Roffel A F, Meurs H, Elzinga C R, Zaagsma J
Department of Pharmacology and Therapeutics, University of Groningen, Netherlands.
Eur J Pharmacol. 1993 Nov 9;249(2):235-8. doi: 10.1016/0014-2999(93)90438-n.
We investigated whether muscarinic M2 receptors, known to inhibit adenylyl cyclase activity in airway smooth muscle, also inhibit isoprenaline-induced relaxation of guinea pig tracheal smooth muscle, as has recently been described for the dog (Fernandes et al., 1992, J. Pharmacol. Exp. Ther. 262, 119). Smooth muscle strips were contracted with various concentrations of methacholine or histamine (which served as a control) in the absence or presence of the M2-selective muscarinic receptor antagonist, gallamine (30 microM), and cumulative isoprenaline-relaxation curves were obtained. It was found that muscarinic M2 receptor blockade had no significant effect on isoprenaline pD2 and Emax values, neither with histamine nor with methacholine. The results show that, in guinea pig trachea, muscarinic M2 receptors do not significantly influence the functional antagonism of cholinergic smooth muscle contraction by isoprenaline.
我们研究了已知可抑制气道平滑肌中腺苷酸环化酶活性的毒蕈碱M2受体,是否也像最近在犬中所描述的那样(Fernandes等人,1992年,《药理学与实验治疗学杂志》262卷,第119页),抑制异丙肾上腺素诱导的豚鼠气管平滑肌舒张。在不存在或存在M2选择性毒蕈碱受体拮抗剂加拉明(30微摩尔)的情况下,用不同浓度的乙酰甲胆碱或组胺(作为对照)使平滑肌条收缩,并获得累积异丙肾上腺素舒张曲线。结果发现,毒蕈碱M2受体阻断对组胺和乙酰甲胆碱的异丙肾上腺素pD2和Emax值均无显著影响。结果表明,在豚鼠气管中,毒蕈碱M2受体对异丙肾上腺素介导的胆碱能平滑肌收缩功能拮抗作用无显著影响。