普萘洛尔对大鼠心肌细胞膜α_1肾上腺素受体密度及α_(1A)/α_(1B)比例的影响(英文)  

Altered a1-adrenoceptor density and a1A/a1B ratio in rat hearts after propranolol treatment

作　　者：张缨[1] 华峥 王晓良[1] 

机构地区：[1]中国医学科学院药物研究所

出　　处：《中国药理学报》1994年第4期308-310,共3页Acta Pharmacologica Sinica

基　　金：National Natural Science Foundation of China,№ 38900068.

摘　　要：放射配基结合实验表明,大鼠ip普萘洛尔(Pro)7 d后,心肌细咆膜α_1肾上腺素能受体密度由137±25增加到178±30fmol/mgprotein(P<0.05),KD值无显著改变,5-MU竞争结合实验表明,使用Pro后α_(1A)亚型在α_1受体总数中所占比例由19±6％增加到31±8％(P<0.05),但两种受体亚型的亲和力都未改变。说明β受体阻断后,α_(1A)亚型变化更为敏感。After rats were treated with propranolol (50 mg·kg-1, bid, ip) for 7 d, the density of a1-adrenoceptors in the rat myo-cardial cell membranes increased from 137 ±25 to 178±30 fmol/mg protein determined by receptor radioligand assay. Whereas the KD value was not significantly changed, the relative proportion of a1A-adrenoceptor subtype increased from 19±6 to 31±8 %. The affinities of two subtypes to 5-methylurapidil were not obviously changed after propranolol treatment. It was suggested that a1A-subtype was more important in a1-receptor mediated alterations after β-adrenoceptor blockade.

关 键 词：普萘洛尔 心肌 细胞膜 

分 类 号：R965.2[医药卫生—药理学]