2017
Reversal of Nicotine Withdrawal Signs Through Positive Allosteric Modulation of α4β2 Nicotinic Acetylcholine Receptors in Male Mice
Hamouda AK, Jackson A, Bagdas D, Damaj M. Reversal of Nicotine Withdrawal Signs Through Positive Allosteric Modulation of α4β2 Nicotinic Acetylcholine Receptors in Male Mice. Nicotine & Tobacco Research 2017, 20: 903-907. PMID: 29059422, PMCID: PMC5991208, DOI: 10.1093/ntr/ntx183.Peer-Reviewed Original ResearchConceptsNicotine withdrawal symptomsSpontaneous nicotine withdrawalNicotine withdrawal signsNicotine withdrawalWithdrawal symptomsPositive allosteric modulatorsCessation aidWithdrawal signsMale miceMouse modelAllosteric modulatorsNicotinic acetylcholine receptor agonistNAChR-positive allosteric modulatorsAcetylcholine receptor agonistDose-dependent reversalICR male miceΑ4β2 nicotinic acetylcholine receptorsPositive allosteric modulationAnxiety-like behaviorNicotinic acetylcholine receptorsPotential clinical useAcute injectionRelapse rateTobacco smokingDay infusionInteractive effects of an N-methyl-d-aspartate receptor antagonist and a nicotinic acetylcholine receptor agonist on mismatch negativity: Implications for schizophrenia
Hamilton HK, D'Souza DC, Ford JM, Roach BJ, Kort NS, Ahn KH, Bhakta S, Ranganathan M, Mathalon DH. Interactive effects of an N-methyl-d-aspartate receptor antagonist and a nicotinic acetylcholine receptor agonist on mismatch negativity: Implications for schizophrenia. Schizophrenia Research 2017, 191: 87-94. PMID: 28711472, PMCID: PMC5745273, DOI: 10.1016/j.schres.2017.06.040.Peer-Reviewed Original ResearchConceptsNicotinic acetylcholine receptor agonistAcetylcholine receptor agonistReceptor agonistHealthy volunteersN-methyl-D-aspartate receptor antagonistPathophysiology of schizophreniaAuditory processing abnormalitiesProfile of effectsMMN amplitudeNicotine preventsNicotine administrationReceptor hypofunctionNMDAR hypofunctionNMDAR antagonistsReceptor antagonistMismatch negativity (MMN) event-related potential (ERP) componentPresent doseNicotinic agonistsSchizophrenia patientsCigarette useKetamineDeviant typesNeurophysiological effectsSecondary analysisMMN abnormalities
2009
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
1996
Nicotinic actions on neurones of the central autonomic area in rat spinal cord slices.
Bordey A, Feltz P, Trouslard J. Nicotinic actions on neurones of the central autonomic area in rat spinal cord slices. The Journal Of Physiology 1996, 497: 175-187. PMID: 8951720, PMCID: PMC1160921, DOI: 10.1113/jphysiol.1996.sp021758.Peer-Reviewed Original ResearchConceptsSpontaneous excitatory postsynaptic currentsCentral autonomic areaSympathetic preganglionic neuronesSpinal cord slicesGlutamate-induced currentsAutonomic areasCord slicesTransverse thoracolumbar spinal cord slicesAgonist rank order potencyAction potentialsRat spinal cord slicesWhole-cell patch-clamp techniqueNicotinic acetylcholine receptor agonistExcitatory synaptic activityPresence of tetrodotoxinAcetylcholine receptor agonistExcitatory postsynaptic currentsMembrane current noisePatch-clamp techniqueCurrent-clamp conditionsDetectable current responseRank order potencySEPSC amplitudeVoltage-clamp conditionsStrong inward rectification
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