Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes

[Image: see text] The imidazolyl-tetrahydro-β-carboline class of sstr3 antagonists have demonstrated efficacy in a murine model of glucose excursion and may have potential as a treatment for type 2 diabetes. The first candidate in this class caused unacceptable QTc interval prolongation in oral, tel...

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הוצא לאור ב:ACS Med Chem Lett
Main Authors: Shah, Shrenik K., He, Shuwen, Guo, Liangqin, Truong, Quang, Qi, Hongbo, Du, Wu, Lai, Zhong, Liu, Jian, Jian, Tianying, Hong, Qingmei, Dobbelaar, Peter, Ye, Zhixiong, Sherer, Edward, Feng, Zhe, Yu, Yang, Wong, Frederick, Samuel, Koppara, Madiera, Maria, Karanam, Bindhu V., Reddy, Vijay B., Mitelman, Stan, Tong, Sharon X., Chicchi, Gary G., Tsao, Kwei-Lan, Trusca, Dorina, Feng, Yue, Wu, Margaret, Shao, Qing, Trujillo, Maria E., Eiermann, George J., Li, Cai, Pachanski, Michele, Fernandez, Guillermo, Nelson, Donald, Bunting, Patricia, Morissette, Pierre, Volksdorf, Sylvia, Kerr, Janet, Zhang, Bei B., Howard, Andrew D., Zhou, Yun-Ping, Pasternak, Alexander, Nargund, Ravi P., Hagmann, William K.
פורמט: Artigo
שפה:Inglês
יצא לאור: American Chemical Society 2015
גישה מקוונת:https://ncbi.nlm.nih.gov/pmc/articles/PMC4434471/
https://ncbi.nlm.nih.gov/pubmed/26005524
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml500514w
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