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Beschreibung

A 1, 2, 4-triazole derived compound that acts as a potent ghrelin receptor (GHS-R1a) antagonist (IC50 = 32 nM in a binding assay, dissociation constant Kb = 19 nM). Shown to reduce hexarelin-induced food intake [hexarelin (80 µ,g/kg, cumulative food intake (g of food/100 g of body weight) at 6 h by acute administration (sc) of JMV 2959 (160 µ,g/kg)] in rats without affecting the basal food intake. Also suppresses ghrelin and fasting-induced food intake at the level of the central nervous system. Reported to suppress genes up-regulated by ghrelin. Does not affect intracellular Ca2+ mobilization.