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The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes

作者	HE SHUWEN; YE ZHIXIONG; QUANG TRUONG; SHAH SHRENIK; DU WU; GUO LIANGQIN; DOBBELAAR PETER H; LAI ZHONG; LIU JIAN; JIAN TIANYING; QI HONGBO; BAKSHI RAMAN K; HONG QINGMEI; DELLUREFICIO JAMES; PASTERNAK ALEXANDER; FENG ZHE; DEJESUS REYNALDA; YANG LIHU; REIBARKH MIKHAIL; BRADLEY SCOTT A; HOLMES MARK A; BALL RICHARD G; RUCK REBECCA T; HUFFINAN MARK A; WONG FREDERICK; SAMUEL KOPPARA; REDDY VIJAY B; MITELMAN STAN; TONG SHARON X; CHICCHI GARY G; TSAO KWEILAN; TRUSCA DONNA; WU MARGARET; SHAO QING; TRUJILLO MARIA E; EIERMANN GEORGE J; LI CAI; ZHANG BEI B; HOWARD ANDREW D; ZHOU YUNPING; NARGUND RAVI P; HAGMANN WILLIAM K

选自	期刊 ACS Medicinal Chemistry Letters; 卷期 2012年3-6; 页码 484-489

关联知识点

[摘要]：A structure-activity relationship study of the imidazolyl-beta-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.
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