文摘
A structure鈥揳ctivity relationship study of the imidazolyl-尾-tetrahydrocarboline series identified MK-4256 as a potent, selective SSTR3 antagonist, which demonstrated superior efficacy in a mouse oGTT model. MK-4256 reduced glucose excursion in a dose-dependent fashion with maximal efficacy achieved at doses as low as 0.03 mg/kg po. As compared with glipizide, MK-4256 showed a minimal hypoglycemia risk in mice.
Keywords:
SSTR3; antagonist; type 2 diabetes; 尾-tetrahydrocarboline