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  • Title: Sigma receptor-mediated effects of a new antiulcer agent, KB-5492, on experimental gastric mucosal lesions and gastric alkaline secretion in rats.
    Author: Hara H, Tanaka K, Harada Y, Sukamoto T.
    Journal: J Pharmacol Exp Ther; 1994 May; 269(2):799-805. PubMed ID: 8182548.
    Abstract:
    Using in vitro receptor autoradiography, we found specific [3H] 1,3-di(2-tolyl)guanidine (DTG) binding to be highly localized in the mucosa of the stomach and duodenum in rats. 4-Methoxyphenyl 4-(3,4,5-trimethoxybenzyl)-1-piperazine acetate monofumarate monohydrate (KB-5492), a novel antiulcer agent and a specific sigma receptor ligand, at 1 and 10 microM inhibited this specific [3H] DTG binding in rat stomach. The effects of KB-5492 and sigma receptor ligands such as DTG and rimcazole on the gastric lesions and alkaline secretion in rats were examined. KB-5492 (25-100 mg/kg, p.o.), DTG (3-30 mg/kg, p.o.) and rimcazole (30-100 mg/kg, p.o.) inhibited ethanol-induced and water-immersion stress-induced gastric mucosal lesions in rats. KB-5492 (30 mg/kg, i.g.) and DTG (30 mg/kg, i.g.) increased the gastric alkaline secretion in rats. These protective and alkaline-stimulated effects of KB-5492 and DTG were attenuated by haloperidol, a sigma receptor antagonist. These findings suggest that KB-5492 and DTG exert ulceroprotective effects through interaction with sigma receptors in the gastric mucosa.
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