INHIBITION OF RABBIT LUNG ANGIOTENSIN-CONVERTING ENZYME BY IDRAPRIL

被引：6
|
作者：
LIPPI, A
CRISCUOLI, M
SARDELLI, G
SUBISSI, A
机构：
[1] Dept. of Pharmacology Laboratori Guidotti SpA Co. related to A. Menarini-Industrie Far-maceutiche Ri, 1-56122 San Piero a Grado, Pisa
来源：
BIOCHEMICAL PHARMACOLOGY | 1993年 / 45卷 / 06期
关键词：
D O I：
10.1016/0006-2952(93)90291-4
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Idrapril, the prototype of a new class of angiotensin converting enzyme (ACE) inhibitors, competitively inhibited, with nanomolar apparent K(i), the hydrolysis of hippuryl-glycyl-glycine by rabbit lung ACE. The pre-steady-state analysis of this tight-binding inhibition showed it to be characterized by slow kinetics, but at variance with what was found for enalaprilat in the same conditions, idrapril appeared to act through a simple, single step mechanism. Kinetic K(i) and k(on) and k(off) values were 470 pM, 3.0 +/- 1.5 x 10(6) M-1 sec-1 and 1.4 +/- 0.3 x 10(-3) sec-1, respectively.
引用
收藏
页码：1358 / 1362
页数：5
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