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. 2008 Jun 15;18(12):3611-5.
doi: 10.1016/j.bmcl.2008.04.070. Epub 2008 May 1.

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 alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity

Brad A Acker  1 , E Jon Jacobsen, Bruce N Rogers, Donn G Wishka, Steven C Reitz, David W Piotrowski, Jason K Myers, Mark L Wolfe, Vincent E Groppi, Bruce A Thornburgh, Paula M Tinholt, Rodney R Walters, Barbara A Olson, Laura Fitzgerald, Brian A Staton, Thomas J Raub, Michael Krause, Kai S Li, William E Hoffmann, Mihaly Hajos, Raymond S Hurst, Daniel P Walker
Affiliations

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 alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity

Brad A Acker et al. Bioorg Med Chem Lett. .

Abstract

A novel alpha7 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 alpha7 in vitro activity, excellent brain penetration, good rat oral bioavailability and robust in vivo efficacy in a rat auditory sensory gating model.

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