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
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