Imipramine inhibits soluble enkephalin-degrading aminopeptidase activity in vitro

被引：8
作者：
Gallego, M
Casis, L
Casis, O
机构：
[1] Univ Basque Country, Sch Pharm, Dept Physiol, Vitoria 01080, Spain
[2] Univ Basque Country, Sch Med, Dept Physiol, Vitoria 01080, Spain
来源：
EUROPEAN JOURNAL OF PHARMACOLOGY | 1998年 / 360卷 / 01期
关键词：
imipramine; aminopeptidase; enzyme inhibition;
D O I：
10.1016/S0014-2999(98)00686-4
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Considerable evidence has appeared recently connecting the mechanism of action of some antidepressant drugs with the inhibition of the enzymes responsible for enkephalin degradation. Imipramine in vitro inhibits the enkephalin-degrading aminopeptidase MII and interacts with the enzyme in a mixed competitive-noncompetitive manner. The present work shows that imipramine in vitro also inhibits reversibly soluble enkephalin-degrading aminopeptidase activity in rat brain. Kinetic analysis showed that this enzyme has two different binding sites for the drug, and that imipramine interacts with the enzyme in a mixed noncompetitive-acompetitive way. (C) 1998 Elsevier Science B.V. All rights reserved.
引用
收藏
页码：113 / 116
页数：4
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