A novel effect of rebamipide: generation of [Ca2+](i) oscillations throughactivation of CCK1 receptors in rat pancreatic acinar cells

The protective effect of 2-(4-chlorobenzoylamino)-3-[2(1H)-quinolinon-4-yl] -propionic acid (rebamipide) on gastric mucosa is well established. Here we demonstrate that rebamipide acts on pancreatic acinar cells to generate os cillations of intracellular Ca2+ concentration ([Ca2+](i)) through the acti vation of cholecystokinin subtype 1 (CCK1) receptors. At concentrations hig her than 5 mu M, rebamipide induced [Ca2+](i) oscillations in individual fu ra-2-loaded pancreatic acinar cells. The frequency of oscillations increase d with increasing concentrations of rebamipide, while the latency between s timulation of cells and initiation of [Ca2+](i) oscillations decreased with increasing concentration. The [Ca2+](i) oscillations evoked by rebamipide were inhibited by the CCK1 receptor antagonist L-364,718 but not by atropin e or the CCK2 receptor antagonist L-365,260 indicating that rebamipide is a nonpeptide CCK1 receptor agonist. (C) 2000 Elsevier Science B.V. All right s reserved.