Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the α7 nicotinic acetylcholine receptor:: In vitro and in vivo activity

被引：60

作者：

Acker, Brad A. ^{[1
]}

Jacobsen, E. Jon ^{[1
]}

Rogers, Bruce N. ^{[1
]}

Wishka, Donn G. ^{[1
]}

Reitz, Steven C. ^{[1
]}

Piotrowski, David W. ^{[1
]}

Myers, Jason K. ^{[1
]}

Wolfe, Mark L. ^{[1
]}

Groppi, Vincent E. ^{[1
]}

Thornburgh, Bruce A. ^{[1
]}

Tinholt, Paula M. ^{[1
]}

Walters, Rodney R. ^{[1
]}

Olson, Barbara A. ^{[1
]}

Fitzgerald, Laura ^{[1
]}

Staton, Brian A. ^{[1
]}

Raub, Thomas J. ^{[1
]}

Krause, Michael ^{[1
]}

Li, Kai S. ^{[1
]}

Hoffmann, William E. ^{[1
]}

Hajos, Mihaly ^{[1
]}

Hurst, Raymond S. ^{[1
]}

Walker, Daniel P. ^{[1
]}

机构：

[1] Pfizer Inc, Global Res & Dev, Neurosci Res, Groton, CT 06340 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 12期

关键词：

azabicyclic; alpha; 7; nicotinic; nAChR; schizophrenia; PHA-543613; PHA-709829;

D O I：

10.1016/j.bmcl.2008.04.070

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel alpha 7 nAChR agonist, N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide ( 3a, PHA-709829), has been identified for the potential treatment of cognitive deficits in schizophrenia. The compound shows potent and selective a7 in vitro activity, excellent brain penetration, good rat oral bioavailability and robust in vivo efficacy in a rat auditory sensory gating model. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：3611 / 3615

页数：5

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