中国药科大学学报2004，Vol.35Issue(6)：552-557,6.
内皮素受体拮抗剂CPU 0213的生物活性及抑制ETA及ETB受体的作用
Endothelin Receptor Antagonist Activity and Selective Blocking the ETA and ETB of Compound 0213
摘要
Abstract
AIM:To search for a novel endothelin receptor antagonist compound 0213 by testing its biological activities.METHOD: The functional suppression tests of endothelin-1 (ET-1) induced contraction of rat thoracic aorta and ET-1 binding on myocardium served as the preliminary tests for 77 new compounds and compound 0213 was chosen to search for the potency and selectivity of effects on the ETA and ETB receptor of rat myocardium,thoracic aortic and guinea pig bronchial smooth muscle.RESULT: Compound 0213 was effective to suppress the vaso-contraction and ET-1 bindings on rat myocardial membrane preparation.The pA2 to suppress ET-1 induced contraction of rat thoracic aorta (mediated by ETA) and sarafotoxin (S6c) induced contraction of guinea pig bronchial smooth muscles (ETB mediated ) was (8.52±0.26) and (7.28±0.04),respectively. The potency to suppress ETA and ETB of compound 0213 was (2.57±1.41) nmol/L (n=9) and (95±34) nmol/L (n=5).The potency and selectivity of compound 0213 was better than that of Bosentan.CONCLUSION:A novel endothelin receptor antagonist compound 0213 is promising to be a useful agent in dealing with cardiovascular disorders.关键词
内皮素受体拮抗剂/放射受体分析/心肌/血管平滑肌Key words
Endothelin receptor antagonists/Radio receptor assay/Myocardium/Vascular smooth muscle/Bronchial smooth muscle/Endothelin receptor subtype分类
医药卫生引用本文复制引用
戴德哉,吉民,黄敏,刘立钢..内皮素受体拮抗剂CPU 0213的生物活性及抑制ETA及ETB受体的作用[J].中国药科大学学报,2004,35(6):552-557,6.基金项目
国家自然科学基金资助项目(No.30230170,No.30171078) （No.30230170,No.30171078）
