肾素抑制剂的研究进展

Progress in the research of renin inhibitors

肾素血管经张素系统在高血压的发生发展过程中起着很重要的作用,肾素抑制剂与血管紧张素转换酶抑制剂、血管紧张素Ⅱ受体拮抗剂等抗高血压药物的作用机制不同,它作用于肾素-血管紧张素系统的限速步骤,是阻断肾素血管紧张素系统的新途径,为高血压的药物治疗提供了新思路。但由于肾素有种属特异性,肾素抑制剂曾因生物利用度低和合成复杂,使其研究遇到了大量困难。随着首个口服非肽类肾素抑制剂阿利吉仑的合成以及临床试验的展开,肾素抑制剂应用于临床治疗高血压及其并发症成为可能。文中对肾素抑制剂研发的文献进行分析和归纳,综述肾素抑制剂类药物以及第一个口服非肽类肾素抑制剂阿利吉仑的研究进展。

Renin-angiotensin systerm （RAS） plays an important role in the development of hypertension. Distinct from commonly used antihypertensive drugs such as angiotensin-converting enzyme inhibitors and blockers of angiotensin Ⅱ receptor, renin inhihitors block rate-limiting step of the activation of the renin-angiotensin system. Thus, they offer a new way to suppress the RAS and control hypertension. The researches of the renin inhibitors has encountered plenty of difficulties because of its low bioavailability and complicated synthesis course as well as its species specificity. As the first oral non-peptide renin inhibitor ＂Aliskiren＂ has been successfully synthesized, it is possible to apply the renin inhibitors in the treatment of essential hypertension and its complications. This article systematically summarized the literature of the development of the renin inhibitors, and then reviewed the studying progress on the research of the first oral non peptide renin inhibitors ＂Aliskiren＂.