2016
First-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 primates
2015
Imaging robust microglial activation after lipopolysaccharide administration in humans with PET
Sandiego CM, Gallezot JD, Pittman B, Nabulsi N, Lim K, Lin SF, Matuskey D, Lee JY, O’Connor K, Huang Y, Carson RE, Hannestad J, Cosgrove KP. Imaging robust microglial activation after lipopolysaccharide administration in humans with PET. Proceedings Of The National Academy Of Sciences Of The United States Of America 2015, 112: 12468-12473. PMID: 26385967, PMCID: PMC4603509, DOI: 10.1073/pnas.1511003112.Peer-Reviewed Original ResearchConceptsMicroglial activationBrain microglial activationLPS administrationInflammatory cytokinesLPS challengeRobust microglial activationSystemic LPS challengeActivation of microgliaInnate immune cellsVital sign changesHealthy male subjectsEscherichia coli lipopolysaccharidePositron emission tomography (PET) radiotracerNeuroinflammatory responseSystemic inflammationLipopolysaccharide administrationAntiinflammatory effectsBlood levelsImmune cellsNew medicationsSystemic administrationColi lipopolysaccharidePET scansPsychiatric diseasesMale subjectsTest–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