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

被引：22

作者：

Elliott, RL ^{[1
]}

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

机构：

[1] Pfizer Inc, PGRD, Cardiovasc & Metab Dis, Groton, CT 06340 USA

[2] Neurogen Corp, Branford, CT 06405 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 05期

关键词：

D O I：

10.1021/jm025584p

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：670 / 673

页数：4

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