EFFECT OF SQ29,852, A NEW ANGIOTENSIN CONVERTING ENZYME (ACE) INHIBITOR WITH A PHOSPHONIC ACID GROUP, ON THE ACTIVITY OF ANGIOTENSIN CONVERTING ENZYME FROM HUMAN KIDNEY

被引：8

作者：

HIWADA, K ^{[1
]}

INOUE, Y ^{[1
]}

KOKUBU, T ^{[1
]}

机构：

[1] EHIME UNIV, SCH MED, DEPT INTERNAL MED 2, SHIGENOBU, EHIME 79102, JAPAN

来源：

GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM | 1990年 / 21卷 / 04期

关键词：

D O I：

10.1016/0306-3623(90)90714-W

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1. An in vitro experiment was carried out to compare the inhibitory effect of SQ29,852 on human renal angiotensin converting enzyme (ACE) with those of captopril, enalapril and enalaprilat. 2. SQ29,852 strongly inhibited human renal ACE; its IC50 value was 1.5 × 10-8 M. In terms of the IC50, SQ29,852′s efficacy was about 1/10 of that of captopril and 1/28 of that of enalaprilat, but it was about 14 times more potent than enalapril. 3. SQ29,852 showed no inhibitory effects on cathepsin D, urinary kallikrein, renal renin, pepsin, trypsin and chymotrypsin. Its ACE-specificity was higher than that of captopril. 4. ACE inhibition by SQ29,852 was shown to be competitive, as revealed by Lineweaver-Burk plots. The affinity of SQ29,852 to ACE was shown to be high by a Ki value of 1.2 × 10-8 M. © 1990.

引用

页码：555 / 558

页数：4

共 19 条

[1]

Alexander JC, 1981, ANGIOTENSIN CONVERTI, P379

[2]

Amundsen E, 1979, Adv Exp Med Biol, V120A, P83

[3]

ATKINSON AB, 1980, LANCET, V2, P105

[4]

BARRETT AJ, 1979, PROTEINASES MAMMALIA, P209

[5]

Bergmeyer H., 1986, METHOD ENZYMAT AN, P119

[6] ORAL ANGIOTENSIN-CONVERTING ENZYME-INHIBITOR IN LONG-TERM TREATMENT OF HYPERTENSIVE PATIENTS [J].

BRUNNER, HR ;

GAVRAS, H ;

WAEBER, B ;

KERSHAW, GR ;

TURINI, GA ;

VUKOVICH, RA ;

MCKINSTRY, DN ;

GAVRAS, I .

ANNALS OF INTERNAL MEDICINE, 1979, 90 (01) :19-23

[7] SPECTROPHOTOMETRIC ASSAY AND PROPERTIES OF ANGIOTENSIN-CONVERTING ENZYME OF RABBIT LUNG [J].

CUSHMAN, DW ;

CHEUNG, HS .

BIOCHEMICAL PHARMACOLOGY, 1971, 20 (07) :1637-+

[8]

Erdos E., 1979, HDB EXPT PHARM S, VXXV, P427

[9] CAPTOPRIL - A PRELIMINARY REVIEW OF ITS PHARMACOLOGICAL PROPERTIES AND THERAPEUTIC EFFICACY [J].

HEEL, RC ;

BROGDEN, RN ;

SPEIGHT, TM ;

AVERY, GS .

DRUGS, 1980, 20 (06) :409-452

[10] LACK OF INHIBITION OF HUMAN RENIN BY HUMAN DES-ANGIOTENSIN-I RENIN SUBSTRATE [J].

HIWADA, K ;

SOGO, Y ;

TAKADA, Y ;

KOKUBU, T .

BIOCHEMICAL PHARMACOLOGY, 1981, 30 (18) :2630-2631

← 1 2 →