HISTAMINE AND 1-METHYL-6,7-DIHYDROXY-1,2,3,4-TETRAHYDROISOQUINOLINE ARE COMPETITIVE INHIBITORS OF DEBRISOQUINE 4-MONOOXYGENASE IN RAT-LIVER

被引：4

作者：

IWAHASHI, K

MATSUO, Y

TSUNEOKA, Y

ICHIKAWA, Y

HOSOKAWA, K

SUWAKI, H

机构：

[1] KAGAWA MED SCH HOSP, MIKI, KAGAWA 76107, JAPAN

[2] KAGAWA MED SCH, DEPT BIOCHEM, MIKI, KAGAWA 76107, JAPAN

来源：

ARCHIVES OF TOXICOLOGY | 1993年 / 67卷 / 07期

关键词：

CYP2D1; ACTIVE SITE; DEBRISOQUINE; DOPAMINE RECEPTOR; MPTP; NEUROLEPTICS;

D O I：

10.1007/BF01969924

中图分类号：

R99 [毒物学（毒理学）];

学科分类号：

100405 ;

摘要：

The effects of histamine and 1-methyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline(salsolinol) on debrisoquine 4-monooxygenation, which is catalyzed by cytochrome P-450db1(CYP2D1) in rat liver microsomes, were studied. Both histamine and salsolinol competitively inhibited the activity of debrisoquine 4-monooxygenase (Ki = 0.31 and 0.43 mM, respectively). These data demonstrate that histamine and salsolinol bind to the active site of CYP2D1, i.e. histamine and salsolinol have structures (molecular shape) corresponding to the active site of CYP2D1.

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页码：514 / 516

页数：3

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