2019
Imaging the Enzyme 11β-Hydroxysteroid Dehydrogenase Type 1 with PET: Evaluation of the Novel Radiotracer 11C-AS2471907 in Human Brain
Gallezot JD, Nabulsi N, Henry S, Pracitto R, Planeta B, Ropchan J, Lin SF, Labaree D, Kapinos M, Shirali A, Lara-Jaime T, Gao H, Matuskey D, Walzer M, Marek GJ, Bellaire S, Yuan N, Carson RE, Huang Y. Imaging the Enzyme 11β-Hydroxysteroid Dehydrogenase Type 1 with PET: Evaluation of the Novel Radiotracer 11C-AS2471907 in Human Brain. Journal Of Nuclear Medicine 2019, 60: 1140-1146. PMID: 30877174, DOI: 10.2967/jnumed.118.219766.Peer-Reviewed Original ResearchConceptsTest-retest variabilityNondisplaceable distribution volumeOccipital cortexEnzyme 11β-hydroxysteroid dehydrogenase type 1White matterDistribution volumeTreatment of depressionDehydrogenase type 1Large cortical regionsPosttraumatic stress disorderHuman brainAdditional scansIntraclass correlation coefficientAge-related cognitive functionBolus administrationFrontal cortexCaudate nucleusAdipose tissueTime-activity curvesNovel radiotracersGlucocorticoid levelsParietal cortexCortical regionsPattern of uptakeType 1
2017
Evaluation of the Lysophosphatidic Acid Receptor Type 1 Radioligand 11C-BMT-136088 for Lung Imaging in Rhesus Monkeys
Gallezot JD, Nabulsi NB, Holden D, Lin SF, Labaree D, Ropchan J, Najafzadeh S, Donnelly DJ, Cao K, Bonacorsi S, Seiders J, Roppe J, Hayes W, Huang Y, Du S, Carson RE. Evaluation of the Lysophosphatidic Acid Receptor Type 1 Radioligand 11C-BMT-136088 for Lung Imaging in Rhesus Monkeys. Journal Of Nuclear Medicine 2017, 59: 327-333. PMID: 28864634, DOI: 10.2967/jnumed.117.195073.Peer-Reviewed Original ResearchConceptsMultilinear analysis 1Rhesus monkeysHighest organ doseLung tissue injuryLung regionsΜSv/MBqPlasma free fractionReceptor type 1Test-retest scansTest-retest variabilityVivo dissociationMolecule lysophosphatidic acidRight lung regionsML of plasmaNondisplaceable volumePulmonary fibrosisLung fibrosisVascular leakageInfusion protocolPlasma concentrationsTissue injuryDrug doseNormal healingOrgan doseType 1Kinetic evaluation and test–retest reproducibility of [11C]UCB-J, a novel radioligand for positron emission tomography imaging of synaptic vesicle glycoprotein 2A in humans
Finnema SJ, Nabulsi NB, Mercier J, Lin SF, Chen MK, Matuskey D, Gallezot JD, Henry S, Hannestad J, Huang Y, Carson RE. Kinetic evaluation and test–retest reproducibility of [11C]UCB-J, a novel radioligand for positron emission tomography imaging of synaptic vesicle glycoprotein 2A in humans. Cerebrovascular And Brain Metabolism Reviews 2017, 38: 2041-2052. PMID: 28792356, PMCID: PMC6259313, DOI: 10.1177/0271678x17724947.Peer-Reviewed Original Research
2016
Imaging of cerebral α4β2* nicotinic acetylcholine receptors with (−)-[18F]Flubatine PET: Implementation of bolus plus constant infusion and sensitivity to acetylcholine in human brain
Hillmer AT, Esterlis I, Gallezot JD, Bois F, Zheng MQ, Nabulsi N, Lin SF, Papke RL, Huang Y, Sabri O, Carson RE, Cosgrove KP. Imaging of cerebral α4β2* nicotinic acetylcholine receptors with (−)-[18F]Flubatine PET: Implementation of bolus plus constant infusion and sensitivity to acetylcholine in human brain. NeuroImage 2016, 141: 71-80. PMID: 27426839, PMCID: PMC5026941, DOI: 10.1016/j.neuroimage.2016.07.026.Peer-Reviewed Original ResearchMeSH KeywordsAcetylcholineAdultBenzamidesBrainBridged Bicyclo Compounds, HeterocyclicComputer SimulationHumansImage Interpretation, Computer-AssistedInfusions, IntraventricularMetabolic Clearance RateMiddle AgedModels, NeurologicalMolecular ImagingNeurotransmitter AgentsPositron-Emission TomographyRadiopharmaceuticalsReceptors, NicotinicReproducibility of ResultsSensitivity and SpecificityTissue DistributionYoung AdultConceptsGray matter regionsQuantitative Analysis of Dynamic 123I-mIBG SPECT Imaging Data in Healthy Humans with a Population-Based Metabolite Correction Method
Wu J, Lin SF, Gallezot JD, Chan C, Prasad R, Thorn S, Stacy MR, Huang Y, Zonouz TH, Liu YH, Lampert RJ, Carson RE, Sinusas AJ, Liu C. Quantitative Analysis of Dynamic 123I-mIBG SPECT Imaging Data in Healthy Humans with a Population-Based Metabolite Correction Method. Journal Of Nuclear Medicine 2016, 57: 1226-1232. PMID: 27081169, DOI: 10.2967/jnumed.115.171710.Peer-Reviewed Original Research3-IodobenzylguanidineAdultAgedAlgorithmsArtifactsComputer SimulationFemaleHeartHumansImage EnhancementImage Interpretation, Computer-AssistedMaleMiddle AgedModels, CardiovascularModels, StatisticalMyocardiumRadiopharmaceuticalsReproducibility of ResultsSensitivity and SpecificityTissue DistributionTomography, Emission-Computed, Single-Photon
2015
Test–retest reproducibility of the metabotropic glutamate receptor 5 ligand [18F]FPEB with bolus plus constant infusion in humans
Park E, Sullivan JM, Planeta B, Gallezot JD, Lim K, Lin SF, Ropchan J, McCarthy TJ, Ding YS, Morris ED, Williams WA, Huang Y, Carson RE. Test–retest reproducibility of the metabotropic glutamate receptor 5 ligand [18F]FPEB with bolus plus constant infusion in humans. European Journal Of Nuclear Medicine And Molecular Imaging 2015, 42: 1530-1541. PMID: 26044120, PMCID: PMC5467218, DOI: 10.1007/s00259-015-3094-6.Peer-Reviewed Original ResearchConceptsVolume of distributionAbsolute test-retest variabilityCerebellar white matterTest-retest reproducibilityMetabotropic glutamate receptor 5Venous blood measurementsGlutamate receptor 5Healthy male subjectsPromising PET radioligandArterial blood concentrationPET imaging tracerTest-retest variabilityTwo-tissue compartment modelRegional BPNDVenous bloodBlood concentrationsArterial bloodReceptor 5Constant infusionMale subjectsWhite matterBlood measurementsGray matterNeuropsychiatric diseasesPET radioligand
2014
Further evaluation of [11C]MP‐10 as a radiotracer for phosphodiesterase 10A: PET imaging study in rhesus monkeys and brain tissue metabolite analysis
Lin S, Labaree D, Chen M, Holden D, Gallezot J, Kapinos M, Teng J, Najafzadeh S, Plisson C, Rabiner EA, Gunn RN, Carson RE, Huang Y. Further evaluation of [11C]MP‐10 as a radiotracer for phosphodiesterase 10A: PET imaging study in rhesus monkeys and brain tissue metabolite analysis. Synapse 2014, 69: 86-95. PMID: 25450608, PMCID: PMC4275380, DOI: 10.1002/syn.21792.Peer-Reviewed Original ResearchConceptsRhesus monkeysPhosphodiesterase 10ASprague-Dawley ratsMP-10Dose-dependent mannerSpecific PET tracersHigh specific bindingPET imaging studiesTissue uptake kineticsBaseline scanBrain regionsImaging studiesFurther evaluationMultilinear analysis methodRegional volumesPET tracersNonhuman primatesPET imagingVivo studiesReference tissueMonkeysBrainCerebellumSpecific bindingPresent studyTest–retest reliability of the novel 5-HT1B receptor PET radioligand [11C]P943
Saricicek A, Chen J, Planeta B, Ruf B, Subramanyam K, Maloney K, Matuskey D, Labaree D, Deserno L, Neumeister A, Krystal JH, Gallezot JD, Huang Y, Carson RE, Bhagwagar Z. Test–retest reliability of the novel 5-HT1B receptor PET radioligand [11C]P943. European Journal Of Nuclear Medicine And Molecular Imaging 2014, 42: 468-477. PMID: 25427881, DOI: 10.1007/s00259-014-2958-5.Peer-Reviewed Original ResearchEvaluation of [18F]-(-)-norchlorofluorohomoepibatidine ([18F]-(-)-NCFHEB) as a PET radioligand to image the nicotinic acetylcholine receptors in non-human primates
Bois F, Gallezot JD, Zheng MQ, Lin SF, Esterlis I, Cosgrove KP, Carson RE, Huang Y. Evaluation of [18F]-(-)-norchlorofluorohomoepibatidine ([18F]-(-)-NCFHEB) as a PET radioligand to image the nicotinic acetylcholine receptors in non-human primates. Nuclear Medicine And Biology 2014, 42: 570-577. PMID: 25858513, PMCID: PMC4441617, DOI: 10.1016/j.nucmedbio.2014.08.003.Peer-Reviewed Original ResearchConceptsRhesus monkeysGood test-retest reproducibilityML/Plasma free fractionReceptor binding profileNicotinic acetylcholine receptorsTest-retest reproducibilityNon-human primatesReceptor radiotracerΑ4β2 receptorsFrontal cortexPET examinationsMonkey brainAcetylcholine receptorsBrain regionsDistribution volumePET radioligandMultilinear analysis methodPharmacokinetic propertiesEnd of synthesisNon-displaceable distribution volumeFree fractionPET measurementsMonkeysEvaluation of the sensitivity of the novel α4β2* nicotinic acetylcholine receptor PET radioligand 18F‐(‐)‐NCFHEB to increases in synaptic acetylcholine levels in rhesus monkeys
Gallezot J, Esterlis I, Bois F, Zheng M, Lin S, Kloczynski T, Krystal JH, Huang Y, Sabri O, Carson RE, Cosgrove KP. Evaluation of the sensitivity of the novel α4β2* nicotinic acetylcholine receptor PET radioligand 18F‐(‐)‐NCFHEB to increases in synaptic acetylcholine levels in rhesus monkeys. Synapse 2014, 68: 556-564. PMID: 25043426, PMCID: PMC4224280, DOI: 10.1002/syn.21767.Peer-Reviewed Original ResearchConceptsSynaptic acetylcholine concentrationPositron emission tomographyAcetylcholine concentrationRhesus monkeysInfusion of physostigmineSynaptic acetylcholine levelsDose-dependent reductionNicotinic acetylcholine receptorsAcetylcholine levelsBolus injectionAcetylcholine receptorsAcetylcholine dynamicsNew radioligandEmission tomographyArterial input functionAcetylcholinesterase inhibitorsRadioligandThalamusPhysostigmineDonepezilΑ4β2Promising tracerBaselineMonkeysShort scan duration
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 ResearchConceptsBody 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
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 ResearchConceptsAttention 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 function
2005
In vivo imaging of human cerebral nicotinic acetylcholine receptors with 2-18F-fluoro-A-85380 and PET.
Gallezot JD, Bottlaender M, Grégoire MC, Roumenov D, Deverre JR, Coulon C, Ottaviani M, Dollé F, Syrota A, Valette H. In vivo imaging of human cerebral nicotinic acetylcholine receptors with 2-18F-fluoro-A-85380 and PET. Journal Of Nuclear Medicine 2005, 46: 240-7. PMID: 15695782.Peer-Reviewed Original ResearchConceptsNicotinic acetylcholine receptorsLogan graphical analysisPET scansTime-activity curvesAcetylcholine receptorsStudy durationCerebral nicotinic acetylcholine receptorsDistribution of nAChRsVolume of distributionDynamic PET scansHuman brainIntravenous injectionFrontal cortexOccipital cortexHuman volunteersPET radioligandCompartment modelCompartmental kinetic analysisLogan analysisVolume of interest