Discovery of N-[(3 R)-1-Azabicyclo [2.2. 2] oct-3-yl] furo [2, 3-c] pyridine-5-carboxamide, an Agonist of the α7 Nicotinic Acetylcholine Receptor, for the Potential …

…, S Jia, JK Myers, KL Olson, EJ Jacobsen…

文献索引：Wishka, Donn G.; Walker, Daniel P.; Yates, Karen M.; Reitz, Steven C.; Jia, Shaojuan; Myers, Jason K.; Olson, Kirk L.; Jacobsen, E. Jon; Wolfe, Mark L.; Groppi, Vincent E.; Hanchar, Alexander J.; Thornburgh, Bruce A.; Cortes-Burgos, Luz A.; Wong, Erik H. F.; Staton, Brian A.; Raub, Thomas J.; Higdon, Nicole R.; Wall, Theron M.; Hurst, Raymond S.; Walters, Rodney R.; Hoffmann, William E.; Hajos, Mihaly; Franklin, Stanley; Carey, Galen; Gold, Lisa H.; Cook, Karen K.; Sands, Steven B.; Zhao, Sabrina X.; Soglia, John R.; Kalgutkar, Amit S.; Arneric, Stephen P.; Rogers, Bruce N. Journal of Medicinal Chemistry, 2006 ,  vol. 49,  # 14  p. 4425 - 4436

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被引用次数: 156

摘要

N-[(3 R)-1-Azabicyclo [2.2. 2] oct-3-yl] furo [2, 3-c] pyridine-5-carboxamide (14, PHA- 543,613), a novel agonist of the α7 neuronal nicotinic acetylcholine receptor (α7 nAChR), has been identified as a potential treatment of cognitive deficits in schizophrenia. Compound 14 is a potent and selective α7 nAChR agonist with an excellent in vitro profile. The compound is characterized by rapid brain penetration and high oral bioavailability in rat ...