Nagata K, Abe K, Wang C H, Saito H, Matsuki N
Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
Jpn J Pharmacol. 1990 Jan;52(1):115-21. doi: 10.1254/jjp.52.115.
Characteristics of beta-adrenoceptor in the tracheal smooth muscle of Suncus murinus (suncus) were studied in comparison with those of rats and guinea pigs. Isoproterenol induced concentration-dependent relaxation of suncus trachea. However, the maximal relaxation was very small, and about 1000 times higher concentration was necessary compared to the case of the guinea pig. The order of the sensitivity to isoproterenol and the maximal relaxation was guinea pig much greater than rat greater than suncus. Tracheae from younger suncus were more sensitive to isoproterenol, but the maximal relaxation was not significantly different from the results using adult animals. Forskolin, a direct activator of adenylate cyclase, relaxed tracheae to similar extents in the three species. Though the affinity of specific [3H]dihydroalprenolol binding was not significantly different, the maximal number of binding sites was in the order of rat greater than guinea pig greater than suncus. However, the differences in density of the binding among the three species were not as great as differences in isoproterenol-induced relaxation. These results suggest that 1) beta-adrenoceptor-mediated relaxation of tracheal smooth muscle is not well-developed in the suncus and 2) the deficient relaxation is probably caused by insufficient coupling between adrenoceptors and adenylate cyclase.
将麝鼩气管平滑肌中的β-肾上腺素能受体特征与大鼠和豚鼠进行了比较研究。异丙肾上腺素可引起麝鼩气管浓度依赖性舒张。然而,最大舒张幅度非常小,与豚鼠相比,所需浓度大约高1000倍。对异丙肾上腺素的敏感性和最大舒张幅度顺序为:豚鼠>大鼠>麝鼩。幼年麝鼩的气管对异丙肾上腺素更敏感,但最大舒张幅度与成年动物的结果无显著差异。福斯高林是一种腺苷酸环化酶的直接激活剂,在这三种动物中使气管舒张的程度相似。虽然特异性[³H]二氢阿普洛尔结合的亲和力无显著差异,但结合位点的最大数量顺序为:大鼠>豚鼠>麝鼩。然而,这三种动物之间结合密度的差异不如异丙肾上腺素诱导舒张的差异大。这些结果表明:1)麝鼩气管平滑肌中β-肾上腺素能受体介导的舒张功能发育不完善;2)舒张功能不足可能是由于肾上腺素能受体与腺苷酸环化酶之间的偶联不足所致。