非诺特罗在豚鼠盲肠带中诱导的β2和β3肾上腺素能受体介导的舒张作用。

The beta2- and beta3-adrenoceptor-mediated relaxation induced by fenoterol in guinea pig taenia caecum.

作者信息

Akimoto Yurie, Horinouchi Takahiro, Tanaka Yoshio, Koike Katsuo

机构信息

Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, 2-2-1, Miyama, Funabashi, Chiba 274-8510, Japan.

出版信息

J Smooth Muscle Res. 2002 Oct;38(4-5):145-51. doi: 10.1540/jsmr.38.145.

DOI:10.1540/jsmr.38.145

PMID:12596892

Abstract

Fenoterol, a beta2-adrenoceptor selective agonist, belongs to the arylethanolamine class. To understand the receptor subtypes responsible for beta-adrenoceptor-mediated relaxation of guinea pig taenia caecum, we investigated the effect of fenoterol. Fenoterol caused concentration-dependent relaxation of the guinea pig taenia caecum. Propranolol, bupranolol and butoxamine produced shifts of the concentration-response curve for fenoterol. Schild regression analyses carried out for propranolol, butoxamine and bupranolol against fenoterol gave pA2 values of 8.41, 6.33 and 8.44, 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 a-adrenoceptor effects, respectively, Schild regression analysis carried out for bupranolol against fenoterol gave pA2 values of 5.80. These results suggest that the relaxant response to fenoterol in the guinea pig taenia caecum is mediated by both the beta2- and the beta3-adrenoceptors.

摘要

非诺特罗是一种β2肾上腺素能受体选择性激动剂，属于芳基乙醇胺类。为了解负责β肾上腺素能受体介导的豚鼠盲肠带松弛的受体亚型，我们研究了非诺特罗的作用。非诺特罗引起豚鼠盲肠带浓度依赖性松弛。普萘洛尔、布普萘洛尔和丁氧胺使非诺特罗的浓度-反应曲线发生位移。对普萘洛尔、丁氧胺和布普萘洛尔与非诺特罗进行的希尔德回归分析得出的pA2值分别为8.41、6.33和8.44。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，对布普萘洛尔与非诺特罗进行的希尔德回归分析得出的pA2值为5.80。这些结果表明，豚鼠盲肠带对非诺特罗的松弛反应是由β2和β3肾上腺素能受体介导的。