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 regionsPreclinical Evaluation of 18F-PF-05270430, a Novel PET Radioligand for the Phosphodiesterase 2A Enzyme
Chen L, Nabulsi N, Naganawa M, Zasadny K, Skaddan MB, Zhang L, Najafzadeh S, Lin SF, Helal CJ, Boyden TL, Chang C, Ropchan J, Carson RE, Villalobos A, Huang Y. Preclinical Evaluation of 18F-PF-05270430, a Novel PET Radioligand for the Phosphodiesterase 2A Enzyme. Journal Of Nuclear Medicine 2016, 57: 1448-1453. PMID: 27199356, PMCID: PMC5093921, DOI: 10.2967/jnumed.115.171454.Peer-Reviewed Original ResearchAnimalsAzabicyclo CompoundsAzetidinesBrainCyclic Nucleotide Phosphodiesterases, Type 2Macaca mulattaMaleMetabolic Clearance RateMolecular ImagingOrgan SpecificityPositron-Emission TomographyRadiopharmaceuticalsRatsRats, Sprague-DawleyReproducibility of ResultsSensitivity and SpecificitySpecies SpecificityTissue DistributionFirst-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
2013
Determination of the In Vivo Selectivity of a New κ-Opioid Receptor Antagonist PET Tracer 11C-LY2795050 in the Rhesus Monkey
Kim SJ, Zheng MQ, Nabulsi N, Labaree D, Ropchan J, Najafzadeh S, Carson RE, Huang Y, Morris ED. Determination of the In Vivo Selectivity of a New κ-Opioid Receptor Antagonist PET Tracer 11C-LY2795050 in the Rhesus Monkey. Journal Of Nuclear Medicine 2013, 54: 1668-1674. PMID: 23918735, PMCID: PMC5824998, DOI: 10.2967/jnumed.112.118877.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBenzamidesBrainComputer SimulationImage Interpretation, Computer-AssistedMacaca mulattaMetabolic Clearance RateModels, BiologicalPositron-Emission TomographyPyrrolidinesRadiopharmaceuticalsReceptors, Opioid, kappaReproducibility of ResultsSensitivity and SpecificityTissue Distribution
2011
Assessing the sensitivity of [11C]p943, a novel 5‐HTIB radioligand, to endogenous serotonin release
Cosgrove KP, Kloczynski T, Nabulsi N, Weinzimmer D, Lin S, Staley JK, Bhagwagar Z, Carson RE. Assessing the sensitivity of [11C]p943, a novel 5‐HTIB radioligand, to endogenous serotonin release. Synapse 2011, 65: 1113-1117. PMID: 21484884, PMCID: PMC3149753, DOI: 10.1002/syn.20942.Peer-Reviewed Original ResearchConceptsFenfluramine-induced changesReceptor occupancyDoses of fenfluraminePositron emission tomography radioligandEndogenous serotonin releaseNonhuman primate brainSerotonin releaseLow doseHigh doseTomography radioligandPrimate brainRhesus monkeysFenfluramineRhesus macaquesPET imagingHuman brainBaboonsDoseDosesRadioligandBrainCurrent studyReceptors