1192807-65-0Relevant articles and documents
BMS-933043, a Selective α7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia
King, Dalton,Iwuagwu, Christiana,Cook, Jim,McDonald, Ivar M.,Mate, Robert,Zusi, F. Christopher,Hill, Matthew D.,Fang, Haiquan,Zhao, Rulin,Wang, Bei,Easton, Amy E.,Miller, Regina,Post-Munson, Debra,Knox, Ronald J.,Gallagher, Lizbeth,Westphal, Ryan,Molski, Thaddeus,Fan, Jingsong,Clarke, Wendy,Benitex, Yulia,Lentz, Kimberley A.,Denton, Rex,Morgan, Daniel,Zaczek, Robert,Lodge, Nicholas J.,Bristow, Linda J.,Macor, John E.,Olson, Richard E.
, p. 366 - 371 (2017/03/17)
The therapeutic treatment of negative symptoms and cognitive dysfunction associated with schizophrenia is a significant unmet medical need. Preclinical literature indicates that α7 neuronal nicotinic acetylcholine (nACh) receptor agonists may provide an effective approach to treating cognitive dysfunction in schizophrenia. We report herein the discovery and evaluation of 1c (BMS-933043), a novel and potent α7 nACh receptor partial agonist with high selectivity against other nicotinic acetylcholine receptor subtypes (>100-fold) and the 5-HT3A receptor (>300-fold). In vivo activity was demonstrated in a preclinical model of cognitive impairment, mouse novel object recognition. BMS-933043 has completed Phase I clinical trials.
Α 7 as intranuclear hydroxynicotinic acetylcholine receptor quinuclidines compd.
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Paragraph 0252; 0254; 0308; 0310, (2018/10/03)
PROBLEM TO BE SOLVED: To provide ligands for the nicotinic α-7 receptor used for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.SOLUTION: The disclosure provides compounds of the specified formula I, including their salts, and compositions and methods using the compounds.
QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
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Page/Page column 91, (2009/10/31)
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.