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
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- 作者：Brad A. Acker ; 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
- 关键词：Azabicyclic ;
; //www.sciencedirect.com/scidirimg/entities/204e.gif"" alt=""greek small letter alpha"" title=""greek small letter alpha"" border=""0"">7 ; Nicotinic ; nAChR ; Schizophrenia ; PHA-543613 ; PHA-709829
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 出版时间：15 June 2008
- 年：2008
- 卷：18
- 期：12
- 页码：3611-3615
- 全文大小：180 K
文摘
A novel ![]()
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 ![]()
7 in vitro activity, excellent brain penetration, good rat oral bioavailability and robust in vivo efficacy in a rat auditory sensory gating model.