2022
Neurotransmitter transporter occupancy following administration of centanafadine sustained-release tablets: A phase 1 study in healthy male adults
Matuskey D, Gallezot J, Nabulsi N, Henry S, Torres K, Dias M, Angarita G, Huang Y, Shoaf S, Carson R, Mehrotra S. Neurotransmitter transporter occupancy following administration of centanafadine sustained-release tablets: A phase 1 study in healthy male adults. Journal Of Psychopharmacology 2022, 37: 164-171. PMID: 36515395, PMCID: PMC9912308, DOI: 10.1177/02698811221140008.Peer-Reviewed Original ResearchAdultBrainDelayed-Action PreparationsDopamine Plasma Membrane Transport ProteinsHumansMaleNorepinephrine Plasma Membrane Transport ProteinsPositron-Emission TomographySerotoninSerotonin Plasma Membrane Transport ProteinsTablets
2019
Norepinephrine transporter availability in brown fat is reduced in obesity: a human PET study with [11C] MRB
Sanchez-Rangel E, Gallezot JD, Yeckel CW, Lam W, Belfort-DeAguiar R, Chen MK, Carson RE, Sherwin R, Hwang JJ. Norepinephrine transporter availability in brown fat is reduced in obesity: a human PET study with [11C] MRB. International Journal Of Obesity 2019, 44: 964-967. PMID: 31636373, PMCID: PMC7259982, DOI: 10.1038/s41366-019-0471-4.Peer-Reviewed Original ResearchMeSH KeywordsAdipose Tissue, BrownAdultCarbon RadioisotopesFemaleHumansNorepinephrine Plasma Membrane Transport ProteinsObesityPositron Emission Tomography Computed TomographyReboxetineYoung AdultConceptsBrown adipose tissueDetectable brown adipose tissueDistribution volume ratioMultilinear reference tissue model 2Norepinephrine transporterSympathetic innervationNorepinephrine transporter availabilityHuman brown adipose tissueDense sympathetic innervationPET-CT imagingReference tissue model 2Human PET studiesSupraclavicular regionCaucasian womenTransporter availabilityOccipital cortexObesityTherapeutic targetAdipose tissueBrown fatPET studiesWomenInnervationSelective ligandsEnergy-dissipating properties
2015
Imaging human brown adipose tissue under room temperature conditions with 11C-MRB, a selective norepinephrine transporter PET ligand
Hwang JJ, Yeckel CW, Gallezot JD, Aguiar RB, Ersahin D, Gao H, Kapinos M, Nabulsi N, Huang Y, Cheng D, Carson RE, Sherwin R, Ding YS. Imaging human brown adipose tissue under room temperature conditions with 11C-MRB, a selective norepinephrine transporter PET ligand. Metabolism 2015, 64: 747-755. PMID: 25798999, PMCID: PMC4408242, DOI: 10.1016/j.metabol.2015.03.001.Peer-Reviewed Original ResearchMeSH KeywordsAdipose Tissue, BrownAdultBody TemperatureFemaleFluorodeoxyglucose F18HumansImage Interpretation, Computer-AssistedMaleMorpholinesNorepinephrine Plasma Membrane Transport ProteinsPositron-Emission TomographyRadiopharmaceuticalsReboxetineSex CharacteristicsTemperatureYoung AdultConceptsBrown adipose tissueDistribution volume ratioSympathetic nervous systemAdipose tissueRole of BATCold stimulationFDG PET-CT imagingNorepinephrine transporterSupraclavicular brown adipose tissueHuman brown adipose tissueTotal body fatLean body massCold-stimulated conditionsBody temperaturePET-CT imagingBioelectrical impedance analysisCore body temperatureFDG uptakePET-CTOccipital cortexBody fatNervous systemBody compositionPET ligandBasal statePreclinical 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
Decreased norepinephrine transporter availability in obesity: Positron Emission Tomography imaging with (S,S)-[11C]O-methylreboxetine
Li CS, Potenza MN, Lee DE, Planeta B, Gallezot JD, Labaree D, Henry S, Nabulsi N, Sinha R, Ding YS, Carson RE, Neumeister A. Decreased norepinephrine transporter availability in obesity: Positron Emission Tomography imaging with (S,S)-[11C]O-methylreboxetine. NeuroImage 2013, 86: 306-310. PMID: 24121204, PMCID: PMC3947246, DOI: 10.1016/j.neuroimage.2013.10.004.Peer-Reviewed Original ResearchMeSH KeywordsAdultBiological AvailabilityCarbon RadioisotopesFemaleHumansMaleMorpholinesNorepinephrineNorepinephrine Plasma Membrane Transport ProteinsObesityPositron-Emission TomographyRadiopharmaceuticalsReboxetineThalamusTissue DistributionConceptsBody mass indexMultilinear reference tissue model 2Norepinephrine transporterNoradrenergic dysfunctionObese individualsLean individualsStructural MR scansBPND valuesNorepinephrine transporter availabilityReference tissue model 2Positron emission tomography (PET) imagingEmission Tomography ImagingPositron emission tomographyBrain norepinephrine transportersNE clearanceMass indexRaphe nucleusLocus coeruleusSynaptic availabilityObese peopleTransporter availabilityOccipital cortexComparison subjectsHealthy individualsObesityClinical doses of atomoxetine significantly occupy both norepinephrine and serotonin transports: Implications on treatment of depression and ADHD
Ding YS, Naganawa M, Gallezot JD, Nabulsi N, Lin SF, Ropchan J, Weinzimmer D, McCarthy TJ, Carson RE, Huang Y, Laruelle M. Clinical doses of atomoxetine significantly occupy both norepinephrine and serotonin transports: Implications on treatment of depression and ADHD. NeuroImage 2013, 86: 164-171. PMID: 23933039, DOI: 10.1016/j.neuroimage.2013.08.001.Peer-Reviewed Original ResearchMeSH KeywordsAdrenergic Uptake InhibitorsAnimalsAtomoxetine HydrochlorideAttention Deficit Disorder with HyperactivityBrainDepressionDose-Response Relationship, DrugMacaca mulattaNorepinephrine Plasma Membrane Transport ProteinsPositron-Emission TomographyPropylaminesSerotonin Plasma Membrane Transport ProteinsTissue DistributionConceptsTreatment of depressionNorepinephrine transporterComparative PET imaging studyMetabolite-corrected arterial input functionFinal infusion rateDoses of atomoxetineDose-dependent occupancyPET imaging studiesSelective serotonin transporter (SERT) ligandNon-human primatesPlasma levelsSelective blockadeSaline infusionClinical dosesTherapeutic effectInfusion rateRelevant dosePET scansAtomoxetineRelevant dosesSerotonin transporter ligandDistribution volumeImaging studiesRhesus monkeysArterial input function
2012
Ex Vivo and In Vivo Evaluation of the Norepinephrine Transporter Ligand [11C]MRB for Brown Adipose Tissue Imaging
Lin SF, Fan X, Yeckel CW, Weinzimmer D, Mulnix T, Gallezot JD, Carson RE, Sherwin RS, Ding YS. Ex Vivo and In Vivo Evaluation of the Norepinephrine Transporter Ligand [11C]MRB for Brown Adipose Tissue Imaging. Nuclear Medicine And Biology 2012, 39: 1081-1086. PMID: 22595487, PMCID: PMC4067762, DOI: 10.1016/j.nucmedbio.2012.04.005.Peer-Reviewed Original ResearchMeSH KeywordsAdipose Tissue, BrownAnimalsFluoxetineLigandsMaleMorpholinesNorepinephrine Plasma Membrane Transport ProteinsPositron-Emission TomographyRatsRats, Sprague-DawleyReboxetineWakefulness
2010
Evaluation of [11C]MRB for assessment of occupancy of norepinephrine transporters: Studies with atomoxetine in non-human primates
Gallezot JD, Weinzimmer D, Nabulsi N, Lin SF, Fowles K, Sandiego C, McCarthy TJ, Maguire RP, Carson RE, Ding YS. Evaluation of [11C]MRB for assessment of occupancy of norepinephrine transporters: Studies with atomoxetine in non-human primates. NeuroImage 2010, 56: 268-279. PMID: 20869448, PMCID: PMC3710586, DOI: 10.1016/j.neuroimage.2010.09.040.Peer-Reviewed Original ResearchMeSH KeywordsAdrenergic Uptake InhibitorsAnimalsAtomoxetine HydrochlorideBrainCarbon RadioisotopesMacaca mulattaNorepinephrine Plasma Membrane Transport ProteinsPositron-Emission TomographyPropylaminesRadiopharmaceuticalsTissue DistributionConceptsAttention deficit hyperactivity disorderPositron emission tomographyNorepinephrine transporterDrug occupancy studiesRhesus monkeysReference regionTreatment of depressionDose-dependent reductionVolume of distributionArterial blood samplingSuitable reference regionOccupancy studiesNon-human primatesBrain norepinephrine transportersPromising radioligandPlasma levelsTherapeutic doseOccipital cortexBlood samplingUptake inhibitorAtomoxetineEmission tomographyEffective dosePET studiesArterial input functionClinically 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 ResearchMeSH KeywordsAdultBrainCentral Nervous System StimulantsDose-Response Relationship, DrugFemaleHumansMagnetic Resonance ImagingMaleMethylphenidateMorpholinesNorepinephrine Plasma Membrane Transport ProteinsPositron-Emission TomographyRadioligand AssayReboxetineConceptsAttention-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
PET imaging of the effects of age and cocaine on the norepinephrine transporter in the human brain using (S,S)‐[11C]O‐methylreboxetine and HRRT
Ding Y, Singhal T, Planeta‐Wilson B, Gallezot J, Nabulsi N, Labaree D, Ropchan J, Henry S, Williams W, Carson RE, Neumeister A, Malison RT. PET imaging of the effects of age and cocaine on the norepinephrine transporter in the human brain using (S,S)‐[11C]O‐methylreboxetine and HRRT. Synapse 2009, 64: 30-38. PMID: 19728366, PMCID: PMC3727644, DOI: 10.1002/syn.20696.Peer-Reviewed Original ResearchMeSH KeywordsAdultAgingBrainCocaineCocaine-Related DisordersDopamine Uptake InhibitorsFemaleHumansImage Processing, Computer-AssistedMaleMiddle AgedMorpholinesNorepinephrine Plasma Membrane Transport ProteinsPositron-Emission TomographyRadiopharmaceuticalsReboxetine