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

ABSTRACT: A structure-activity relationship study of the imidazolyl-?-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.

SUBMITTER: He S 

PROVIDER: S-EPMC4025728 | biostudies-literature | 2012 Jun

REPOSITORIES: biostudies-literature

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

He Shuwen S   Ye Zhixiong Z   Truong Quang Q   Shah Shrenik S   Du Wu W   Guo Liangqin L   Dobbelaar Peter H PH   Lai Zhong Z   Liu Jian J   Jian Tianying T   Qi Hongbo H   Bakshi Raman K RK   Hong Qingmei Q   Dellureficio James J   Pasternak Alexander A   Feng Zhe Z   deJesus Reynalda R   Yang Lihu L   Reibarkh Mikhail M   Bradley Scott A SA   Holmes Mark A MA   Ball Richard G RG   Ruck Rebecca T RT   Huffman Mark A MA   Wong Frederick F   Samuel Koppara K   Reddy Vijay B VB   Mitelman Stan S   Tong Sharon X SX   Chicchi Gary G GG   Tsao Kwei-Lan KL   Trusca Dorina D   Wu Margaret M   Shao Qing Q   Trujillo Maria E ME   Eiermann George J GJ   Li Cai C   Zhang Bei B BB   Howard Andrew D AD   Zhou Yun-Ping YP   Nargund Ravi P RP   Hagmann William K WK  

ACS medicinal chemistry letters 20120507 6

A structure-activity relationship study of the imidazolyl-β-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. ...[more]

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