The Affinity of Bopindolol and Its Two Metabolites for a β_2-Adrenoceptor in the Bovine Mesenteric Artery

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概要

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• Bopindolol and its two metabolites (18-502 and 20-785) were examined for their affinity to a β_2-adrenoceptor in the bovine mesenteric artery using the radioligand binding assay method with [^3H]CGP12177 as a radioligand. The Scatchard analysis of the data demonstrated a uniphasic plot with K_d and B_<max> values of 0.86±0.16 nM, and 13.34±1.11 fmol/mg protein, respectively. The pK_i values of bopindolol and its two metabolites for β_2-adrenoceptors in the bovine mesenteric artery were 7.70±0.13,8.07±0.13,8.20±0.24,respectively, with 20-785 showing the highest values among these drugs. The present findings indicate that the bovine mesenteric artery membrane is predominantly β_2-adrenoceptor tissue, and that bopindolol and its two metabolites were potent for β_2-adrenoceptors in the bovine mesenteric artery.

• 公益社団法人日本薬学会の論文
• 1994-09-15

著者

• 長友 孝文

  Department of Pharmacology, Niigata College of Pharmacy

• 長友 孝文

  新潟薬科大学薬学部薬理学教室

• 丸山 恵子

  アリゾナ大学医学部薬理

• 鈴木 政彦

  Department Of Pharmacology Niigata College Of Pharmacy

• 長友 孝文

  新潟薬科大学・薬・薬理

• 細機 好章

  Department of Pharmacology, Niigata College of Pharmacy

• 唐木澤 裕子

  Department of Pharmacology, Niigata College of Pharmacy

• 丸山 恵子

  Department of Pharmacology, Niigata College of Pharmacy

• 細機 好章

  アリゾナ大学医学部薬理学教室

• 長友 孝文

  Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App

• 唐木澤 裕子

  Department Of Pharmacology Niigata College Of Pharmacy

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