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
2010
Brain β2*-nicotinic acetylcholine receptor occupancy after use of a nicotine inhaler
Esterlis I, Mitsis EM, Batis JC, Bois F, Picciotto MR, Stiklus SM, Kloczynski T, Perry E, Seibyl JP, McKee S, Staley JK, Cosgrove KP. Brain β2*-nicotinic acetylcholine receptor occupancy after use of a nicotine inhaler. The International Journal Of Neuropsychopharmacology 2010, 14: 389-398. PMID: 21029513, PMCID: PMC3510008, DOI: 10.1017/s1461145710001227.Peer-Reviewed Original ResearchConceptsNicotine inhalerWithdrawal symptomsReceptor occupancyTobacco smokingLow nicotine cigarettesAdministration of nicotineHigh receptor occupancyDoses of nicotineNicotinic acetylcholine receptorsInhaler useTobacco smokersBaseline scanRegular cigarettesInhalerConstant infusionAcetylcholine receptorsSPECT studiesCigarettesSymptomsBeta 2Significant decreaseNicotineSignificant differencesSmokingNAChRs