鉴于血管紧张素Ⅱ(AngⅡ)在调节心血管功能方面的关键作用,自其发现了30余年来,已进行了广泛的研究。在此期间,肾素-血管紧张素系统(RAS),的组分已经被作为治疗的靶。早期的进展是解释其血管紧张素肽的构效关系(SAR),并找到AngⅡ的强的特异性肽类拮抗剂,但FDA对此类化合物只批准了一个有限地用于心血管疾病的药物,即沙拉新(saralasin),但未能开发成治疗药物。原因是其具有肽的本性,残余的激动活性以及口服无效。 Given the pivotal role of angiotensin II in the regulation of cardiovascular function, extensive research has been conducted since it was discovered for more than 30 years. During this time, the components of the renin-angiotensin system (RAS) have been used as targets for therapy. Early advances explained the structure-activity relationship (SAR) of its angiotensin and found strong, specific peptide antagonists of angiotensin II, but the FDA approved only a limited class of drugs for cardiovascular disease , Namely saralasin, but failed to develop a therapeutic drug. The reason is that it has the nature of peptide, residual agonistic activity, and oral inactivity.