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本文采取累积剂量—效应曲线法研究包甲素对离体大鼠肠肌M—胆碱受体动力学参数。包甲素的介离常数(K_a)为匹罗卡晶的1/39,表明包甲素对M受体的亲和力比匹罗卡品大39倍。包甲素的最大效应(E_(Amax))是匹罗卡品的1.6倍,说明包甲素有较高的内在活性。阿托品1.0nM浓度时对包甲素和匹罗卡品呈竞争性对抗关系,两者的拮抗参数(pAx)相近。两者合并用药最终效应取决于占优势浓度药物的内在活性,呈典型竞争协同现象。实验证明包甲素属最强M—胆碱受体激动剂之列。
In this paper, cumulative dose-response curve method to study the kinetic parameters of M-cholinergic receptors in the intestinal muscle of the isolated rat intestinal muscle. The dissociation constant (K_a) of aplasma is 1/39 of that of pilocarpine, indicating that the affinity of atrophycin for M receptor is 39 times greater than that of pilocarpine. The maximum effect of palmatine (E_ (Amax)) is 1.6 times that of pilocarpine, indicating that Palladin has a higher intrinsic activity. Atropine at a concentration of 1.0 nM showed a competitive antagonistic relationship between naringin and pilocarpine, with similar antagonistic parameters (pAx). The combined effect of the two drugs depends on the intrinsic activity of the predominant drug concentration, showing a typical competitive synergy. Experiments show that matrine is the strongest M-choline receptor agonists.