Literature DB >> 24900499

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

Shuwen He1, Zhixiong Ye1, Quang Truong1, Shrenik Shah1, Wu Du1, Liangqin Guo1, Peter H Dobbelaar1, Zhong Lai1, Jian Liu1, Tianying Jian1, Hongbo Qi1, Raman K Bakshi1, Qingmei Hong1, James Dellureficio1, Alexander Pasternak1, Zhe Feng1, Reynalda deJesus1, Lihu Yang1, Mikhail Reibarkh1, Scott A Bradley1, Mark A Holmes1, Richard G Ball1, Rebecca T Ruck1, Mark A Huffman1, Frederick Wong1, Koppara Samuel1, Vijay B Reddy1, Stan Mitelman1, Sharon X Tong1, Gary G Chicchi1, Kwei-Lan Tsao1, Dorina Trusca1, Margaret Wu1, Qing Shao1, Maria E Trujillo1, George J Eiermann1, Cai Li1, Bei B Zhang1, Andrew D Howard1, Yun-Ping Zhou1, Ravi P Nargund1, William K Hagmann1.   

Abstract

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.

Entities:  

Keywords:  SSTR3; antagonist; type 2 diabetes; β-tetrahydrocarboline

Year:  2012        PMID： 24900499      PMCID： PMC4025728          DOI： 10.1021/ml300063m

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  19 in total

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