Stereospecific oxidation of the (S)-enantiomer of RS-8359, a selective and reversible monoamine oxidase A (MAO-A) inhibitor, by aldehyde oxidase.
作者： K. Itoh , M. Yamamura , S. Muramatsu , K. Hoshino , A. Masubuchi
DOI: 10.1080/00498250500202106
关键词:
摘要: In a previous paper by the authors on RS-8359, new selective and reversible monoamine oxidase A (MAO-A) inhibitor, it was reported that (S)-enantiomer of RS-8359 is rapidly eliminated from rats, monkeys humans as result formation 2-oxidative metabolite. The present study investigates properties enzyme responsible for 2-oxidation RS-8359. Subcellular localization, cofactor requirement inhibitory effects typical compounds were studied using rat liver preparations. addition, purified cytosol further characterization. activity localized in cytosolic fraction without need any extensively inhibited menadione, chlorpromazine quinacrine. also homodimer with monomeric molecular weight 140 kDa had an A280/A450 ratio 5.1 absorption spectrum. results suggest biotransformation to gi...
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