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甲基黄酮醇胺盐酸盐对β受体的阻断作用
引用本文:尹亚林,周尔风.甲基黄酮醇胺盐酸盐对β受体的阻断作用[J].药学学报,1987,22(6):465-467.
作者姓名:尹亚林  周尔风
作者单位:*青岛医学院药理教研室;山西医学院药理教研室,太原
摘    要:The β-receptor blocking action of methylflavonolamine hydrochloride(MFA) was studied and compared with those of propranolol. The doseresponse curves of isoproterenol were shifted to the right by MFA on isolated rabbit atrium in this experiment. The pA2 value and the slope of the regression line of MFA calculated from Schild plot were 5.53 and -0.84 respectively. The effects of MFA and propranolol on duck erythrocyte membranes were studied by the radioligand binding method. Both MFA and propranolol inhibited the binding of 3H] dihydroalprenolol to β-receptors. Their apparent equilibrium dissociation constants were 1.12×10-5 mol/L and 5.50×10-9 mol/L respectively. The affinity of propranolol to β-receptors of duck erythrocyte membranes was 2039-fold higher than that of MFA. These results demonstrates that MFA is a weak competitive β-receptor blocking agent.

关 键 词:甲基黄酮醇胺盐酸盐  心得安  β肾上腺素受体  鸭红细胞膜  放射配基结合测定法
收稿时间:1986-05-10

Beta-adrenergic receptor blocking action of methylflavonolamine hydrochloride
YIN Ya-Lin and ZHOU Er-Feng.Beta-adrenergic receptor blocking action of methylflavonolamine hydrochloride[J].Acta Pharmaceutica Sinica,1987,22(6):465-467.
Authors:YIN Ya-Lin and ZHOU Er-Feng
Abstract:The β-receptor blocking action of methylflavonolamine hydrochloride(MFA) was studied and compared with those of propranolol. The doseresponse curves of isoproterenol were shifted to the right by MFA on isolated rabbit atrium in this experiment. The pA2 value and the slope of the regression line of MFA calculated from Schild plot were 5.53 and -0.84 respectively. The effects of MFA and propranolol on duck erythrocyte membranes were studied by the radioligand binding method. Both MFA and propranolol inhibited the binding of 3H] dihydroalprenolol to β-receptors. Their apparent equilibrium dissociation constants were 1.12×10-5 mol/L and 5.50×10-9 mol/L respectively. The affinity of propranolol to β-receptors of duck erythrocyte membranes was 2039-fold higher than that of MFA. These results demonstrates that MFA is a weak competitive β-receptor blocking agent.
Keywords:Propranolol  β-Adrenoceptor  Duck erythrocyte membrane  Radioligand method  Methylflavonolamine hydrochloride
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