Hosohata Y, Suzuki M, Karakisawa Y, Maruyama K, Nagatomo T
Department of Pharmacology, Niigata College of Pharmacy, Japan.
Biol Pharm Bull. 1994 Sep;17(9):1296-8. doi: 10.1248/bpb.17.1296.
Bopindolol and its two metabolites (18-502 and 20-785) were examined for their affinity to a beta 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 Kd and Bmax values of 0.86 +/- 0.16 nM, and 13.34 +/- 1.11 fmol/mg protein, respectively. The pKi values of bopindolol and its two metabolites for beta 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 beta 2-adrenoceptor tissue, and that bopindolol and its two metabolites were potent for beta 2-adrenoceptors in the bovine mesenteric artery.
使用以[3H]CGP12177作为放射性配体的放射性配体结合测定法，研究了波吲洛尔及其两种代谢物（18 - 502和20 - 785）对牛肠系膜动脉中β2 - 肾上腺素能受体的亲和力。对数据进行的Scatchard分析显示为单相图，Kd值和Bmax值分别为0.86±0.16 nM和13.34±1.11 fmol/mg蛋白质。波吲洛尔及其两种代谢物对牛肠系膜动脉中β2 - 肾上腺素能受体的pKi值分别为7.70±0.13、8.07±0.13、8.20±0.24，其中20 - 785在这些药物中显示出最高值。目前的研究结果表明，牛肠系膜动脉膜主要是β2 - 肾上腺素能受体组织，并且波吲洛尔及其两种代谢物对牛肠系膜动脉中的β2 - 肾上腺素能受体具有强效作用。
