2019
Novel Kappa Opioid Receptor Agonist as Improved PET Radiotracer: Development and in Vivo Evaluation
Li S, Zheng M, Naganawa M, Gao H, Pracitto R, Shirali A, Lin SF, Teng JK, Ropchan J, Huang Y. Novel Kappa Opioid Receptor Agonist as Improved PET Radiotracer: Development and in Vivo Evaluation. Molecular Pharmaceutics 2019, 16: 1523-1531. PMID: 30726092, DOI: 10.1021/acs.molpharmaceut.8b01209.Peer-Reviewed Original ResearchConceptsKappa-opioid receptorsAgonist radiotracerOpioid receptorsNovel kappa-opioid receptor agonistKappa-opioid receptor agonistFast tissue kineticsNonselective opioid receptorTissue kineticsOpioid receptor agonistsDose-dependent mannerMultilinear analysis-1 (MA1) methodHigh specific bindingSpecific bindingAgonist tracersHigh binding regionsReceptor agonistRegional time-activity curvesSpecific binding signalsTime-activity curvesArterial activityImproved imaging propertiesRhesus monkeysDrug abusePET radiotracersParent fraction
2016
Preclinical 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 primates
2013
Clinical doses of atomoxetine significantly occupy both norepinephrine and serotonin transports: Implications on treatment of depression and ADHD
Ding YS, Naganawa M, Gallezot JD, Nabulsi N, Lin SF, Ropchan J, Weinzimmer D, McCarthy TJ, Carson RE, Huang Y, Laruelle M. Clinical doses of atomoxetine significantly occupy both norepinephrine and serotonin transports: Implications on treatment of depression and ADHD. NeuroImage 2013, 86: 164-171. PMID: 23933039, DOI: 10.1016/j.neuroimage.2013.08.001.Peer-Reviewed Original ResearchMeSH KeywordsAdrenergic Uptake InhibitorsAnimalsAtomoxetine HydrochlorideAttention Deficit Disorder with HyperactivityBrainDepressionDose-Response Relationship, DrugMacaca mulattaNorepinephrine Plasma Membrane Transport ProteinsPositron-Emission TomographyPropylaminesSerotonin Plasma Membrane Transport ProteinsTissue DistributionConceptsTreatment of depressionNorepinephrine transporterComparative PET imaging studyMetabolite-corrected arterial input functionFinal infusion rateDoses of atomoxetineDose-dependent occupancyPET imaging studiesSelective serotonin transporter (SERT) ligandNon-human primatesPlasma levelsSelective blockadeSaline infusionClinical dosesTherapeutic effectInfusion rateRelevant dosePET scansAtomoxetineRelevant dosesSerotonin transporter ligandDistribution volumeImaging studiesRhesus monkeysArterial input function
2008
Shortened protocol in practical [11C]SA4503-PET studies for sigma1 receptor quantification
Sakata M, Kimura Y, Naganawa M, Ishikawa M, Oda K, Ishii K, Hashimoto K, Chihara K, Ishiwata K. Shortened protocol in practical [11C]SA4503-PET studies for sigma1 receptor quantification. Annals Of Nuclear Medicine 2008, 22: 143-146. PMID: 18311540, DOI: 10.1007/s12149-007-0088-x.Peer-Reviewed Original ResearchMeSH KeywordsAdultBrain ChemistryBrain MappingCarbon RadioisotopesClinical ProtocolsFluvoxamineHumansImage Interpretation, Computer-AssistedImage Processing, Computer-AssistedIsotope LabelingMaleParoxetinePiperazinesPositron-Emission TomographyRadioligand AssayRadiopharmaceuticalsReceptors, sigmaSelective Serotonin Reuptake InhibitorsTissue DistributionConceptsTotal distribution volumePET scansSelective serotonin reuptake inhibitorsSerotonin reuptake inhibitorsReuptake inhibitorsHealthy subjectsLogan plot analysisReceptor measurementsTomography diagnosisTime-activity curvesBrain disordersDistribution volumePET studiesReceptor quantificationTissue time-activity curvesScansCompartmental analysisFull-length protocolsPositron Emission Tomography DiagnosisPatientsPlot analysisRegion of interestProtocolDiagnosisAdministration
2007
Wavelet denoising for voxel-based compartmental analysis of peripheral benzodiazepine receptors with 18F-FEDAA1106
Shidahara M, Ikoma Y, Seki C, Fujimura Y, Naganawa M, Ito H, Suhara T, Kanno I, Kimura Y. Wavelet denoising for voxel-based compartmental analysis of peripheral benzodiazepine receptors with 18F-FEDAA1106. European Journal Of Nuclear Medicine And Molecular Imaging 2007, 35: 416. PMID: 18026949, DOI: 10.1007/s00259-007-0623-y.Peer-Reviewed Original ResearchEvaluation of distribution of adenosine A2A receptors in normal human brain measured with [11C]TMSX PET
Mishina M, Ishiwata K, Kimura Y, Naganawa M, Oda K, Kobayashi S, Katayama Y, Ishii K. Evaluation of distribution of adenosine A2A receptors in normal human brain measured with [11C]TMSX PET. Synapse 2007, 61: 778-784. PMID: 17568431, DOI: 10.1002/syn.20423.Peer-Reviewed Original ResearchConceptsPositron emission tomographyPosterior putamenCaudate nucleusFrontal lobeHuman brainPromising PET ligandSelective A2AR antagonistNormal male subjectsMetabolite-corrected plasmaPosterior cingulate gyrusAdenosine A2A receptorsNormal human brainCerebral cortexA2AR antagonistCingulate gyrusArterial bloodOccipital lobeParkinson's diseaseTemporal lobePET scansA2A receptorsThree-compartment modelParietal lobePET ligandMale subjects