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
- 1 February 2003
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 46 (5), 670-673
- https://doi.org/10.1021/jm025584p
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.Keywords
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