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  • Title: Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists.
    Author: Cameron KO, Beretta EE, Chen Y, Chu-Moyer M, Fernando D, Gao H, Kohrt J, Lavergne S, Jardine Pda S, Guzman-Perez A, Hoth C, Perry DA, Hadcock JR, Gautreau D, Makowski M, Perez S, Polivkova J, Rogers L, Scott DO, Swick AG, Thiede L, Trebino CE, Trilles RV, Wilmowski J, Zhang Y.
    Journal: Bioorg Med Chem Lett; 2012 Apr 15; 22(8):2943-7. PubMed ID: 22424974.
    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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