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J Med Chem. 2003 Feb 27;46(5):670-3.

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.

Author information

1
Cardiovascular and Metabolic Diseases, PGRD, Pfizer Inc., Groton, Connecticut 06340, and Neurogen Corporation, Branford, Connecticut 06405, USA. richard_l_elliot@groton.pfizer.com

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.

PMID:
12593645
DOI:
10.1021/jm025584p
[Indexed for MEDLINE]

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