Koike K, Ichino T, Horinouchi T, Takayanagi I
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.
J Smooth Muscle Res. 1997 Jun;33(3):99-106. doi: 10.1540/jsmr.33.99.
To understand the receptor subtypes responsible for beta-adrenoceptor-mediated relaxation of guinea pig taenia caecum, we investigated the effects of isoprenaline and salbutamol. Isoprenaline and salbutamol caused dose-dependent relaxation of the guinea pig taenia caecum. Propranolol, bupranolol and butoxamine produced shifts of the concentration response curves for isoprenaline and salbutamol. Schild regression analyses carried out for propranolol against isoprenaline and salbutamol gave pA2 values of 8.43 and 8.88, respectively. Schild regression analyses carried out for butoxamine against isoprenaline and salbutamol gave pA2 values of 6.46 and 6.68, respectively. Schild regression analyses carried out for bupranolol against isoprenaline and salbutamol gave pA2 values of 8.60 and 8.69, respectively. However, in the presence of 3 x 10(-4) M atenolol, 10(-4) M butoxamine and 10(-6) M phentolamine to block the beta1-, beta2- and alpha-adrenoceptor effects, respectively, Schild regression analyses carried out for bupranolol against isoprenaline and salbutamol gave pA2 values of 5.77 and 5.97, respectively. These results suggest that the relaxant responses to isoprenaline and salbutamol in the guinea pig taenia caecum are mediated by both the beta2- and the beta3-adrenoceptors.
为了解负责β-肾上腺素能受体介导的豚鼠盲肠绦虫舒张的受体亚型,我们研究了异丙肾上腺素和沙丁胺醇的作用。异丙肾上腺素和沙丁胺醇引起豚鼠盲肠绦虫剂量依赖性舒张。普萘洛尔、布普洛尔和丁氧胺使异丙肾上腺素和沙丁胺醇的浓度-反应曲线发生位移。对普萘洛尔针对异丙肾上腺素和沙丁胺醇进行的希尔德回归分析分别给出pA2值为8.43和8.88。对丁氧胺针对异丙肾上腺素和沙丁胺醇进行的希尔德回归分析分别给出pA2值为6.46和6.68。对布普洛尔针对异丙肾上腺素和沙丁胺醇进行的希尔德回归分析分别给出pA2值为8.60和8.69。然而,在分别存在3×10⁻⁴ M阿替洛尔、10⁻⁴ M丁氧胺和10⁻⁶ M酚妥拉明以阻断β1-、β2-和α-肾上腺素能受体效应的情况下,对布普洛尔针对异丙肾上腺素和沙丁胺醇进行的希尔德回归分析分别给出pA2值为5.77和5.97。这些结果表明,豚鼠盲肠绦虫对异丙肾上腺素和沙丁胺醇的舒张反应是由β2-和β3-肾上腺素能受体介导的。