文章基本信息

标题：The Affinity of Bopindolol and Its Two Metabolites for a β2-Adrenoceptor in the Bovine Mesenteric Artery
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作者：Yoshiaki HOSOHATA ; Masahiko SUZUKI ; Yuko KARAKISAWA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1994
卷号：17
期号：9
页码：1296-1298
DOI：10.1248/bpb.17.1296
出版社：The Pharmaceutical Society of Japan
摘要：Bopindolol and its two metabolites (18-502 and 20-785) were examined for their affinity to a β₂-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 β₂-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 β₂-adrenoceptor tissue, and that bopindolol and its two metabolites were potent for β₂-adrenoceptors in the bovine mesenteric artery.
关键词：bopindolol;bopindolol metabolite;bovine mesenteric artery;β2-adrenoceptor;[3H] CGP12177;radioligand binding assay