2. Academic Validation
  3. Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship

Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship

  • J Med Chem. 2006 Jul 13;49(14):4425-36. doi: 10.1021/jm0602413.
Donn G Wishka 1,  Daniel P Walker,  Karen M Yates,  Steven C Reitz,  Shaojuan Jia,  Jason K Myers,  Kirk L Olson,  E Jon Jacobsen,  Mark L Wolfe,  Vincent E Groppi,  Alexander J Hanchar,  Bruce A Thornburgh,  Luz A Cortes-Burgos,  Erik H F Wong,  Brian A Staton,  Thomas J Raub,  Nicole R Higdon,  Theron M Wall,  Raymond S Hurst,  Rodney R Walters,  William E Hoffmann,  Mihaly Hajos,  Stanley Franklin,  Galen Carey,  Lisa H Gold,  Karen K Cook,  Steven B Sands,  Sabrina X Zhao,  John R Soglia,  Amit S Kalgutkar,  Stephen P Arneric,  Bruce N Rogers
Affiliations

Affiliation

  • 1 Pfizer Global Research & Development, Eastern Point Road, Groton, Connecticut 06340, USA.
PMID: 16821801 DOI: 10.1021/jm0602413
Abstract

N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (14, PHA-543,613), a novel agonist of the alpha7 neuronal nicotinic acetylcholine receptor (alpha7 nAChR), has been identified as a potential treatment of cognitive deficits in schizophrenia. Compound 14 is a potent and selective alpha7 nAChR Agonist with an excellent in vitro profile. The compound is characterized by rapid brain penetration and high oral bioavailability in rat and demonstrates in vivo efficacy in auditory sensory gating and, in an in vivo model to assess cognitive performance, novel object recognition.

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