虽然1934年 Goldblatt 就提出了实验性肾缺血性高血压的著名实验,但六十年代以后才逐渐阐明了肾素-血管紧张素-醛固酮(R-A-A)系统与高血压的关系,近年来又有了许多新进展,其拮抗剂的寻找与应用,应运而生。为阐明其药理机制与临床应用,先简要复习 R-A-A 系统在高血压发病中的重要作用(图1)。八肽的血管紧张素Ⅱ(A_Ⅱ)具有强烈的缩血管作用,并刺激肾上腺皮质球状带释放醛固酮,使水钠潴留。A_Ⅱ还可被氨基肽酶水解为七肽的血管紧张素Ⅲ(A_Ⅲ), Although Goldblatt proposed a well-known experiment in experimental renal ischemic hypertension in 1934, the relationship between the renin-angiotensin-aldosterone (RAA) system and hypertension was gradually elucidated after the 1960s and in recent years A lot of new progress, the search for its antagonist and application, came into being. To elucidate its pharmacological mechanisms and clinical applications, a brief review of the R-A-A system in the pathogenesis of hypertension plays an important role (Figure 1). Octapeptide angiotensin Ⅱ (A_ Ⅱ) has a strong vasoconstrictor effect, and stimulate the release of corticospinal aldosterone, sodium and water retention. A_Ⅱ can also be hydrolyzed by aminopeptidase to heptapeptide angiotensin Ⅲ (A_Ⅲ)