血管肽酶抑制剂新药研发的进展.pdfVIP

现代药物与临床 Drugs Clinic 第 27 卷 第 5 期 2012 年 9 月 • 493 • 血管肽酶抑制剂新药研发的进展 1,2 1 1* 梁 艳 ，徐向伟 ，赵专友 1. 天津市新药安全评价研究中心，天津 300193 2. 天津中医药大学，天津 300193 摘 要：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。 关键词：血管肽酶抑制剂；血管紧张素转化酶；中性内肽酶；药理作用；新药研发 中图分类号：R973 文献标志码：A 文章编号：1674 - 5515(2012)05 - 0493 - 05 Research progress in new drugs of vasopeptidase inhibitors 1, 2 1 1 LIANG Yan , XU Xiang-wei , ZHAO Zhuan-you 1. Tianjin Centre for New Drug Safety Assessment and Research, Tianjin 300193, China 2. Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China Abstract: 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. Key words: vasopeptidase inhibitors; angiotensin-converting enzyme (ACE); neutral endopeptidase (NEP); pharmacological actions; new drug research and development 血管内皮细胞和神经体液系统在调节血管张力 不足作用，且看到了两者合用后所