INHIBITORY POTENCY OF SOME ISATIN ANALOGS ON HUMAN MONOAMINE OXIDASE-A AND OXIDASE-B

被引：44
|
作者：
MEDVEDEV, AE
GOODWIN, B
CLOW, A
HALKET, J
GLOVER, V
SANDLER, M
机构：
[1] QUEEN CHARLOTTES & CHELSEA HOSP,DEPT CHEM PATHOL,GOLDHAWK RD,LONDON W6 0XG,ENGLAND
[2] ACAD MED SCI,INST BIOL & MED CHEM,MOSCOW,USSR
来源：
BIOCHEMICAL PHARMACOLOGY | 1992年 / 44卷 / 03期
关键词：
D O I：
10.1016/0006-2952(92)90454-Q
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Isatin is an endogenous compound which acts as a selective inhibitor of monoamine oxidase (MAO) B. In this study a range of isatin analogues were tested for their in vitro inhibition of human MAO A and B. Most of the analogues were less potent than isatin. Hydroxylation of the aromatic ring changed the inhibitory potency in favour of MAO A, with 5-hydroxyisatin being a potent and selective MAO A inhibitor (IC50 8-mu-M). Isatinic acid, which is formed reversibly from isatin at alkaline pH, showed no inhibition.
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页码：590 / 592
页数：3
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