Karahan F, Alican I, Ozkutlu U, Onat F, Yegen B C, Ulusoy N B, Oktay S
Department of Pharmacology, Marmara University School of Medicine, Turkey.
Arch Int Pharmacodyn Ther. 1991 Jul-Aug;312:140-5.
The antagonism of carbachol-induced contractions of guinea-pig common bile duct smooth muscle strips by various antagonists has been investigated in order to find out the muscarinic receptor subtype(s) of common bile duct smooth muscle. Atropine, pirenzepine, 4-DAMP and AF-DX 116 were used as nonselective, M1-selective, M1- and M3-selective and M2-selective muscarinic antagonists, respectively. All muscarinic antagonists examined displaced the concentration-response curves to the right, parallelly and in a concentration-dependent manner, without affecting maximum response. Schild analysis of data was consistent with competitive antagonism. pA2 values of the antagonists were as follows: atropine, 9.59; pirenzepine, 7.32; 4-DAMP, 8.99; AF-DX 116, 6.85. When these pA2 values are compared with those obtained in the ileum, it may be concluded that the muscarinic receptors of the guinea-pig common bile duct mediating cholinomimetic-induced contractions, are of the M3 subtype, but not of the M1 and M2 subtypes.
为了确定豚鼠胆总管平滑肌条中介导拟胆碱药诱导收缩的毒蕈碱受体亚型,研究了各种拮抗剂对卡巴胆碱诱导的豚鼠胆总管平滑肌条收缩的拮抗作用。阿托品、哌仑西平、4-二甲基氨基吡啶(4-DAMP)和AF-DX 116分别用作非选择性、M1选择性、M1和M3选择性以及M2选择性毒蕈碱拮抗剂。所有检测的毒蕈碱拮抗剂均使浓度-反应曲线平行右移,且呈浓度依赖性,不影响最大反应。对数据进行的Schild分析符合竞争性拮抗作用。拮抗剂的pA2值如下:阿托品,9.59;哌仑西平,7.32;4-DAMP,8.99;AF-DX 116,6.85。将这些pA2值与在回肠中获得的值进行比较时,可以得出结论,介导拟胆碱药诱导收缩的豚鼠胆总管毒蕈碱受体属于M3亚型,而非M1和M2亚型。