Antagonism of l-stepholidine on ?-adrenoceptors
- VernacularTitle:左旋千金藤啶碱对?肾上腺素受体的拮抗作用
- Author:
Lei WANG
;
Minghua WANG
;
- Publication Type:Journal Article
- Keywords:
?-adrenergic receptor;
l stepholidine;
binding site;
coronary vessels
- From:
Chinese Traditional and Herbal Drugs
1994;0(01):-
- CountryChina
- Language:Chinese
-
Abstract:
Object To study the effect of l stepholidine (l SPD) on ? adrenoceptors Methods The affinity of l SPD to ? 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 ? adrenoceptors was tested on pig coronary artery rings in vitro. Results [ 3H] DHA binding assay showed that l SPD specifically displayed binding affinity to ? adrenoceptors The Ki value was (5 75?0 56) ?mol/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 ? adrenoceptor antagonist and has affinities to more than one kind of receptor
