Alpha-1 and beta-adrenergic receptor blocking potencies of bopindolol and its two metabolites (18-502 and 20-785) as assessed by radioligand binding assay methods.
1. The pKi 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 pKi 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 pKi value to beta 1- and beta 2-adrenoceptor subtypes and the rank order of these beta-blocking potencies were 18-502 > bopindolol > 20-785.
Hosohata
Y
Y
Department of Pharmacology, Niigata College of Pharmacy, Japan.
Sasaki
K
K
Suzuki
M
M
Karakisawa
Y
Y
Maruyama
K
K
Tsuchihashi
H
H
Nagatomo
T
T
D058668:Adrenergic alpha-1 Receptor Antagonists; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D000818:Animals; D002417:Cattle; D004285:Dogs; D006321:Heart / Q000187:drug effects; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009206:Myocardium / Q000378:metabolism; D010656:Phenylephrine / Q000494:pharmacology; D010869:Pindolol / Q000031:analogs & derivatives* / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D013154:Spleen / Q000187:drug effects / Q000378:metabolism; D014132:Trachea / Q000187:drug effects
D058668:Adrenergic alpha-1 Receptor Antagonists; D000319:Adrenergic beta-Antagonists; D010656:Phenylephrine; C038186:4-(2-hydroxy-3-tert-butylaminopropoxy)-2-methylindole; C061293:4-(3-tert-butylamino-2-hydroxypropoxy)-2-carboxyindole; D010869:Pindolol; C036007:bopindolol