ALPHA-1 AND BETA-ADRENERGIC-RECEPTOR BLOCKING POTENCIES OF BOPINDOLOL AND ITS 2 METABOLITES (18-502 AND 20-785) AS ASSESSED BY RADIOLIGAND BINDING ASSAY-METHODS

被引：9

作者：

HOSOHATA, Y ^{[1
]}

SASAKI, K ^{[1
]}

SUZUKI, M ^{[1
]}

KARAKISAWA, Y ^{[1
]}

MARUYAMA, K ^{[1
]}

TSUCHIHASHI, H ^{[1
]}

NAGATOMO, T ^{[1
]}

机构：

[1] NIIGATA COLL PHARM,DEPT PHARMACOL,NIIGATA 95021,JAPAN

来源：

GENERAL PHARMACOLOGY | 1995年 / 26卷 / 04期

关键词：

BOPINDOLOL; METABOLITES OF BOPINDOLOL; ALPHA(1) AND BETA-ADRENOCEPTORS; RADIOLIGAND BINDING ASSAY; PARTIAL AGONIST ACTIVITY;

D O I：

10.1016/0306-3623(94)00255-L

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1. The pK(i) value of bopindolol for alpha(1High)-subtypes in canine aorta, rat hearts and rat brain was 5.71, 5.52 and 6.56, respectively, In addition, the pK(i) values of these drugs in canine aorta, rat hearts and rat brain for the alpha(1Low)-subtype was very low. 2. The phenylephrine induced-contractions of aortae of guinea pigs and rats were not inhibited by these agents. 3. Both bovine hearts and tracheal smooth muscles indicated that 18-502 had the highest pK(i) value to beta(1)- and beta(2)-adrenoceptor subtypes and the rank order of these beta-blocking potencies were 18-502 > bopindolol > 20-785.

引用

页码：743 / 747

页数：5