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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.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2006 Jul 13 , DOI: 10.1021/jm0602413 Donn G. Wishka 1 , Daniel P. Walker 1 , Karen M. Yates 1 , Steven C. Reitz 1 , Shaojuan Jia 1 , Jason K. Myers 1 , Kirk L. Olson 1 , E. Jon Jacobsen 1 , Mark L. Wolfe 1 , Vincent E. Groppi 1 , Alexander J. Hanchar 1 , Bruce A. Thornburgh 1 , Luz A. Cortes-Burgos 1 , Erik H. F. Wong 1 , Brian A. Staton 1 , Thomas J. Raub 1 , Nicole R. Higdon 1 , Theron M. Wall 1 , Raymond S. Hurst 1 , Rodney R. Walters 1 , William E. Hoffmann 1 , Mihaly Hajos 1 , Stanley Franklin 1 , Galen Carey 1 , Lisa H. Gold 1 , Karen K. Cook 1 , Steven B. Sands 1 , Sabrina X. Zhao 1 , John R. Soglia 1 , Amit S. Kalgutkar 1 , Stephen P. Arneric 1 , Bruce N. Rogers 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2006 Jul 13 , DOI: 10.1021/jm0602413 Donn G. Wishka 1 , Daniel P. Walker 1 , Karen M. Yates 1 , Steven C. Reitz 1 , Shaojuan Jia 1 , Jason K. Myers 1 , Kirk L. Olson 1 , E. Jon Jacobsen 1 , Mark L. Wolfe 1 , Vincent E. Groppi 1 , Alexander J. Hanchar 1 , Bruce A. Thornburgh 1 , Luz A. Cortes-Burgos 1 , Erik H. F. Wong 1 , Brian A. Staton 1 , Thomas J. Raub 1 , Nicole R. Higdon 1 , Theron M. Wall 1 , Raymond S. Hurst 1 , Rodney R. Walters 1 , William E. Hoffmann 1 , Mihaly Hajos 1 , Stanley Franklin 1 , Galen Carey 1 , Lisa H. Gold 1 , Karen K. Cook 1 , Steven B. Sands 1 , Sabrina X. Zhao 1 , John R. Soglia 1 , Amit S. Kalgutkar 1 , Stephen P. Arneric 1 , Bruce N. Rogers 1
Affiliation
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.
中文翻译：
发现N-[（3R）-1-氮杂双环[2.2.2] oct-3-基]呋喃[2,3-c]吡啶-5-甲酰胺，α7烟碱乙酰胆碱受体激动剂，可能用于治疗精神分裂症认知功能障碍的研究：合成与结构-活动关系。
N-[（3R）-1-Azabicyclo [2.2.2] oct-3-yl] furo [2,3-c] pyridine-5-carboxamide（14，PHA-543,613），一种新型的α7神经元烟碱激动剂。乙酰胆碱受体（alpha7 nAChR）已被确定为精神分裂症认知功能障碍的潜在治疗方法。化合物14是一种有效的，选择性的α7nAChR激动剂，具有出色的体外特性。该化合物的特点是大鼠具有快速的脑部渗透能力和较高的口服生物利用度，并在听觉感觉门控方面具有体内功效，并且在评估认知能力的体内模型中具有新颖的物体识别能力。
更新日期：2017-01-31
中文翻译：
发现N-[（3R）-1-氮杂双环[2.2.2] oct-3-基]呋喃[2,3-c]吡啶-5-甲酰胺，α7烟碱乙酰胆碱受体激动剂，可能用于治疗精神分裂症认知功能障碍的研究：合成与结构-活动关系。
N-[（3R）-1-Azabicyclo [2.2.2] oct-3-yl] furo [2,3-c] pyridine-5-carboxamide（14，PHA-543,613），一种新型的α7神经元烟碱激动剂。乙酰胆碱受体（alpha7 nAChR）已被确定为精神分裂症认知功能障碍的潜在治疗方法。化合物14是一种有效的，选择性的α7nAChR激动剂，具有出色的体外特性。该化合物的特点是大鼠具有快速的脑部渗透能力和较高的口服生物利用度，并在听觉感觉门控方面具有体内功效，并且在评估认知能力的体内模型中具有新颖的物体识别能力。
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