| Literature DB >> 22424974 |
Kimberly O Cameron1, Elena E Beretta, Yue Chen, Margaret Chu-Moyer, Dilinie Fernando, Hua Gao, Jeffrey Kohrt, Sophie Lavergne, Paul Da Silva Jardine, Angel Guzman-Perez, Christopher Hoth, David A Perry, John R Hadcock, Denise Gautreau, Michael Makowski, Sylvie Perez, Jana Polivkova, Lucy Rogers, Dennis O Scott, Andrew G Swick, Lucinda Thiede, Catherine E Trebino, Richard V Trilles, Julie Wilmowski, Yingxin Zhang.
Abstract
New cholecystokinin-1 receptor (CCK1R) agonist 'triggers' were identified using iterative library synthesis. Structural activity relationship studies led to the discovery of compound 10e, a potent CCK1R agonist that demonstrated robust weight loss in a diet-induced obese rat model with very low systemic exposure. Pharmacokinetic data suggest that efficacy is primarily driven through activation of CCK1R's located within the intestinal wall.Entities:
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Year: 2012 PMID： 22424974 DOI： 10.1016/j.bmcl.2012.02.049
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823