PHARMACOLOGICAL PROFILE OF A NONPEPTIDIC DUAL INHIBITOR OF NEUTRAL ENDOPEPTIDASE-24.11 AND ENDOTHELIN-CONVERTING ENZYME

被引：83

作者：

DELOMBAERT, S

GHAI, RD

JENG, AY

TRAPANI, AJ

WEBB, RL

机构：

[1] Research Department, Pharmaceuticals Division, CIBA-GEIGY Corporation, Summit

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1994年 / 204卷 / 01期

关键词：

D O I：

10.1006/bbrc.1994.2473

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

CGS 26303 is a potent and structurally unique non-peptidic inhibitor of neutral endopeptidase (NEP) capable of protecting atrial natriuretic peptide (ANP) from enzymatic degradation. In addition, CGS 26303 displays modest endothelin-converting enzyme (ECE) inhibitory activity in vitro. Unlike CGS 24592, a potent but selective NEP inhibitor, CGS 26303 significantly blocks endothelin-1 production in rats after exogenous administration of big ET-1 and reduces the mean arterial pressure in spontaneously hypertensive rats during chronic administration. These results suggest that CGS 26303 represents a new class of therapeutic agents with potential benefits for the treatment of cardiovascular and renal disorders. (C) 1994 Academic Press,

引用

页码：407 / 412

页数：6

共 30 条

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