新型血管紧张素Ⅱ受体和内皮素受体双重拮抗剂研究进展  

Development of Novel Dual Angiotesin Ⅱ and Endothelin Receptor Antagonists

作　　者：魏臻[1] 徐进宜[1] 吴晓明[1] 华维一[1] 

机构地区：[1]中国药科大学药物化学教研室,江苏南京210009

出　　处：《药学进展》2006年第5期193-199,共7页Progress in Pharmaceutical Sciences

基　　金：国家自然科学基金项目(30371688);教育部重点项目(重点03089)

摘　　要：简要介绍新型血管紧张素Ⅱ和内皮素受体双重拮抗剂的研究开发近况,并讨论其作用机制及构效关系。血管紧张素受体和内皮素受体双重拮抗剂以AngⅡ和ET1之间的双向正反馈机制作为其治疗高血压的主要靶点。此类化合物对AngⅡ受体和ET1受体兼有拮抗作用,因此有可能比单一的血管紧张素受体或内皮素受体拮抗剂疗效好,适应范围更广。Dual angiotensin Ⅱ and endothelin receptor antagonist is a novel class of potent and oral cardiovascular agents for the treatment of hypertension and hypertension complication. The main target of this class of antagonist is the bidirectional feedback mechanism between angiotensin Ⅱ and endothelin. Thus, the dual action receptor antagonists （DARAs） may have greater efficacy and broader utility compared with each drug alone. In the paper, the molecular basis, structure-activity relationship （SAR） as well as the advances in R＆D of DARAs were reviewed.

关 键 词：血管紧张素Ⅱ受体 内皮素受体 双重拮抗荆 BMS-248360 BMS-346567 

分 类 号：R972[医药卫生—药品]