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Alpha 7 nicotinic acetylcholine receptor (alpha(7) nAChR) agonists are promising therapeutic candidates for the treatment of cognitive impairment associated with a variety of disorders including Alzheimer's disease and schizophrenia. Alpha 7 nAChRs are expressed in brain regions associated with cognitive function, regulate cholinergic neurotransmission and have been shown to be down regulated in both schizophrenia and Alzheimer's disease. Herein we report a novel, potent small molecule agonist of the alpha 7 nAChR, SEN12333/WAY-317538. This compound is a selective agonist of the alpha(7) nAChR with excellent in vitro and in vivo profiles, excellent brain penetration and oral bioavailability, and demonstrates in vivo efficacy in multiple behavioural cognition models. The SAR and biological evaluation of this series of compounds are discussed.


Simon N Haydar, Chiara Ghiron, Laura Bettinetti, Hendrick Bothmann, Thomas A Comery, John Dunlop, Salvatore La Rosa, Iolanda Micco, Martina Pollastrini, Joanna Quinn, Renza Roncarati, Carla Scali, Michela Valacchi, Maurizio Varrone, Riccardo Zanaletti. SAR and biological evaluation of SEN12333/WAY-317538: Novel alpha 7 nicotinic acetylcholine receptor agonist. Bioorganic & medicinal chemistry. 2009 Jul 15;17(14):5247-58

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PMID: 19515567

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