血管肽酶抑制劑是單一結(jié)構(gòu)的化合物分子，具有雙重的抑制作用，即抑制血管緊張素轉(zhuǎn)化酶和中性內(nèi)肽酶的活性。能降低腎素–血管緊張素–醛固酮系統(tǒng)的活性，減少血管緊張素Ⅱ及醛固酮的生成；阻止中性內(nèi)肽酶降解心房鈉利尿肽、腦鈉利尿肽等鈉利尿肽及緩激肽，從而產(chǎn)生利尿排鈉、增加血管舒張性的作用，其作用比單用血管緊張素轉(zhuǎn)化酶抑制劑或中性內(nèi)肽酶抑制劑更有效。主要概述了血管肽酶抑制劑的藥理作用及新藥研發(fā)情況。

Vasopeptidase inhibitors are a series of single structure compounds with dual inhibition, that is the inhibition of both angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP). Vasopeptidase inhibitors could decrease the activity of renin-angiotensin-aldosterone system and restrain the generation of angiotensin II and aldosterone, prevent the neutral endopeptidase from degradation against natriuretic peptide, such as atrial natriuretic peptide and bradykinin-related peptides, thereby causing diuretic and natriuretic, increasing blood vessel diastolic function. The functions are more effective than those of ACE inhibitors or NEP inhibitors. This article mainly summarizes the pharmacological functions and new drug development of vasopeptidase inhibitors.