Morisset J, Geoffrion L, Larose L, Lanöe J, Poirier G G
Pharmacology. 1981;22(3):189-95. doi: 10.1159/000137489.
We have studied the binding of the potent muscarinic antagonist, (3H)-quinuclidinyl benzilate [(3H)-QNB], in order to characterize muscarinic receptors of the digestive tract organs and evaluate their population. In each tissue examined, the binding sites were saturable and stereoselective; (3H)-QNB could also be displaced by known muscarinic agonists and antagonists. Along the digestive tract, the stomach (for stomach, fundus, antrum) and the colon possess the highest number of binding sites while the secretory (parotid, mandibular and pancreas), with a comparable amount of sites, are among those with less receptors. This study presents for the first time a complete distribution of the muscarinic receptors in organs of the digestive system evaluated under identical experimental conditions.
我们研究了强效毒蕈碱拮抗剂(3H)-喹核醇基苯甲酸酯[(3H)-QNB]的结合情况,以表征消化道器官的毒蕈碱受体并评估其数量。在每个检测的组织中,结合位点是可饱和的且具有立体选择性;(3H)-QNB也可被已知的毒蕈碱激动剂和拮抗剂取代。在整个消化道中,胃(包括胃底、胃窦)和结肠的结合位点数量最多,而分泌腺(腮腺、下颌下腺和胰腺)的位点数量相当,但受体数量较少。本研究首次在相同实验条件下评估了毒蕈碱受体在消化系统器官中的完整分布。