine. Although a major metabolite of DMA is known to be DMA N-oxide (DMANO), which may be catalysed by flavin-containing monooxygenase (FMO), the specific enzyme(s) involved in this biotransformation has not been identified. In this study, the specific enzyme(s) involved with DMA N-oxidation was characterized by several assays. When DMA was incubated with different 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: K(m) of 44.5 mu M, V(max) of 7.59 nmol min(-1) mg(-1) protein, and intrinsic clearance of 171 mu l min(-1) mg(-1) protein, which was about twelve-fold higher than that by FMO3. Imipramine, an FMO1-specific inhibitor, selectively inhibited DMA N oxidation. The resulting data showed that DMA N oxidation is mainly mediated by FMO1.
URI
https://www.tandfonline.com/doi/abs/10.1080/00498250902998699http://repository.hanyang.ac.kr/handle/20.500.11754/76309
ISSN
0049-8254
DOI
10.1080/00498250902998699
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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