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
2009
Varenicline has antidepressant-like activity in the forced swim test and augments sertraline's effect
Rollema H, Guanowsky V, Mineur YS, Shrikhande A, Coe JW, Seymour PA, Picciotto MR. Varenicline has antidepressant-like activity in the forced swim test and augments sertraline's effect. European Journal Of Pharmacology 2009, 605: 114-116. PMID: 19168054, PMCID: PMC2707785, DOI: 10.1016/j.ejphar.2009.01.002.Peer-Reviewed Original ResearchConceptsAntidepressant-like activitySwim testPartial agonistNicotinic acetylcholine receptor activityNicotinic acetylcholine receptor partial agonistSelective serotonin reuptake inhibitor sertralineSerotonin reuptake inhibitor sertralineSelective serotonin reuptake inhibitorsAntidepressant-like propertiesAcetylcholine receptor activitySerotonin reuptake inhibitorsSmoking cessation aidReceptor partial agonistSertraline effectsVarenicline doseAntidepressant responseReuptake inhibitorsAntidepressant potentialCessation aidActive dosesAcetylcholine receptorsReceptor activityVareniclineMouse strainsAgonists
2007
Cytisine, a partial agonist of high-affinity nicotinic acetylcholine receptors, has antidepressant-like properties in male C57BL/6J mice
Mineur YS, Somenzi O, Picciotto MR. Cytisine, a partial agonist of high-affinity nicotinic acetylcholine receptors, has antidepressant-like properties in male C57BL/6J mice. Neuropharmacology 2007, 52: 1256-1262. PMID: 17320916, PMCID: PMC1959230, DOI: 10.1016/j.neuropharm.2007.01.006.Peer-Reviewed Original ResearchConceptsAntidepressant-like effectsAntidepressant-like propertiesAntidepressant efficacyNicotinic acetylcholine receptorsPartial agonistBasolateral amygdalaAcetylcholine receptorsHigh-affinity nicotinic acetylcholine receptorsC-Fos immunoreactivityNovel antidepressant drugsC-fos expressionPotential neurobiological correlatesAlpha3/Classical antidepressantsAntidepressant drugsRodent modelsImmunohistochemical analysisNeuronal activityAnimal modelsFull agonistAgonistsNeuronal systemsEfficacyNeurobiological correlatesCytisine
2005
Galanin can attenuate opiate reinforcement and withdrawal
Picciotto MR, Hawes JJ, Brunzell DH, Zachariou V. Galanin can attenuate opiate reinforcement and withdrawal. Neuropeptides 2005, 39: 313-315. PMID: 15944028, DOI: 10.1016/j.npep.2004.12.001.Peer-Reviewed Original ResearchConceptsOpiate reinforcementGalanin receptor agonistAction of opiatesUseful therapeutic agentEndogenous galaninReceptor agonistGalaninKnockout miceBrain areasTransgenic miceBrain regionsBehavioral signsOpiate addictionTherapeutic agentsBody of dataAltered susceptibilityWithdrawalMiceReceptorsAgonistsOpiates
2002
Nicotinic receptors in aging and dementia
Picciotto MR, Zoli M. Nicotinic receptors in aging and dementia. Developmental Neurobiology 2002, 53: 641-655. PMID: 12436427, DOI: 10.1002/neu.10102.Peer-Reviewed Original ResearchConceptsNicotinic agonistsCognitive functionNeuronal nicotinic acetylcholine receptorsDevelopment of dementiaNicotinic acetylcholine receptorsCholinergic markersCholinergic functionNeuronal degenerationNicotinic receptorsEpidemiological studiesNicotinic functionAnimal studiesNeurodegenerative illnessesAcetylcholine receptorsCognitive deficitsDementiaNeurodegenerative diseasesImpaired subjectsDistinct actionsPatientsAgonistsDiseaseNicotineReceptorsSmokingCharacterization of [125I]epibatidine binding and nicotinic agonist‐mediated 86Rb+ efflux in interpeduncular nucleus and inferior colliculus of β2 null mutant mice
Marks MJ, Whiteaker P, Grady SR, Picciotto MR, McIntosh JM, Collins AC. Characterization of [125I]epibatidine binding and nicotinic agonist‐mediated 86Rb+ efflux in interpeduncular nucleus and inferior colliculus of β2 null mutant mice. Journal Of Neurochemistry 2002, 81: 1102-1115. PMID: 12065623, DOI: 10.1046/j.1471-4159.2002.00910.x.Peer-Reviewed Original ResearchMeSH KeywordsAcetylcholineAlkaloidsAnimalsAzocinesBinding, CompetitiveBridged Bicyclo Compounds, HeterocyclicDose-Response Relationship, DrugInferior ColliculiIodine RadioisotopesMesencephalonMiceMice, Mutant StrainsNicotinic AgonistsNicotinic AntagonistsPyridinesQuinolizinesReceptors, NicotinicRubidium RadioisotopesTritiumConceptsInterpeduncular nucleusInferior colliculusBrain regionsAccessory olfactory nucleusNull mutant miceOlfactory nucleusNicotinic antagonistsD-tubocurarineMedial habenulaSelective antagonistNicotinic agonistsSuperior colliculusMouse brainAgonistsColliculusMutant micePotent agonistSimilar potencyAntagonistNicotinic activityEfflux
2001
Nicotinic agonists stimulate acetylcholine release from mouse interpeduncular nucleus: a function mediated by a different nAChR than dopamine release from striatum
Grady S, Meinerz N, Cao J, Reynolds A, Picciotto M, Changeux J, McIntosh J, Marks M, Collins A. Nicotinic agonists stimulate acetylcholine release from mouse interpeduncular nucleus: a function mediated by a different nAChR than dopamine release from striatum. Journal Of Neurochemistry 2001, 76: 258-268. PMID: 11145999, DOI: 10.1046/j.1471-4159.2001.00019.x.Peer-Reviewed Original ResearchMeSH KeywordsAcetylcholineAlkaloidsAnimalsAzocinesCalciumCholineConotoxinsCorpus StriatumDopamineDose-Response Relationship, DrugFemaleHeterozygoteHomozygoteMaleMesencephalonMiceMice, Inbred C57BLMice, Mutant StrainsNicotinic AgonistsNicotinic AntagonistsPresynaptic TerminalsProtein SubunitsQuinolizinesReceptors, NicotinicSynaptosomesConceptsAgonist-stimulated releaseAcetylcholine releaseInterpeduncular nucleusStriatal synaptosomesDopamine releaseNicotinic agonistsAlpha-conotoxin MIIMouse striatal synaptosomesAlpha-conotoxin AuIBNicotinic acetylcholine receptorsDose-response curveAcetylcholine receptorsExternal calciumDifferent nAChRsDesensitization ratePersistent phaseAgonistsL nicotineSynaptosomesNull mutationSimilar decreaseInhibition curvesMiceReleaseAcetylcholine
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
Pharmacological characterization of nicotinic receptor-stimulated GABA release from mouse brain synaptosomes.
Lu Y, Grady S, Marks M, Picciotto M, Changeux J, Collins A. Pharmacological characterization of nicotinic receptor-stimulated GABA release from mouse brain synaptosomes. Journal Of Pharmacology And Experimental Therapeutics 1998, 287: 648-57. PMID: 9808692.Peer-Reviewed Original ResearchConceptsGamma-aminobutyric acidGABA releaseMouse brain synaptosomesBrain synaptosomesNicotinic agonistsNicotine bindingBeta2 null mutant miceNull mutant miceRecent electrophysiological studiesRodent brain tissueConcentration-dependent mannerAgonist inhibitionAlpha-BungarotoxinNeurochemical approachesPharmacological characterizationNM tetrodotoxinElectrophysiological studiesSame agonistBrain regionsBrain tissueMutant miceAgonistsEmax valuesBeta2 subunitMaximal release