左旋千金藤啶碱对β肾上腺素受体的拮抗作用  

Antagonism of l-stepholidine on β-adrenoceptors

作　　者：王蕾[1] 汪明华[2] 

机构地区：[1]青岛大学医学院药理教研室,山东青岛266021 [2]上海医科大学药学院药理教研室,上海200032

出　　处：《中草药》2001年第1期46-48,共3页Chinese Traditional and Herbal Drugs

摘　　要：目的　研究左旋千金藤啶碱 (l- SPD)对β肾上腺素受体的作用。方法　应用放射配体结合实验 ,通过竞争[3H]双氢烯丙洛尔 ([3H]DHA)特异性结合 ,研究 l- SPD对 β肾上腺素受体的亲和力 ;在离体猪冠状动脉环实验中 ,观察 l- SPD对 β肾上腺素受体的拮抗作用。结果　 l- SPD能竞争 [3H]DHA和兔肺细胞膜的结合部位 ,其 K i值为(5 .75± 0 .5 6 ) μmol/ L;l- SPD使去甲肾上腺素 (NA)对数累加量效曲线 (L CCRC)右移又压低 ,其 PA2 和 PD′2 值分别为 7.2 1± 0 .78,5 .32± 0 .13,而普萘洛尔 (Pro)使 NA的 L CCRC平行右移 ,PA2 值 9.19± 0 .17。结论　 l- SPD对β受体有拮抗作用。此外 。Object To study the effect of l stepholidine (l SPD) on β adrenoceptors Methods The affinity of l SPD to β adrenoceptors was investigated by radioligand binding assay by means of competitive [ 3H] labelled Dihydro Aprenolol ([ 3H] DHA) specific binding The antagonism of l SPD on β adrenoceptors was tested on pig coronary artery rings in vitro. Results [ 3H] DHA binding assay showed that l SPD specifically displayed binding affinity to β adrenoceptors The Ki value was (5 75±0 56) μmol/L; the logarithmic cumulative concentration response curves (LCCRC) of l[WT5,5”BZ] SPD for NA on the pig coronary artery rings showed that the position of curves shifted to the right and the crest depressed The values of pA 2 an pD′ 2 were 7 21±0 78 and 5 32±0 13 respectively As a control, propranolol (Pro) could shift the curves parallelly to the right and the pA 2 value of Pro was 9 19±0 17 Conclusion The results suggested that l SPD is a β adrenoceptor antagonist and has affinities to more than one kind of receptor

关 键 词：Β肾上腺素受体 左旋千金藤啶碱 冠状血管 放射配体结合实验 

分 类 号：R285.5[医药卫生—中药学]