INHIBITION OF HISTAMINE-N-METHYLTRANSFERASE (HNMT) BY FRAGMENTS OF 9-AMINO-1,2,3,4-TETRAHYDROACRIDINE (TACRINE) AND BY BETA-CARBOLINES

被引：25

作者：

CUMMING, P ^{[1
]}

VINCENT, SR ^{[1
]}

机构：

[1] UNIV BRITISH COLUMBIA,DEPT PSYCHIAT,VANCOUVER V6T 1W5,BC,CANADA

来源：

BIOCHEMICAL PHARMACOLOGY | 1992年 / 44卷 / 05期

关键词：

D O I：

10.1016/0006-2952(92)90133-4

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Histamine-N-methyltransferase (HNMT), the major enzyme for the metabolism of histamine in rat brain, is potently inhibited by 9-amino-1,2,3,4-tetrahydroacridine (tacrine). Structural fragments of tacrine were less potent inhibitors of rat brain HNMT than was tacrine itself. Harmaline and a number of other beta-carbolines inhibited HNMT with IC50 values in the range of 1-10-mu-M. HNMT inhibition by harmaline was competitive with respect to both substrates, S-adenosylmethionine and histamine (K(i) = 1.4-mu-M). These findings are discussed in the context of mechanisms for HNMT inhibition.

引用

页码：989 / 992

页数：4

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