Effects of Chronic Administration of Bopindolol on the Binding Characteristics of Cardiac α_<1H>-, α_<1L>-, β_1- and β_2-Adrenoceptor Subtypes in Cardiac Muscles of Spontaneously Hypertensive Rats (SHR)

概要

論文の詳細を見る
The effects of the chronic administration of bopindolol on the binding characteristics of [^3H]CGP12177 and [^3H]prazosin to cardiac α_<1H>-, α_<1L>-, β_1- and β_2-adrenoceptor subtypes of spontaneously hypertensive rats (SHR) and Wistar Kyoto rats (WKY) were compared with those of two other β-blockers, atenolol and propranolol. Bopindolol (1 and 3 mg/kg/d), atenolol (50 mg/kg/d) and propranolol (60 mg/kg/d) were given to 10-week-old SHR for 12 weeks. The changes in K_d and B_<max> values of the myocardium of SHR treated without and with those drugs were assessed by Scatchard analysis, and the ratio and B_<max> values of the β_1- and β_2-adrenoceptor subtypes were also calculated from displacemental curves using ICI 118,551. The systolic blood pressure in SHR was dose-dependently lowered by the administration of dopindolol, and was also lowered by the administration of atenolol and propranolol. The B_<max> values of β_1- and β_2-adrenoceptors were lowered by the administration of bopindolol (1 and 3 mg/kg/d) without any changes in the K_d values or the ratio of β_1- and β_2-adrenoceptors. Propranolol lowered 3-fold the affinity to the β-adrenoceptor. On the other hand, the K_d and B_<max> values of α_<1H>- and α_<1L>-adrenoceptor subtypes (high and low affinity binding sites for [^3H]prazosin) were not changed by these drugs. These findings suggest that bopidolol had a beneficial effect on β-adrenoceptors in the membranes of cardiac muscles of SHR, simplying that these effects may contribute to lowering hypertension.
公益社団法人日本薬学会の論文
1996-07-15

Effects of Chronic Administration of Bopindolol on the Binding Characteristics of Cardiac α_<1H>-, α_<1L>-, β_1- and β_2-Adrenoceptor Subtypes in Cardiac Muscles of Spontaneously Hypertensive Rats (SHR)

スポンサーリンク

概要

著者

関連論文

スポンサーリンク