Chiba Y, Sakai H, Misawa M
Department of Pharmacology, School of Pharmacy, Hoshi University, Tokyo, Japan.
Res Commun Mol Pathol Pharmacol. 1998 Nov;102(2):205-8.
This study was undertaken to assess the important muscarinic receptor subtype in acetylcholine (ACh)-induced rat bronchial smooth muscle contraction. Ring smooth muscle strips of the left main bronchus were used. Isometrical contraction was measured in response to ACh in cumulative concentrations (10(-7)-10(-3) M) with and without preincubations with the muscarinic receptor antagonists, pirenzepine (an M1 antagonist), methoctramine (an M2 antagonist), and 4-diphenylacetoxy N-methylpiperidine (4-DAMP; an M1/M3 antagonist). Preincubation with these antagonists resulted in concentration-dependent rightward shifts of the concentration-response curves to ACh. pA2 values (means+/-sem) were 8.80+/-0.10 for 4-DAMP, 7.03+/-0.06 for pirenzepine and 5.91+/-0.36 for methoctramine, indicating that the most important muscarinic receptor mediating ACh-induced contraction of rat bronchial smooth muscle is of the M3 type.
本研究旨在评估乙酰胆碱(ACh)诱导大鼠支气管平滑肌收缩中重要的毒蕈碱受体亚型。使用左主支气管的环形平滑肌条。在有和没有与毒蕈碱受体拮抗剂哌仑西平(一种M1拮抗剂)、甲溴东莨菪碱(一种M2拮抗剂)和4-二苯基乙酰氧基-N-甲基哌啶(4-DAMP;一种M1/M3拮抗剂)预孵育的情况下,测量对累积浓度(10^(-7)-10^(-3) M)的ACh的等长收缩。用这些拮抗剂预孵育导致对ACh的浓度-反应曲线呈浓度依赖性右移。4-DAMP的pA2值(均值±标准误)为8.80±0.10,哌仑西平为7.03±0.06,甲溴东莨菪碱为5.91±0.36,表明介导ACh诱导大鼠支气管平滑肌收缩的最重要毒蕈碱受体是M3型。