GIP receptor antagonist (IC50
M). Inhibits GIP-stimulated insulin release from pancreatic β
cells in vitro
. In ob/ob
mice, blocks the effects of GIP on insulin release and plasma glucose levels. Also improves intraperitoneal glucose tolerance, insulin sensitivity, and glucose response to feeding in ob/ob
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Early administration of the glucose-dependent insulinotropic polypeptide receptor antagonist (Pro3)GIP prevents the development of diabetes and related metabolic abnormalities associated with genetically inherited obesity in ob/ob mice.
Irwin et al.
Characterization of the cellular and metabolic effects of a novel enzyme-resistant antagonist of glucose-dependent insulinotropic polypeptide.
Gault et al.
Biochem Biophys Res Commun., 2002;290:1420