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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.

作者信息

Hosohata Y, Sasaki K, Suzuki M, Karakisawa Y, Maruyama K, Tsuchihashi H, Nagatomo T

机构信息

Department of Pharmacology, Niigata College of Pharmacy, Japan.

出版信息

Gen Pharmacol. 1995 Jul;26(4):743-7. doi: 10.1016/0306-3623(94)00255-l.

DOI:10.1016/0306-3623(94)00255-l
PMID:7635249
Abstract
  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.
摘要

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