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

Authors
HOSOHATA Y SASAKI K SUZUKI M KARAKISAWA Y MARUYAMA K TSUCHIHASHI H NAGATOMO T
Citation
Y. Hosohata et al., ALPHA-1 AND BETA-ADRENERGIC-RECEPTOR BLOCKING POTENCIES OF BOPINDOLOLAND ITS 2 METABOLITES (18-502 AND 20-785) AS ASSESSED BY RADIOLIGAND BINDING ASSAY-METHODS, General pharmacology, 26(4), 1995, pp. 743-747
Citations number
17
Categorie Soggetti
Pharmacology & Pharmacy
Journal title
General pharmacology → ACNP
ISSN journal
03063623
Volume
26
Issue
4
Year of publication
1995
Pages
743 - 747
Database
ISI
SICI code
0306-3623(1995)26:4<743:AABBPO>2.0.ZU;2-2
Abstract
1. The pK(i) value of bopindolol for alpha(1High)-subtypes in canine a orta, 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 hear ts and rat brain for the alpha(1Low)-subtype was very low. 2. The phen ylephrine induced-contractions of aortae of guinea pigs and rats were not inhibited by these agents. 3. Both bovine hearts and tracheal smoo th 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.