2019
A silent agonist of α7 nicotinic acetylcholine receptors modulates inflammation ex vivo and attenuates EAE
Godin J, Roy P, Quadri M, Bagdas D, Toma W, Narendrula-Kotha R, Kishta O, Damaj M, Horenstein N, Papke R, Simard A. A silent agonist of α7 nicotinic acetylcholine receptors modulates inflammation ex vivo and attenuates EAE. Brain Behavior And Immunity 2019, 87: 286-300. PMID: 31874200, PMCID: PMC7604877, DOI: 10.1016/j.bbi.2019.12.014.Peer-Reviewed Original ResearchConceptsNicotinic acetylcholine receptorsSilent agonistInflammatory painCytokine productionΑ7 nAChRsAnimal modelsAcetylcholine receptorsΑ7 nicotinic acetylcholine receptorNon-neuronal nAChRsExperimental autoimmune encephalomyelitisChronic inflammatory painAnti-inflammatory compoundsInflammation ex vivoChannel openingAutoimmune encephalomyelitisAntagonist mecamylamineMultiple sclerosisInflammatory disordersModulates inflammationMacrophage numbersDisease manifestationsNervous systemReceptor desensitizationInflammationAgonists
2018
Pharmacological modulation of the α7 nicotinic acetylcholine receptor in a mouse model of mecamylamine-precipitated nicotine withdrawal
Jackson A, Papke RL, Damaj MI. Pharmacological modulation of the α7 nicotinic acetylcholine receptor in a mouse model of mecamylamine-precipitated nicotine withdrawal. Psychopharmacology 2018, 235: 1897-1905. PMID: 29549391, PMCID: PMC6015775, DOI: 10.1007/s00213-018-4879-7.Peer-Reviewed Original ResearchConceptsPositive allosteric modulatorsΑ7 nicotinic acetylcholine receptorMecamylamine-precipitated nicotine withdrawalNicotine withdrawal behaviorsNicotine withdrawalNicotinic acetylcholine receptorsSomatic signsPharmacological modulationNon-selective nAChR antagonist mecamylamineAcetylcholine receptorsNicotine withdrawal-induced hyperalgesiaWithdrawal-induced hyperalgesiaDose-related fashionNicotine withdrawal signsNAChR antagonist mecamylamineAnxiety-like behaviorAntagonist mecamylamineWithdrawal signsPreclinical dataNicotine rewardΑ7 nAChRsAgonist PNU282987Mouse modelWithdrawal behaviorAllosteric modulators
2016
Nicotine Enhances the Hypnotic and Hypothermic Effects of Alcohol in the Mouse
Slater CA, Jackson A, Muldoon PP, Dawson A, O'Brien M, Soll LG, Abdullah R, Carroll FI, Tapper AR, Miles MF, Banks ML, Bettinger JC, Damaj IM. Nicotine Enhances the Hypnotic and Hypothermic Effects of Alcohol in the Mouse. Alcohol Clinical And Experimental Research 2016, 40: 62-72. PMID: 26727524, PMCID: PMC4700556, DOI: 10.1111/acer.12918.Peer-Reviewed Original ResearchMeSH Keywordsalpha7 Nicotinic Acetylcholine ReceptorAnimalsAzetidinesBody TemperatureCentral Nervous System DepressantsDrug InteractionsEthanolHypnotics and SedativesHypothermiaKetamineMecamylamineMiceMice, Inbred C57BLMice, Inbred DBAMice, KnockoutNicotineNicotinic AgonistsNicotinic AntagonistsPentobarbitalPyridinesReceptors, NicotinicReflex, RightingVareniclineConceptsHypnotic effectsLORR testEtOH intakeReceptor efficacyAcute nicotine injectionDuration of EtOHNicotinic acetylcholine receptor subtypesΑ7 knockout miceNicotinic partial agonist vareniclineAcetylcholine receptor subtypesEffects of nicotineNicotinic antagonist mecamylamineDevelopment of toleranceEffects of EtOHPartial agonist vareniclineAcute injectionAcute nicotineNicotine administrationNicotine exposureAntagonist mecamylamineNicotine injectionHypothermic effectNicotine effectsHypnotic propertiesPharmacological interactions
2015
Multiple Nicotinic Acetylcholine Receptor Subtypes in the Mouse Amygdala Regulate Affective Behaviors and Response to Social Stress
Mineur YS, Fote GM, Blakeman S, Cahuzac EL, Newbold SA, Picciotto MR. Multiple Nicotinic Acetylcholine Receptor Subtypes in the Mouse Amygdala Regulate Affective Behaviors and Response to Social Stress. Neuropsychopharmacology 2015, 41: 1579-1587. PMID: 26471256, PMCID: PMC4832019, DOI: 10.1038/npp.2015.316.Peer-Reviewed Original ResearchConceptsDepression-like behaviorBasolateral amygdalaΑ7 nAChRsCholinergic signalingMultiple nicotinic acetylcholine receptor subtypesNon-selective nAChR antagonist mecamylamineNicotinic acetylcholine receptor activityNicotinic acetylcholine receptor subtypesStress-mediated behaviorsAntidepressant-like effectsAcetylcholine receptor activityC-Fos immunoreactivityNAChR antagonist mecamylamineAcetylcholine receptor subtypesEffects of nicotineMajor depressive disorderSocial defeat stressAnxiety-like behaviorPre-clinical studiesHuman clinical trialsModels of anxietyMouse behavioral modelsHypercholinergic stateAntagonist mecamylamineLocal infusion
2011
ACSL6 Is Associated with the Number of Cigarettes Smoked and Its Expression Is Altered by Chronic Nicotine Exposure
Chen J, Brunzell DH, Jackson K, van der Vaart A, Z. J, Payne TJ, Sherva R, Farrer LA, Gejman P, Levinson DF, Holmans P, Aggen SH, Damaj I, Kuo PH, Webb BT, Anton R, Kranzler HR, Gelernter J, Li MD, Kendler KS, Chen X. ACSL6 Is Associated with the Number of Cigarettes Smoked and Its Expression Is Altered by Chronic Nicotine Exposure. PLOS ONE 2011, 6: e28790. PMID: 22205969, PMCID: PMC3243669, DOI: 10.1371/journal.pone.0028790.Peer-Reviewed Original ResearchConceptsACSL6 geneNicotine exposureNicotinic receptor antagonist mecamylaminePrevious schizophrenia studiesChronic nicotine exposureNicotinic receptor activationHippocampus of miceNumber of cigarettesOsmotic mini pumpsQuantity of cigarettesNon-schizophrenic subjectsAssociation of schizophreniaCigarettes SmokedHeavy smokersTobacco smokingNicotine administrationAntagonist mecamylamineControl subjectsIndependent associationTobacco dependenceFTND scoreHigh riskMini pumpsChronic exposureReceptor activationDissociation 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
Effects of the nicotinic receptor antagonist mecamylamine on ad-lib smoking behavior, topography, and nicotine levels in smokers with and without schizophrenia: A preliminary study
McKee SA, Weinberger AH, Harrison EL, Coppola S, George TP. Effects of the nicotinic receptor antagonist mecamylamine on ad-lib smoking behavior, topography, and nicotine levels in smokers with and without schizophrenia: A preliminary study. Schizophrenia Research 2009, 115: 317-324. PMID: 19700263, PMCID: PMC2784178, DOI: 10.1016/j.schres.2009.07.019.Peer-Reviewed Original ResearchMeSH KeywordsAdolescentAdultBehavior, AddictiveDouble-Blind MethodFemaleHumansMaleMecamylamineMiddle AgedNeuropsychological TestsNicotinic AntagonistsReaction TimeSchizophreniaSelf AdministrationSmokingSmoking CessationSubstance Withdrawal SyndromeSurveys and QuestionnairesTobacco Use DisorderYoung AdultConceptsAd lib smoking behaviorNicotine levelsSmoking behaviorControl smokersSmoking topographyNicotinic receptor antagonist mecamylamineNicotinic acetylcholine receptor antagonistHealthy control smokersHigh-affinity nAChRsIntensity of smokingAd lib smokingEffects of mecamylamineNumber of cigarettesPlacebo-controlled designAcetylcholine receptor antagonistNicotine exposureAntagonist mecamylamineCompensatory smokingReceptor antagonistSmoking intensityMecamylamineSmokersSmokingSchizophreniaPreliminary study
2006
The nicotinic antagonist mecamylamine has antidepressant-like effects in wild-type but not β2- or α7-nicotinic acetylcholine receptor subunit knockout mice
Rabenstein RL, Caldarone BJ, Picciotto MR. The nicotinic antagonist mecamylamine has antidepressant-like effects in wild-type but not β2- or α7-nicotinic acetylcholine receptor subunit knockout mice. Psychopharmacology 2006, 189: 395-401. PMID: 17016705, DOI: 10.1007/s00213-006-0568-z.Peer-Reviewed Original ResearchConceptsAntidepressant-like effectsAntagonist mecamylamineNicotinic acetylcholine receptor activityNoncompetitive nAChR antagonist mecamylamineAntagonist dihydro-β-erythroidineΑ7 knockout miceΑ7-nAChR subunitAcetylcholine receptor activityEffects of mecamylamineNAChR antagonist mecamylamineDihydro-β-erythroidineNicotinic antagonist mecamylamineSubunit knockout miceBaseline locomotor activityDose-response studyMethodsAdult miceAntagonist hexamethoniumAntidepressant efficacyAntidepressant responseCentral nAChRsImmobility timeCholinergic transmissionSwim testMecamylamineSuspension testNeuropsychological deficits in nonsmokers with schizophrenia: Effects of a nicotinic antagonist
Sacco KA, Termine A, Dudas MM, Seyal AA, Allen TM, Vessicchio JC, Wexler BE, George TP. Neuropsychological deficits in nonsmokers with schizophrenia: Effects of a nicotinic antagonist. Schizophrenia Research 2006, 85: 213-221. PMID: 16678390, DOI: 10.1016/j.schres.2006.03.025.Peer-Reviewed Original ResearchConceptsWisconsin Card Sorting TestContinuous Performance TestControl nonsmokersNeuropsychological performanceStroop Color-Word TestNeuropsychological deficitsNicotinic acetylcholine receptor systemAcetylcholine receptor systemPosition testVisuospatial working memoryCigarette smokingAntagonist mecamylamineNicotinic antagonistsNeuropsychological dysfunctionNAChR blockadeNonsmokersSchizophrenia diagnosisColor-Word TestMecamylamineReceptor systemNeuropsychological assessmentSchizophreniaCard Sorting TestCounterbalanced designTest week
2004
High-affinity nicotinic acetylcholine receptors are required for antidepressant effects of amitriptyline on behavior and hippocampal cell proliferation
Caldarone BJ, Harrist A, Cleary MA, Beech RD, King SL, Picciotto MR. High-affinity nicotinic acetylcholine receptors are required for antidepressant effects of amitriptyline on behavior and hippocampal cell proliferation. Biological Psychiatry 2004, 56: 657-664. PMID: 15522249, DOI: 10.1016/j.biopsych.2004.08.010.Peer-Reviewed Original ResearchMeSH KeywordsAmitriptylineAnalysis of VarianceAnimalsAntidepressive Agents, TricyclicBehavior, AnimalBromodeoxyuridineCell CountCell ProliferationDose-Response Relationship, DrugDrosophila ProteinsDrug InteractionsHelplessness, LearnedHindlimb SuspensionHippocampusImmunohistochemistryMecamylamineMiceMice, Inbred C57BLMice, KnockoutNeuronsNicotinic AntagonistsNortriptylineReceptors, NicotinicSwimmingConceptsHigh-affinity nAChRsHippocampal cell proliferationNicotinic acetylcholine receptorsSwim testAcetylcholine receptorsCell proliferationHigh-affinity nicotinic acetylcholine receptorsNoncompetitive nAChR antagonist mecamylamineAntagonism of nAChRsAntidepressant-induced increasesAntidepressant-like effectsNAChR antagonist mecamylamineWild-type miceInhibition of nAChRsAntidepressants actAntidepressant actionAntidepressant effectsChronic treatmentAntagonist mecamylamineAntidepressant propertiesTricyclic antidepressantsAntidepressant activityTherapeutic effectKnockout miceNoncompetitive antagonist
2001
Nicotine Receptor Inactivation Decreases Sensitivity to Cocaine
Zachariou V, Caldarone B, Weathers-Lowin A, George T, Elsworth J, Roth R, Changeux J, Picciotto M. Nicotine Receptor Inactivation Decreases Sensitivity to Cocaine. Neuropsychopharmacology 2001, 24: 576-589. PMID: 11282258, DOI: 10.1016/s0893-133x(00)00224-4.Peer-Reviewed Original ResearchConceptsPlace preferenceDA turnoverLow doseHigh-affinity nicotinic acetylcholine receptorsMesolimbic DA systemHigh-affinity nAChRsNicotinic antagonist mecamylamineWild-type miceMesolimbic dopamine systemFos-related antigensProperties of nicotineCocaine place preferenceΒ2 subunitNicotinic acetylcholine receptorsAntagonist mecamylamineDA releaseMetabolite DOPACNeurochemical changesSubthreshold doseType miceDopamine systemPsychomotor stimulantsAcetylcholine receptorsHigh dosesBrain regions
2000
Nicotine inhibits firing activity of dorsal raphe 5-HT neurones in vivo
Engberg G, Erhardt S, Sharp T, Hajós M. Nicotine inhibits firing activity of dorsal raphe 5-HT neurones in vivo. Naunyn-Schmiedeberg's Archives Of Pharmacology 2000, 362: 41-45. PMID: 10935531, DOI: 10.1007/s002100000252.Peer-Reviewed Original ResearchConceptsEffects of nicotineDorsal rapheChloral hydrate-anaesthetised ratsNicotine antagonist mecamylamineBrain monoaminergic systemsDependence-inducing drugsExtracellular electrophysiological recordingsMicroiontophoretic applicationAntagonist mecamylamineAfferent pathwaysMonoaminergic systemsReceptor antagonistNicotine inhibitsApparent tachyphylaxisElectrophysiological recordingsFiring rateNeuronesNicotineInhibitory effectRapheTransient inhibitionPossible involvementInhibitionTachyphylaxisChlorisondamine
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