哌仑西平能否区分毒蕈碱受体的“亚型”？
Does pirenzepine distinguish between 'subtypes' of muscarinic receptors?
作者信息
Szelenyi I
出版信息
Br J Pharmacol. 1982 Dec;77(4):567-9. doi: 10.1111/j.1476-5381.1982.tb09332.x.
Abstract
Pharmacological studies with pirenzepine were carried out on the isolated ileum and atrium of the guinea-pig and on the acid secretion from the isolated stomach of the mouse. Pirenzepine inhibited the bethanechol-evoked changes in all three organs in a dose-dependent manner. The slopes of the Schild-plots confirmed the competitive nature of the antagonism by pirenzepine. The estimated pA2-values were very similar. Based on these data, it might be concluded that pirenzepine is an anticholinoceptor compound without specific affinity for gastric muscarinic receptors.
摘要
用哌仑西平对豚鼠离体回肠和心房以及小鼠离体胃的胃酸分泌进行了药理学研究。哌仑西平以剂量依赖性方式抑制了这三种器官中由氨甲酰甲胆碱诱发的变化。Schild图的斜率证实了哌仑西平拮抗作用的竞争性本质。估计的pA2值非常相似。基于这些数据，可能得出结论，哌仑西平是一种对胃毒蕈碱受体无特异性亲和力的抗胆碱能受体化合物。
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