期刊论文详细信息
FEBS Letters
Characterization of muscarinic acetylcholine receptors on the rat pancreatic gastrin‐producing cell line B6 RIN
Chayvialle, Jean-Alain2  Cuber, Jean-Claude2  Abello, Jacques2  Bernard, Christine2  Philippe, Jacques1  Roche, Colette2 
[1] Centre Médical Universitaire, Laboratoire de Microbiologie, Geneva, Switzerland;NSERM U45, Pavillon Hbis, Hôpital E. Herriot, F-69437 Lyon Cedex 3, France
关键词: Muscarinic acetylcholine receptor;    Cytosolic free calcium;    Carbachol;    Gastrin release;    B6 RIN cell;    [3H]NMS;    [N-methyl-3H]scopolamine methyl chloride;    AF-DX 116;    11-([12-{(diethylamino)methyl}-1-piperidinyl]acetyl)-5;    11-dihydro-6H-pyridol [2;    3-b][1;    4]benzodizepine-6-one;   
DOI  :  10.1016/0014-5793(90)81229-H
学科分类:生物化学/生物物理
来源: John Wiley & Sons Ltd.
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【 摘 要 】

The mechanisms of cholinergic stimulation of gastrin cells were studied in the rat pancreatic cell line B6 RIN. Carbachol induced an increase in intracellular Ca2+ and stimulated gastrin release in a dose-dependent manner over the range 10−5-10−3 M. These effects were completely abolished by atropine, suggesting the implication of muscarinic cholinergic receptors. The binding properties of these receptors were investigated. [N-Methyl-3H]scopolamine ([3h]nms) binding on cell homogenates was time-dependent, saturable and consistent with a single high-affinity binding class (K d = 39.5 pM, and B max = 7.9 math formula DNA). Carbachol competitively inhibited [3H]NMS binding. The potency of inhibition of [3H]NMS binding by subtype selective antagonists was hexahydrodifenidol > pirenzepine > AF-DX 116. These results suggest the M3, muscarinic receptors may be involved in the carbachol-induced gastrin release from B6 RIN cells.

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