Characterization of muscarinic acetylcholine receptors on the rat pancreatic gastrin‐producing cell line B6 RIN

FEBS Letters

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.

【 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 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.

【 授权许可】

Unknown