2011
Dissociation between duration of action in the forced swim test in mice and nicotinic acetylcholine receptor occupancy with sazetidine, varenicline, and 5-I-A85380
Caldarone BJ, Wang D, Paterson NE, Manzano M, Fedolak A, Cavino K, Kwan M, Hanania T, Chellappan SK, Kozikowski AP, Olivier B, Picciotto MR, Ghavami A. Dissociation between duration of action in the forced swim test in mice and nicotinic acetylcholine receptor occupancy with sazetidine, varenicline, and 5-I-A85380. Psychopharmacology 2011, 217: 199-210. PMID: 21487659, PMCID: PMC3266849, DOI: 10.1007/s00213-011-2271-y.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsAntidepressive AgentsAzetidinesBehavior, AnimalBenzazepinesBrainData Interpretation, StatisticalDose-Response Relationship, DrugLigandsMaleMiceMice, Inbred BALB CMice, Inbred C57BLMolecular StructureMotor ActivityNicotinic AgonistsProtein BindingPyridinesQuinoxalinesReceptors, NicotinicSwimmingTime FactorsVareniclineConceptsAntidepressant-like effectsAntidepressant-like actionSwim testDuration of actionReceptor occupancyNAChR antagonist mecamylamineDihydro-β-erythroidineAcetylcholine receptor agonistRole of β2Partial agonist vareniclineSymptoms of depressionNAChR β2Antagonist mecamylamineReceptor agonistActive dosesAgonist vareniclineSazetidinePartial agonistVareniclineObjectivesThe studyBehavioral efficacyNAChRsBehavioral responsesAgonistsPromising target
1999
Two pharmacologically distinct components of nicotinic receptor-mediated rubidium efflux in mouse brain require the beta2 subunit.
Marks MJ, Whiteaker P, Calcaterra J, Stitzel JA, Bullock AE, Grady SR, Picciotto MR, Changeux JP, Collins AC. Two pharmacologically distinct components of nicotinic receptor-mediated rubidium efflux in mouse brain require the beta2 subunit. Journal Of Pharmacology And Experimental Therapeutics 1999, 289: 1090-103. PMID: 10215692.Peer-Reviewed Original ResearchConceptsBeta2 subunitBeta2 null mutant miceConcentration-effect curvesMouse brain synaptosomesAlpha4beta2 receptorsBrain synaptosomesNicotinic agonistsMouse brainRubidium effluxMutant miceLine radioactivity detectionDHbetaEAgonistsEffluxBrainStimulationRadioactivity detectionPotencyHexamethoniumErythroidineResponseAcetylcholineMethyllycaconitineAntagonistBungarotoxin
1998
Identification of Four Classes of Brain Nicotinic Receptors Using β2 Mutant Mice
Zoli M, Léna C, Picciotto M, Changeux J. Identification of Four Classes of Brain Nicotinic Receptors Using β2 Mutant Mice. Journal Of Neuroscience 1998, 18: 4461-4472. PMID: 9614223, PMCID: PMC6792706, DOI: 10.1523/jneurosci.18-12-04461.1998.Peer-Reviewed Original ResearchConceptsBeta2-/- miceElectrophysiological experimentsBrain regionsNeuronal nicotinic acetylcholine receptor subunitBrain nicotinic receptorsNicotinic acetylcholine receptor subunitsMost brain regionsPatch-clamp recordingsReceptor autoradiography studiesOrder of potencyDifferent brain areasAcetylcholine receptor subunitsThin brain slicesDifferent brain regionsIndividual alpha subunitsAutoradiography studiesBrain slicesNicotinic receptorsNicotinic agonistsHigh affinitySubunit compositionBrain areasAlpha subunitAlpha7 subunitType 2