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

被引：45

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.

引用

页码：590 / 592

页数：3

共 16 条

[1] DISTRIBUTION OF ENDOGENOUS BENZODIAZEPINE RECEPTOR LIGAND-MONOAMINE OXIDASE INHIBITORY ACTIVITY (TRIBULIN) IN TISSUES [J].