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Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists. | LitMetric

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Article 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.

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http://dx.doi.org/10.1016/j.bmcl.2012.02.049DOI Listing

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