Discovery of 4-(5-Methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a Novel α7 Nicotinic Acetylcholine Receptor Agonist for the Treatment of Cognitive Disorders in Schizophrenia: Synthesis, SAR Development, and in Vivo Efficacy in Cognition Models
O’Donnell C, Rogers B, Bronk B, Bryce D, Coe J, Cook K, Duplantier A, Evrard E, Hajós M, Hoffmann W, Hurst R, Maklad N, Mather R, McLean S, Nedza F, O’Neill B, Peng L, Qian W, Rottas M, Sands S, Schmidt A, Shrikhande A, Spracklin D, Wong D, Zhang A, Zhang L. Discovery of 4-(5-Methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a Novel α7 Nicotinic Acetylcholine Receptor Agonist for the Treatment of Cognitive Disorders in Schizophrenia: Synthesis, SAR Development, and in Vivo Efficacy in Cognition Models. Journal Of Medicinal Chemistry 2009, 53: 1222-1237. PMID: 20043678, DOI: 10.1021/jm9015075.Peer-Reviewed Original ResearchMeSH Keywordsalpha7 Nicotinic Acetylcholine ReceptorAnimalsAzabicyclo CompoundsBiological AvailabilityCells, CulturedCognition DisordersEpithelial CellsFemaleHippocampusHumansKidneyMicrosomes, LiverNicotinic AgonistsNootropic AgentsOocytesOxazolesRatsReceptors, NicotinicSchizophreniaSkinStructure-Activity RelationshipXenopus laevisConceptsVivo efficacyΑ7 nicotinic acetylcholine receptor agonistCognitive deficitsAlpha 7Nicotinic acetylcholine receptor agonistExcellent brain penetrationAcetylcholine receptor agonistNovel object recognitionAuditory sensory gatingHigh oral bioavailabilityBrain penetrationReceptor agonistNeurological conditionsCognitive disordersPotential treatmentReceptor occupancySensory gatingAlzheimer's diseaseOral bioavailabilityAgonistsSchizophreniaTreatmentDiseaseCompound 24Efficacy
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