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
Pfizer Global Research & Development, Eastern Point Road, Groton, Connecticut 06340, USA.
J Med Chem. 2006 Jul 13;49(14):4425-36. doi: 10.1021/jm0602413.
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.
N-[(3R)-1-氮杂双环[2.2.2]辛-3-基]呋喃并[2,3-c]吡啶-5-甲酰胺（14，PHA-543,613）是α7神经元烟碱型乙酰胆碱受体（α7 nAChR）的新型激动剂，已被确定为治疗精神分裂症认知缺陷的潜在药物。化合物14是一种强效且选择性的α7 nAChR激动剂，具有出色的体外特性。该化合物的特点是在大鼠体内脑内快速渗透且口服生物利用度高，并在听觉感觉门控以及评估认知表现的体内模型——新物体识别中显示出体内疗效。
