四氢小檗碱对β-肾上腺素受体的作用(英文)  

Effect of tetrahydroberberine on β-adrenoceptors

作　　者：江明华[1] 王蕾[1] 杨申[1] 彭红丽[1] 缪永生[1] 金国章 

机构地区：[1]上海医科大学药学院,上海200032 [2]中国科学院上海药物研究所

出　　处：《中国药理学与毒理学杂志》1991年第4期273-275,共3页Chinese Journal of Pharmacology and Toxicology

摘　　要：四氢小檗碱为四氢原小檗碱同类物，但四氢原小檗碱同类物的降压和抗心律失常的作用机理尚待阐明。本文应用放射配基结合试验和离体猪冠状动脉环研究THB对β-肾上腺素受体的作用。结果表明，THB能竞争[^3H]DHA和兔肺细胞膜的部位，其Ki值为2．7±0．4μmol/L;Pro能拮抗NE对猪冠状动脉的扩张，NE的pD2值为6．3±0．2，Pro的pA2为8．8±0．2，THB的作用与Pro既相似又有区别，表现为NE的对数浓度反应曲线右移又压低的双重拮抗作用，其pA2为7．7±1．3，PD2值为5．1±，以上结果提示，THB为β-肾上腺素受体拮抗剂，此外，它对其它受体 能有亲和力。The affinity of tetrahydroberberine (THB) to β-adrenoceptors was investigated in the isolated rabbit lung cell membranes by radioligand binding assay. [3H]DHA binding assay showed that THB specifically displayed binding affinity to β-adrenoceptors. The K; of THB was 2.7+ 0.4 μmol/L. The logarithmic cumulative concentration-response curves of THB for NE on the pig coronary artery rings showed that the position of curves was changed and the crest depressed. The values of pA2 and pD2 were 7.7?1.3 and 5.1?0.2 respectively. As a control, propranolol (Pro) could shift the curves parallelly to the right and the pA2 value of Pro was 8.8 ?0.2.It is suggested that THB is a β-adrenoceptor antagonist and has affinities to more than one kind of receptor.

关 键 词：结合位点 冠状血管 Β-肾上腺素受体 四氢小檗碱 普萘洛尔 

分 类 号：R972[医药卫生—药品]