Ek B, Lundgren B
Eur J Pharmacol. 1982 Jan 8;77(1):25-31. doi: 10.1016/0014-2999(82)90530-1.
The inhibition of spontaneous contractile activity in isolated cat colon strips by isoprenaline, prenalterol and terbutaline was studied. Isoprenaline produced a concentration-dependent complete inhibition with an EC50 of 6.18 nM. Prenalterol and terbutaline produced a concentration-dependent partial inhibition of 68 and 75% respectively, with EC50 of 0.52 and 0.43 microM respectively. The inhibitory effects of the three agonists were blocked by metoprolol and IPS 339 in such a way as to suggest that the prenalterol effect was mediated by beta 1-adrenoceptors and the terbutaline effect was mediated by beta 2-adrenoceptors, whereas the effect of isoprenaline appeared to be mediated by both types of receptors. Thus, the results indicate that both beta 1- and beta 2-adrenoceptors are involved in the adrenergic inhibition of spontaneous contractile activity in the cat colon strip. Qualitative effects of prenalterol and terbutaline on the spontaneous contractile activity in the cat colon strip indicated that the beta 1-adrenoceptor-mediated effects may be related to inhibition of the activity in cholinergic neurons, whereas the beta 2-adrenoceptors may be acting on the smooth muscle cells per se.
研究了异丙肾上腺素、普瑞特罗和特布他林对离体猫结肠条自发收缩活性的抑制作用。异丙肾上腺素产生浓度依赖性的完全抑制,EC50为6.18 nM。普瑞特罗和特布他林分别产生浓度依赖性的部分抑制,抑制率分别为68%和75%,EC50分别为0.52和0.43 μM。美托洛尔和IPS 339可阻断这三种激动剂的抑制作用,表明普瑞特罗的作用由β1-肾上腺素能受体介导,特布他林的作用由β2-肾上腺素能受体介导,而异丙肾上腺素的作用似乎由两种受体介导。因此,结果表明β1-和β2-肾上腺素能受体均参与了猫结肠条中肾上腺素能对自发收缩活性的抑制作用。普瑞特罗和特布他林对猫结肠条自发收缩活性的定性作用表明,β1-肾上腺素能受体介导的作用可能与胆碱能神经元活性的抑制有关,而β2-肾上腺素能受体可能直接作用于平滑肌细胞本身。