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Bioorg Med Chem Lett
; 22(8): 2943-7, 2012 Apr 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-22424974
RESUMEN
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.