Kilbinger H, von Bardeleben R S, Siefken H, Wolf D
Department of Pharmacology, University of Mainz, Germany.
Life Sci. 1995;56(11-12):981-7. doi: 10.1016/0024-3205(95)00037-7.
Prejunctional pA2 values of five muscarinic antagonists were determined in the guinea-pig trachea under stimulation conditions in which the antagonists alone did not enhance acetylcholine release. The antagonists were partly selective at M1 (pirenzepine), M2 (AQ-RA 741, himbacine) and M3 receptors (hexahydrosiladifenidol, dicyclomine). The profile of the antagonist affinities was different from that obtained at cardiac M2 receptors but resembled the profile reported in the literature for the cloned m4 receptor. This suggests that autoinhibition of acetylcholine release in the trachea is mediated via M4 receptors.
在豚鼠气管中，于刺激条件下测定了五种毒蕈碱拮抗剂的接头前pA2值，在该刺激条件下单独使用拮抗剂不会增强乙酰胆碱释放。这些拮抗剂对M1（哌仑西平）、M2（AQ-RA 741、樟柳碱）和M3受体（六甲硅烷二苯哌啶、双环胺）具有部分选择性。拮抗剂亲和力的概况与在心脏M2受体上获得的不同，但与文献中报道的克隆m4受体的概况相似。这表明气管中乙酰胆碱释放的自身抑制是通过M4受体介导的。
