Document Report Card

ID: ALA1145972

Journal: J Med Chem

Title: In vitro and in vivo characterization of 3-[2-[6-(2-tert-butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl]benzonitrile hydrochloride salt, a potent and selective NPY5 receptor antagonist.

Authors: Elliott RL, Oliver RM, Hammond M, Patterson TA, She L, Hargrove DM, Martin KA, Maurer TS, Kalvass JC, Morgan BP, DaSilva-Jardine PA, Stevenson RW, Mack CM, Cassella JV.

Abstract: To investigate the anorectic potential of NPY5 receptor antagonists, we have profiled the in vitro and in vivo properties of 3-[2-[6-(2-tert-butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl]benzonitrile hydrochloride salt (1). This compound was found to have excellent NPY5 receptor affinity and selectivity, potent functional antagonism, and good peripheral and central nervous system exposure in rats. This compound attenuated bovine pancreatic polypeptide induced food intake in rats but failed to demonstrate anorectic activity in rodent natural feeding models.

CiteXplore: 12593645

DOI: 10.1021/jm025584p