血管肽酶抑制剂是单一结构的化合物分子，具有双重的抑制作用，即抑制血管紧张素转化酶和中性内肽酶的活性。能降低肾素–血管紧张素–醛固酮系统的活性，减少血管紧张素Ⅱ及醛固酮的生成；阻止中性内肽酶降解心房钠利尿肽、脑钠利尿肽等钠利尿肽及缓激肽，从而产生利尿排钠、增加血管舒张性的作用，其作用比单用血管紧张素转化酶抑制剂或中性内肽酶抑制剂更有效。主要概述了血管肽酶抑制剂的药理作用及新药研发情况。

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.