KINETIC-PROPERTIES OF THE METABOLISM OF IMIPRAMINE AND DESIPRAMINE IN ISOLATED RAT HEPATOCYTES

被引：11

作者：

CHIBA, M ^{[1
]}

FUJITA, S ^{[1
]}

SUZUKI, T ^{[1
]}

机构：

[1] CHIBA UNIV,FAC PHARMACEUT SCI,DEPT BIOPHARMACEUT,1-33 YAYOI CHO,CHIBA 260,JAPAN

来源：

BIOCHEMICAL PHARMACOLOGY | 1990年 / 39卷 / 02期

关键词：

D O I：

10.1016/0006-2952(90)90036-K

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The metabolism of imipramine and desipramine was examined by using isolated rat hepatocytes. The enzyme systems having high-affinity-and-low-capacity and low-affinity-and-high-capacity kinetic properties were found to catalyze aromatic 2-hydroxylations of imipramine and desipramine, and aliphatic N-demethylation of imipramine, respectively. The Km and Vmax values for N-demethylation of imipramine (which formed desipramine) were about 5-10 and 5 times larger than those of both 2-hydroxylations respectively. A competitive inhibition between the 2-hydroxylations of imipramine and desipramine ("parallel pathway interaction") (Chiba M, Fujita S and Suzuki T, J Pharm Sci 77: 944-947, 1988), observed using liver microsomes, was found also in isolated hepatocytes. It was concluded that the characteristics of imipramine metabolism observed in liver microsomes were well reproduced in isolated rat hepatocytes. © 1989.

引用

页码：367 / 372

页数：6

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