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大鼠结肠上皮细胞毒蕈碱受体的体内鉴定。[3H] - 喹核醇基苯甲酸酯的结合

In vivo identification of muscarinic receptors on rat colonic epithelial cells. Binding of [3H]-quinuclidinyl benzilate.

作者信息

Rimele T J, Gaginella T S

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1982 Apr;319(1):18-21. doi: 10.1007/BF00491472.

Abstract

(1) We have demonstrated that intravenously administered [3H]-quinuclidinyl benzilate binds to rat colonic and ileal epithelial cells. The binding was prevented by pretreatment with atropine and QNB. (2) Binding was stereoselective in favor of dexetimide, the biologically more active optical isomer of benzetimide. (3) The results with intestinal epithelial cells were qualitatively the same as those obtained using heart and gut muscle as controls. (4) QNB inhibited pilocarpine-induced fluid accumulation in ligated gut segments. (5) The results support the concept that cholinergic receptors, which mediate intestinal secretion, exist on rat intestinal epithelial cell membranes.

摘要

(1) 我们已经证明,静脉注射的[3H]-奎宁环基苯甲酸酯能与大鼠结肠和回肠上皮细胞结合。这种结合可被阿托品和QNB预处理所阻断。(2) 结合具有立体选择性,有利于右苯甲酰甲酯,它是苯酰甲酯生物学活性更强的光学异构体。(3) 肠道上皮细胞的结果在性质上与以心脏和肠道肌肉作为对照所获得的结果相同。(4) QNB抑制毛果芸香碱诱导的结扎肠段液体蓄积。(5) 这些结果支持这样一种概念,即介导肠道分泌的胆碱能受体存在于大鼠肠道上皮细胞膜上。

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