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 regionsFirst-in-Human Assessment of the Novel PDE2A PET Radiotracer 18F-PF-05270430
Naganawa M, Waterhouse RN, Nabulsi N, Lin SF, Labaree D, Ropchan J, Tarabar S, DeMartinis N, Ogden A, Banerjee A, Huang Y, Carson RE. First-in-Human Assessment of the Novel PDE2A PET Radiotracer 18F-PF-05270430. Journal Of Nuclear Medicine 2016, 57: 1388-1395. PMID: 27103022, PMCID: PMC5093918, DOI: 10.2967/jnumed.115.166850.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsAzabicyclo CompoundsAzetidinesBrainComputer SimulationCyclic Nucleotide Phosphodiesterases, Type 2Feasibility StudiesFemaleHumansIsotope LabelingMacaca mulattaMaleMetabolic Clearance RateModels, BiologicalMolecular ImagingOrgan SpecificityPilot ProjectsPositron-Emission TomographyRadiopharmaceuticalsReproducibility of ResultsSensitivity and SpecificityTissue DistributionConceptsTest-retest variabilityHuman studiesPET ligandWhite matterNeocortical regionsMultilinear analysis 1MSv/MBqHealthy male subjectsDetectable pharmacologic effectsAppropriate tracer kinetic modelsTest-retest protocolAdverse eventsBrain uptakePharmacologic effectsRegional time-activity curvesTarget doseTime-activity curvesTracer uptakeMale subjectsWhole brainBrain regionsEffective doseCritical organsPET radiotracersNonhuman primatesIn vivo variation in same-day estimates of metabotropic glutamate receptor subtype 5 binding using [11C]ABP688 and [18F]FPEB
DeLorenzo C, Gallezot JD, Gardus J, Yang J, Planeta B, Nabulsi N, Ogden RT, Labaree DC, Huang YH, Mann JJ, Gasparini F, Lin X, Javitch JA, Parsey RV, Carson RE, Esterlis I. In vivo variation in same-day estimates of metabotropic glutamate receptor subtype 5 binding using [11C]ABP688 and [18F]FPEB. Cerebrovascular And Brain Metabolism Reviews 2016, 37: 2716-2727. PMID: 27742888, PMCID: PMC5536783, DOI: 10.1177/0271678x16673646.Peer-Reviewed Original ResearchConceptsMetabotropic glutamate receptor subtype 5Test-retest studySubtype 5Absolute test-retest variabilityBrain glutamatergic systemSame dayPositron emission tomography (PET) tracerTest-retest variabilityEmission tomography tracerGlutamatergic systemLarge cohortSmall cohortStudy designTomography tracerMGluR5ScansCohortVivo variationsDaysReplication studyBinding increasesResidual radioactivitySubjectsBinding differences
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
Evaluation 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
2000
Measurement of dopamine release with continuous infusion of [11C]raclopride: optimization and signal-to-noise considerations.
Watabe H, Endres CJ, Breier A, Schmall B, Eckelman WC, Carson RE. Measurement of dopamine release with continuous infusion of [11C]raclopride: optimization and signal-to-noise considerations. Journal Of Nuclear Medicine 2000, 41: 522-30. PMID: 10716328.Peer-Reviewed Original ResearchConceptsOptimal timingAdministration of amphetamineReceptor imaging studiesHuman dataContinuous infusionDopamine releaseOptimal scan timeHealthy volunteersHuman studiesSynaptic dopamineImaging studiesPET studiesDopamine responsePercentage changeCareful assessmentStatistical significanceDeltaBPInfusionMeasurement of changesIndirect measureActivity curvesPrePatients
1999
Bolus Injection Versus Slow Infusion of [15O]Water for Positron Emission Tomography Activation Studies
Beason-Held L, Desmond R, Herscovitch P, Carson R. Bolus Injection Versus Slow Infusion of [15O]Water for Positron Emission Tomography Activation Studies. Cerebrovascular And Brain Metabolism Reviews 1999, 19: 843-852. PMID: 10458591, DOI: 10.1097/00004647-199908000-00003.Peer-Reviewed Original ResearchAdultBrainBrain MappingCerebrovascular CirculationFaceFemaleHumansImage Processing, Computer-AssistedInfusions, IntravenousInjections, IntravenousMemory, Short-TermModels, CardiovascularModels, NeurologicalOxygen RadioisotopesPattern Recognition, VisualReference ValuesRegional Blood FlowSensitivity and SpecificityTomography, Emission-ComputedWater
1998
Assessment of Dynamic Neurotransmitter Changes With Bolus or Infusion Delivery of Neuroreceptor Ligands
Endres C, Carson R. Assessment of Dynamic Neurotransmitter Changes With Bolus or Infusion Delivery of Neuroreceptor Ligands. Cerebrovascular And Brain Metabolism Reviews 1998, 18: 1196-1210. PMID: 9809509, DOI: 10.1097/00004647-199811000-00006.Peer-Reviewed Original ResearchBrainCarbon RadioisotopesComputer SimulationDopamineDopamine AntagonistsFlumazenilHumansInfusions, ParenteralInjectionsKineticsMicrodialysisModels, NeurologicalNaltrexoneNarcotic AntagonistsRacloprideRadioligand AssayReceptors, DopamineSalicylamidesSensitivity and SpecificityTomography, Emission-Computed