2017
Effects of varenicline on alcohol self-administration and craving in drinkers with depressive symptoms
Roberts W, Verplaetse TL, Moore K, Oberleitner L, Picciotto MR, McKee SA. Effects of varenicline on alcohol self-administration and craving in drinkers with depressive symptoms. Journal Of Psychopharmacology 2017, 31: 906-914. PMID: 28351203, PMCID: PMC5823265, DOI: 10.1177/0269881117699618.Peer-Reviewed Original ResearchConceptsDepressive symptomsAlcohol cravingAlcohol useEffects of vareniclineRole of nAChRsHuman laboratory studiesDSM-IV criteriaSymptoms of depressionAlcohol use disorderLaboratory testing sessionsMore depressive symptomsMedication pretreatmentPlasma levelsPriming doseVareniclineUse disordersTreatment moderatorsAlcohol consumptionDepression symptomsHeavy drinkersAlcohol usersDrinking taskSymptomsLess drinkingDrinkers
2013
Differential Modulation of Brain Nicotinic Acetylcholine Receptor Function by Cytisine, Varenicline, and Two Novel Bispidine Compounds: Emergent Properties of a Hybrid Molecule
Peng C, Stokes C, Mineur YS, Picciotto MR, Tian C, Eibl C, Tomassoli I, Guendisch D, Papke RL. Differential Modulation of Brain Nicotinic Acetylcholine Receptor Function by Cytisine, Varenicline, and Two Novel Bispidine Compounds: Emergent Properties of a Hybrid Molecule. Journal Of Pharmacology And Experimental Therapeutics 2013, 347: 424-437. PMID: 23959137, PMCID: PMC3807070, DOI: 10.1124/jpet.113.206904.Peer-Reviewed Original ResearchMeSH KeywordsAlkaloidsAnimalsAzocinesBehavior, AnimalBenzazepinesBrainBridged Bicyclo Compounds, HeterocyclicDose-Response Relationship, DrugDrug Partial AgonismHEK293 CellsHumansMaleMembrane PotentialsMiceMolecular StructureNicotinic AgonistsOocytesPatch-Clamp TechniquesQuinolizinesQuinoxalinesRatsRats, Sprague-DawleyReceptors, NicotinicTobacco Use DisorderVareniclineXenopus laevisConceptsPartial agonistLGN neuronsMouse tail suspension testLateral geniculate nucleus neuronsNicotinic acetylcholine receptor functionPartial agonist therapiesTail suspension testStratum radiatum interneuronsSmoking cessation drugNicotinic partial agonistAcetylcholine receptor functionHuman embryonic kidney 293 cellsSteady-state activationAgonist therapyRadiatum interneuronsEmbryonic kidney 293 cellsCessation drugsNucleus neuronsSuspension testΑ7 currentsNicotine addictionSide effectsVareniclineΑ4β2 nAChRsSR interneurons
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
Nicotine receptors and depression: revisiting and revising the cholinergic hypothesis
Mineur YS, Picciotto MR. Nicotine receptors and depression: revisiting and revising the cholinergic hypothesis. Trends In Pharmacological Sciences 2010, 31: 580-586. PMID: 20965579, PMCID: PMC2991594, DOI: 10.1016/j.tips.2010.09.004.Peer-Reviewed Original ResearchConceptsEffects of nicotineDepressive symptomsNeuronal nAChRsNovel antidepressant medicationsDepression-like behaviorMajor depressive disorderNicotinic acetylcholine receptorsAntidepressant medicationNicotine receptorsCholinergic systemDepressive disorderCholinergic hypothesisPreclinical studiesNicotinic drugsPharmacological agentsNicotinic agentsAcetylcholine receptorsEndogenous neurotransmittersSymptomsNAChRsNicotineSmokingDepressed individualsAcetylcholineReceptorsThe Nicotinic Acetylcholine Receptor Partial Agonist Varenicline Increases the Ataxic and Sedative‐Hypnotic Effects of Acute Ethanol Administration in C57BL/6J Mice
Kamens HM, Andersen J, Picciotto MR. The Nicotinic Acetylcholine Receptor Partial Agonist Varenicline Increases the Ataxic and Sedative‐Hypnotic Effects of Acute Ethanol Administration in C57BL/6J Mice. Alcohol Clinical And Experimental Research 2010, 34: 2053-2060. PMID: 20946306, PMCID: PMC2988947, DOI: 10.1111/j.1530-0277.2010.01301.x.Peer-Reviewed Original ResearchConceptsSedative-hypnotic effectsBaseline locomotor activityFixed-speed rotarodAlcohol abuseEthanol consumptionNicotinic acetylcholine receptor partial agonist vareniclineLocomotor activityEthanol-induced motor incoordinationAbility of vareniclineAcute ethanol injectionDuration of LORRLocomotor activity chambersEffects of vareniclineAcute ethanol administrationNew pharmacologic strategiesDowel testDuration of lossPartial agonist vareniclineEthanol-induced ataxiaBalance beamNicotinic modulationPharmacologic strategiesMotor incoordinationEthanol administrationSedative effectsModulation of ethanol consumption by genetic and pharmacological manipulation of nicotinic acetylcholine receptors in mice
Kamens HM, Andersen J, Picciotto MR. Modulation of ethanol consumption by genetic and pharmacological manipulation of nicotinic acetylcholine receptors in mice. Psychopharmacology 2010, 208: 613-626. PMID: 20072781, PMCID: PMC2901400, DOI: 10.1007/s00213-009-1759-1.Peer-Reviewed Original ResearchConceptsEffects of vareniclineEthanol consumptionNicotinic acetylcholine receptorsEthanol intakeAcetylcholine receptorsPharmacological manipulationΒ2 subunitRole of nAChRsTwo-bottle choice paradigmWild-type micePartial agonist vareniclineSubunit knockout miceMesolimbic dopamine systemNicotinic controlVarenicline doseAlcohol drinkingAgonist vareniclineKnockout miceDopamine systemNicotine responseChallenge studiesVareniclineNAChRsReceptor subunitsMice
2009
Varenicline Reduces Alcohol Self-Administration in Heavy-Drinking Smokers
McKee SA, Harrison EL, O'Malley SS, Krishnan-Sarin S, Shi J, Tetrault JM, Picciotto MR, Petrakis IL, Estevez N, Balchunas E. Varenicline Reduces Alcohol Self-Administration in Heavy-Drinking Smokers. Biological Psychiatry 2009, 66: 185-190. PMID: 19249750, PMCID: PMC2863311, DOI: 10.1016/j.biopsych.2009.01.029.Peer-Reviewed Original ResearchConceptsHeavy drinking smokersSelf-administration periodAlcohol consumptionPartial nicotinic agonistPlacebo-controlled investigationEffects of vareniclineReduced ethanol intakeAlcohol Self-AdministrationAlcohol use disorderNicotinic acetylcholine receptorsMedication pretreatmentAdverse eventsNumber of drinksPreclinical evidenceAdditional drinkEthanol intakeTobacco dependenceDaily smokersPriming doseVareniclineComorbid disordersNicotinic agonistsUse disordersPriming drinkPotential treatmentVarenicline 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