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胃中的毒蕈碱受体

Muscarinic receptors in the stomach.

作者信息

Hammer R

出版信息

Scand J Gastroenterol Suppl. 1980;66:5-11.

PMID:6941378
Abstract

Using tritiated N-methyl-scopolamine (3H-NMS), muscarinic receptor binding was demonstrated in broken cell preparation of mucosa and smooth muscle of the fundus of the canine stomach. Binding curves of pirenzepine were established in competition experiments against 3H-NMS. Pirenzepine shows a considerably higher affinity to muscarinic receptors from fundic mucosa than those from smooth muscle, suggesting a difference of muscarinic receptors in these two regions of the stomach. Different properties of mucosal and smooth muscle receptors could be further substantiated by agonist binding studies. Whilst carbachol binding to muscarinic receptors from fundic smooth muscle was modulated by guanine nucleotides, no such effect was found in fundic mucosa. Direct binding studies with 3H-NMS demonstrated muscarinic receptors in peripheral ganglia (sympathetic trunk ganglia from the calf, stellate ganglia from the dog). These are characterized by high affinity pirenzepine binding so that besides its direct action on gastric secretory glands, pirenzepine may influence indirectly gastrointestinal functions via peripheral, presumably intramural, ganglia.

摘要

利用氚标记的N-甲基东莨菪碱(3H-NMS),在犬胃底部黏膜和平滑肌的破碎细胞制剂中证实了毒蕈碱受体结合。在与3H-NMS的竞争实验中建立了哌仑西平的结合曲线。哌仑西平对胃底部黏膜毒蕈碱受体的亲和力明显高于平滑肌毒蕈碱受体,提示胃这两个区域的毒蕈碱受体存在差异。激动剂结合研究可进一步证实黏膜和平滑肌受体的不同特性。虽然卡巴胆碱与胃底部平滑肌毒蕈碱受体的结合受鸟嘌呤核苷酸调节,但在胃底部黏膜未发现此类效应。用3H-NMS进行的直接结合研究在周围神经节(小牛的交感干神经节、犬的星状神经节)中证实了毒蕈碱受体。这些受体的特征是对哌仑西平有高亲和力结合,因此除了对胃分泌腺的直接作用外,哌仑西平可能通过周围神经节(可能是壁内神经节)间接影响胃肠功能。

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