The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes
ACS Medicinal Chemistry Letters2012Vol. 3(6), pp. 484–489
Citations Over TimeTop 16% of 2012 papers
Shuwen He, Zhixiong Ye, Quang Truong, Shrenik Shah, Wu Du, Liangqin Guo, Peter H. Dobbelaar, Zhong Lai, Jian Liu, Tianying Jian, Hongbo Qi, Raman K. Bakshi, Qingmei Hong, James Dellureficio, Alexander Pasternak, Zhe Feng, Reynalda deJesus, Lihu Yang, Mikhail Reibarkh, Scott A. Bradley, Mark A. Holmes, Richard G. Ball, Rebecca T. Ruck, Mark A. Huffman, Frederick Wong, Koppara Samuel, Vijay Reddy, Stan Mitelman, Sharon Tong, Gary G. Chicchi, Kwei‐Lan Tsao, Dorina Trusca, Margaret Wu, Qing Shao, Maria E. Trujillo, George J. Eiermann, Cai Li, Bei B. Zhang, Andrew D. Howard, Yunping Zhou, Ravi P. Nargund, William K. Hagmann
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.
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