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
2007
Mapping of human cerebral sigma1 receptors using positron emission tomography and [11C]SA4503
Sakata M, Kimura Y, Naganawa M, Oda K, Ishii K, Chihara K, Ishiwata K. Mapping of human cerebral sigma1 receptors using positron emission tomography and [11C]SA4503. NeuroImage 2007, 35: 1-8. PMID: 17240168, DOI: 10.1016/j.neuroimage.2006.11.055.Peer-Reviewed Original ResearchMeSH KeywordsAdultBiotransformationBrainBrain ChemistryBrain MappingChromatography, High Pressure LiquidData Interpretation, StatisticalDopamine AntagonistsHaloperidolHumansImage Processing, Computer-AssistedMaleNonlinear DynamicsPiperazinesPositron-Emission TomographyRadioligand AssayRadiopharmaceuticalsReceptors, sigmaConceptsTotal distribution volumePositron emission tomographyEmission tomographyMetabolite correctionHealthy male subjectsSigma receptor antagonistLogan plotHuman brainPlasma input functionReceptor antagonistOral administrationClinical studiesPET scansThree-compartment modelPartial blockadePsychiatric diseasesMale subjectsSigma1RSigma1 receptorsBaseline measurementsDistribution volumeTwo-tissueHaloperidolBrainReceptors
2006
A feasibility study of [11C]SA4503-PET for evaluating sigma1 receptor occupancy by neuroleptics: The binding of haloperidol to sigma1 and dopamine D2-like receptors
Ishiwata K, Oda K, Sakata M, Kimura Y, Kawamura K, Oda K, Sasaki T, Naganawa M, Chihara K, Okubo Y, Ishii K. A feasibility study of [11C]SA4503-PET for evaluating sigma1 receptor occupancy by neuroleptics: The binding of haloperidol to sigma1 and dopamine D2-like receptors. Annals Of Nuclear Medicine 2006, 20: 569-573. PMID: 17134027, DOI: 10.1007/bf03026824.Peer-Reviewed Original ResearchConceptsReceptor occupancy ratesPositron emission tomographyDopamine D2-like receptorsD2-like receptorsHealthy male subjectsNon-selective antagonistPET scansReceptor occupancyHaloperidolMale subjectsBaseline measurementsPeroral administrationEmission tomographyBinding of haloperidolNeurolepticsAdministrationReceptorsPutamenCaudateDrugsDaysOccupancy rateAntagonistFeasibility study