2022
Differences in Quantification of the Metabotropic Glutamate Receptor 5 Across Bipolar Disorder and Major Depressive Disorder
Holmes S, Asch R, Davis M, DellaGioia N, Pashankar N, Gallezot J, Nabulsi N, Matuskey D, Sanacora G, Carson R, Blumberg H, Esterlis I. Differences in Quantification of the Metabotropic Glutamate Receptor 5 Across Bipolar Disorder and Major Depressive Disorder. Biological Psychiatry 2022, 93: 1099-1107. PMID: 36764853, PMCID: PMC10164841, DOI: 10.1016/j.biopsych.2022.10.018.Peer-Reviewed Original ResearchMeSH KeywordsBipolar DisorderDepressive Disorder, MajorHumansMagnetic Resonance ImagingPositron-Emission TomographyPrefrontal CortexReceptor, Metabotropic Glutamate 5ConceptsMajor depressive disorderMetabotropic glutamate receptor 5Glutamate receptor 5MGluR5 availabilityBipolar disorderPositron emission tomographyHC groupDepressive disorderReceptor 5Emission tomographyHealthy control individualsPossible treatment targetsGlutamate transmissionBD depressionTreatment strategiesBD groupMGluR5Depressive symptomsNovel treatmentsCognitive alterationsTreatment targetsSynaptic plasticityControl individualsAccurate diagnosisSignificant negative correlation
2019
Measuring the effects of ketamine on mGluR5 using [18F]FPEB and PET
Holmes SE, Gallezot JD, Davis MT, DellaGioia N, Matuskey D, Nabulsi N, Krystal JH, Javitch JA, DeLorenzo C, Carson RE, Esterlis I. Measuring the effects of ketamine on mGluR5 using [18F]FPEB and PET. Cerebrovascular And Brain Metabolism Reviews 2019, 40: 2254-2264. PMID: 31744389, PMCID: PMC7585925, DOI: 10.1177/0271678x19886316.Peer-Reviewed Original ResearchConceptsEffects of ketamineKetamine infusionGlutamate transmissionMetabotropic glutamate receptor 5Ketamine-induced effectsKetamine-induced changesGlutamate receptor 5Promising treatment targetDrug challenge studiesTwo-tissue compartment modelMGluR5 radioligandBlood pressureMGluR5 availabilityBaseline scanOutcome measuresHealthy subjectsHeart ratePsychiatric disordersReceptor 5Modulatory effectsMGluR5Treatment targetsChallenge studiesArterial input functionChallenge paradigm
2015
Measurement of Bmax and Kd with the Glycine Transporter 1 Radiotracer 18F-MK6577 using a Novel Multi-Infusion Paradigm
Xia Y, Zheng MQ, Holden D, Lin SF, Kapinos M, Ropchan J, Gallezot JD, Huang Y, Carson RE. Measurement of Bmax and Kd with the Glycine Transporter 1 Radiotracer 18F-MK6577 using a Novel Multi-Infusion Paradigm. Cerebrovascular And Brain Metabolism Reviews 2015, 35: 2001-2009. PMID: 26198176, PMCID: PMC4671121, DOI: 10.1038/jcbfm.2015.163.Peer-Reviewed Original ResearchConceptsGlycine transporter-1 inhibitorNew positron emission tomography radiotracerPositron emission tomography (PET) radiotracerPotential therapeutic agentNondisplaceable distribution volumeNMDA receptorsVivo affinityBaboon brainDistribution volumeBmax valuesTomography radiotracerTherapeutic agentsVivo KDBrainRank orderUnlabeled compoundsRadiotracerKdBrainstem11C-PBR28 imaging in multiple sclerosis patients and healthy controls: test-retest reproducibility and focal visualization of active white matter areas
Park E, Gallezot JD, Delgadillo A, Liu S, Planeta B, Lin SF, O’Connor K, Lim K, Lee JY, Chastre A, Chen MK, Seneca N, Leppert D, Huang Y, Carson RE, Pelletier D. 11C-PBR28 imaging in multiple sclerosis patients and healthy controls: test-retest reproducibility and focal visualization of active white matter areas. European Journal Of Nuclear Medicine And Molecular Imaging 2015, 42: 1081-1092. PMID: 25833352, DOI: 10.1007/s00259-015-3043-4.Peer-Reviewed Original ResearchConceptsNormal-appearing white matterVolume of distributionTest-retest variabilityWhole brain white matterHealthy controlsMicroglial activationTest-retest reproducibilityGray matterMultiple sclerosisMS subjectsWhite matterWhole brain gray matterGood test-retest reproducibilityAbsolute test-retest variabilityActive MS patientsPositron emission tomography (PET) ligandMultiple sclerosis patientsMain outcome measuresWhite matter areasMS WM lesionsBrain gray matterDemyelinating injuryTest-retest resultsVT valuesMS patientsPreclinical to Clinical Translation of CNS Transporter Occupancy of TD-9855, a Novel Norepinephrine and Serotonin Reuptake Inhibitor
Smith J, Patil D, Daniels O, Ding YS, Gallezot JD, Henry S, Kim K, Kshirsagar S, Martin W, Obedencio G, Stangeland E, Tsuruda P, Williams W, Carson R, Patil. Preclinical to Clinical Translation of CNS Transporter Occupancy of TD-9855, a Novel Norepinephrine and Serotonin Reuptake Inhibitor. The International Journal Of Neuropsychopharmacology 2015, 18: pyu027. PMID: 25522383, PMCID: PMC4368888, DOI: 10.1093/ijnp/pyu027.Peer-Reviewed Original ResearchMeSH KeywordsAdultAniline CompoundsAnimalsBlood Chemical AnalysisBrainHalf-LifeHumansMagnetic Resonance ImagingMaleModels, BiologicalMorpholinesNeurotransmitter Uptake InhibitorsNorepinephrine Plasma Membrane Transport ProteinsPhenyl EthersPiperidinesPositron-Emission TomographyRadiopharmaceuticalsRats, Sprague-DawleyReboxetineSerotonin Plasma Membrane Transport ProteinsSpinal CordSulfidesConceptsReuptake inhibitorsPositron emission tomographyNorepinephrine transporterSerotonin transporterSerotonin reuptake inhibitorsSingle oral doseUnique clinical profileMonoamine reuptake inhibitorsFuture clinical evaluationRat spinal cordNET occupancySERT occupancyClinical profileOral dosePlasma levelsTransporter profilesClinical evaluationSpinal cordTransporter occupancyCNS penetrationHealthy malesPharmacodynamic modelingNorepinephrineEmission tomographyPET studies
2013
Reductions in Brain 5-HT1B Receptor Availability in Primarily Cocaine-Dependent Humans
Matuskey D, Bhagwagar Z, Planeta B, Pittman B, Gallezot JD, Chen J, Wanyiri J, Najafzadeh S, Ropchan J, Geha P, Huang Y, Potenza MN, Neumeister A, Carson RE, Malison RT. Reductions in Brain 5-HT1B Receptor Availability in Primarily Cocaine-Dependent Humans. Biological Psychiatry 2013, 76: 816-822. PMID: 24433854, PMCID: PMC4037398, DOI: 10.1016/j.biopsych.2013.11.022.Peer-Reviewed Original ResearchMeSH KeywordsAdultBrainCarbon RadioisotopesCocaine-Related DisordersFemaleHumansMagnetic Resonance ImagingMalePositron-Emission TomographyReceptor, Serotonin, 5-HT1BConceptsRegional binding potentialPositron emission tomographyCocaine dependenceEmission tomographyFrontal cortexReceptor availabilityAge-matched healthy control subjectsSignificant gray matter reductionsYears of cocaineIllicit substance abuseHealthy control subjectsDaily tobacco useCocaine-dependent humansGray matter reductionsEffects of cocaineMagnetic resonance imagingSignificant reductionPreclinical evidenceControl subjectsPrimary addictionSerotonin receptorsHealthy subjectsTobacco useMedication developmentAnterior cingulateImaging Nicotine- and Amphetamine-Induced Dopamine Release in Rhesus Monkeys with [11C]PHNO vs [11C]raclopride PET
Gallezot JD, Kloczynski T, Weinzimmer D, Labaree D, Zheng MQ, Lim K, Rabiner EA, Ridler K, Pittman B, Huang Y, Carson RE, Morris ED, Cosgrove KP. Imaging Nicotine- and Amphetamine-Induced Dopamine Release in Rhesus Monkeys with [11C]PHNO vs [11C]raclopride PET. Neuropsychopharmacology 2013, 39: 866-874. PMID: 24220025, PMCID: PMC3924521, DOI: 10.1038/npp.2013.286.Peer-Reviewed Original ResearchConceptsAmphetamine-induced DA releaseD2/D3 receptorsDA releaseD3 receptorsRhesus monkeysAmphetamine-Induced Dopamine ReleaseDopamine D2/D3 receptorsHuman tobacco smokersAmphetamine-induced changesClinical neuroimaging studiesAdult rhesus monkeysPositron emission tomography (PET) imagingEmission Tomography ImagingLow-affinity receptorsNon-human primatesTobacco smokersSubstantia nigraGlobus pallidusDopamine releaseNucleus accumbensNicotineNeuroimaging studiesTomography imagingBPNDReceptorsThe neuroinflammation marker translocator protein is not elevated in individuals with mild-to-moderate depression: A [11C]PBR28 PET study
Hannestad J, DellaGioia N, Gallezot JD, Lim K, Nabulsi N, Esterlis I, Pittman B, Lee JY, O’Connor K, Pelletier D, Carson RE. The neuroinflammation marker translocator protein is not elevated in individuals with mild-to-moderate depression: A [11C]PBR28 PET study. Brain Behavior And Immunity 2013, 33: 131-138. PMID: 23850810, PMCID: PMC3899398, DOI: 10.1016/j.bbi.2013.06.010.Peer-Reviewed Original ResearchConceptsLevels of TSPOControl subjectsSystemic inflammationPositron emission tomographyModerate depressionTSPO levelsActivation of microgliaTranslocator protein 18Total ligand bindingAcute episodePrimary outcomePostmortem studiesSevere depressionMajor depressionPET scansTSPO genotypeBrain regionsEmission tomographySubject factorsPET studiesArterial input functionInflammationElevated levelsProtein 18Depression
2010
Clinically Relevant Doses of Methylphenidate Significantly Occupy Norepinephrine Transporters in Humans In Vivo
Hannestad J, Gallezot JD, Planeta-Wilson B, Lin SF, Williams WA, van Dyck CH, Malison RT, Carson RE, Ding YS. Clinically Relevant Doses of Methylphenidate Significantly Occupy Norepinephrine Transporters in Humans In Vivo. Biological Psychiatry 2010, 68: 854-860. PMID: 20691429, PMCID: PMC3742016, DOI: 10.1016/j.biopsych.2010.06.017.Peer-Reviewed Original ResearchConceptsAttention-deficit/hyperactivity disorderNET-rich regionsPositron emission tomographyNorepinephrine transporterDopamine transporterHyperactivity disorderRelevant dosesEmission tomographySingle-blind placeboMultilinear reference tissue modelEffective dose 50Attention deficit hyperactivity disorderDose-dependent mannerMechanism of actionDeficit hyperactivity disorderBrain norepinephrine transportersReference tissue modelMaintenance doseOral methylphenidateHealthy subjectsTherapeutic effectOccipital cortexCommon treatmentPsychiatric disordersMethylphenidate
2009
Kinetic Modeling of the Serotonin 5-HT1B Receptor Radioligand [11C]P943 in Humans
Gallezot JD, Nabulsi N, Neumeister A, Planeta-Wilson B, Williams WA, Singhal T, Kim S, Maguire RP, McCarthy T, Frost JJ, Huang Y, Ding YS, Carson RE. Kinetic Modeling of the Serotonin 5-HT1B Receptor Radioligand [11C]P943 in Humans. Cerebrovascular And Brain Metabolism Reviews 2009, 30: 196-210. PMID: 19773803, PMCID: PMC2949107, DOI: 10.1038/jcbfm.2009.195.Peer-Reviewed Original ResearchMeSH KeywordsBrainChromatography, High Pressure LiquidElectron Spin Resonance SpectroscopyHumansImage Processing, Computer-AssistedIsotope LabelingLinear ModelsMagnetic Resonance ImagingMental DisordersModels, StatisticalPiperazinesPositron-Emission TomographyPyrrolidinonesRadiopharmaceuticalsReceptor, Serotonin, 5-HT1B