期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 8, 期 3, 页码 366-371出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.7b00032
关键词
Schizophrenia; alpha 7 neuronal nicotinic acetylcholine receptor; alpha 7 nAChR partial agonist; quinuclidine; clinical candidate
The therapeutic treatment of negative symptoms and cognitive dysfunction associated with schizophrenia is a significant unmet medical need. Preclinical literature indicates that a? 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 alpha 7 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.
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