2020
Kinetic Modeling and Test–Retest Reproducibility of 11C-EKAP and 11C-FEKAP, Novel Agonist Radiotracers for PET Imaging of the κ-Opioid Receptor in Humans
Naganawa M, Li S, Nabulsi N, Lin SF, Labaree D, Ropchan J, Gao H, Mei M, Henry S, Matuskey D, Carson RE, Huang Y. Kinetic Modeling and Test–Retest Reproducibility of 11C-EKAP and 11C-FEKAP, Novel Agonist Radiotracers for PET Imaging of the κ-Opioid Receptor in Humans. Journal Of Nuclear Medicine 2020, 61: 1636-1642. PMID: 32169917, PMCID: PMC9364890, DOI: 10.2967/jnumed.119.227694.Peer-Reviewed Original Research
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 fractionDevelopment and In Vivo Evaluation of a κ-Opioid Receptor Agonist as a PET Radiotracer with Superior Imaging Characteristics
Li S, Zheng MQ, Naganawa M, Kim S, Gao H, Kapinos M, Labaree D, Huang Y. Development and In Vivo Evaluation of a κ-Opioid Receptor Agonist as a PET Radiotracer with Superior Imaging Characteristics. Journal Of Nuclear Medicine 2019, 60: 1023-1030. PMID: 30630942, PMCID: PMC6604690, DOI: 10.2967/jnumed.118.220517.Peer-Reviewed Original ResearchConceptsMultilinear analysis 1Κ-opioid receptor agonistCentral nervous system diseaseNervous system diseasesHigh specific bindingAgonist tracersGlobus pallidusReceptor abnormalitiesReceptor agonistFrontal cortexSystem diseasesPrimate brainReceptor occupancySuperior imaging characteristicsCingulate cortexAlzheimer's diseasePeak uptakeImaging characteristicsRhesus monkeysOptimal radiotracerPET studiesArterial input functionBlocking studiesPET radiotracersAnalysis 1
2014
Evaluation of the agonist PET radioligand [11C]GR103545 to image kappa opioid receptor in humans: Kinetic model selection, test–retest reproducibility and receptor occupancy by the antagonist PF-04455242
Naganawa M, Jacobsen LK, Zheng MQ, Lin SF, Banerjee A, Byon W, Weinzimmer D, Tomasi G, Nabulsi N, Grimwood S, Badura LL, Carson RE, McCarthy TJ, Huang Y. Evaluation of the agonist PET radioligand [11C]GR103545 to image kappa opioid receptor in humans: Kinetic model selection, test–retest reproducibility and receptor occupancy by the antagonist PF-04455242. NeuroImage 2014, 99: 69-79. PMID: 24844744, PMCID: PMC4140089, DOI: 10.1016/j.neuroimage.2014.05.033.Peer-Reviewed Original ResearchConceptsKappa-opioid receptorsTest-retest reproducibilityTest-retest variabilityAbsolute test-retest variabilityPF-04455242Time-activity curvesIntra-class coefficientOpioid receptorsRegional time-activity curvesMetabolite-corrected arterial input functionHuman positron emission tomography studiesPositron emission tomography studySelective KOR antagonistEmission tomography studiesReceptor occupancy studiesSuitable reference regionHalf maximal inhibitory concentrationAgonist tracersRegional VTAgonist PET radioligandOral doseKOR antagonistsMaximal inhibitory concentrationOral administrationPreclinical models
2009
Improvement of likelihood estimation in Logan graphical analysis using maximum a posteriori for neuroreceptor PET imaging
Shidahara M, Seki C, Naganawa M, Sakata M, Ishikawa M, Ito H, Kanno I, Ishiwata K, Kimura Y. Improvement of likelihood estimation in Logan graphical analysis using maximum a posteriori for neuroreceptor PET imaging. Annals Of Nuclear Medicine 2009, 23: 163-171. PMID: 19225940, DOI: 10.1007/s12149-008-0226-0.Peer-Reviewed Original Research
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
Distribution volume as an alternative to the binding potential for sigma1 receptor imaging
Kimura Y, Naganawa M, Sakata M, Ishikawa M, Mishina M, Oda K, Ishii K, Ishiwata K. Distribution volume as an alternative to the binding potential for sigma1 receptor imaging. Annals Of Nuclear Medicine 2007, 21: 533-535. PMID: 18030587, DOI: 10.1007/s12149-007-0063-6.Peer-Reviewed Original ResearchMeSH KeywordsAdultAgedAnatomy, RegionalBrainBrain MappingCarbon RadioisotopesData Interpretation, StatisticalFemaleHumansImage Processing, Computer-AssistedMaleMiddle AgedNonlinear DynamicsPiperazinesPositron-Emission TomographyRadioligand AssayRadiopharmaceuticalsReceptors, sigmaReference StandardsConceptsPositron emission tomographyDistribution volumeTotal distribution volumeReference regionReceptor densityClinical investigationReceptor imagingSigma1 receptorsEmission tomographyAppropriate reference regionReceptorsTarget receptorsPhysiological situationsNeuroreceptor mappingHigh affinityImagingDVTDiseaseRadioligandBrainHigh Occupancy of Sigma-1 Receptors in the Human Brain after Single Oral Administration of Fluvoxamine: A Positron Emission Tomography Study Using [11C]SA4503
Ishikawa M, Ishiwata K, Ishii K, Kimura Y, Sakata M, Naganawa M, Oda K, Miyatake R, Fujisaki M, Shimizu E, Shirayama Y, Iyo M, Hashimoto K. High Occupancy of Sigma-1 Receptors in the Human Brain after Single Oral Administration of Fluvoxamine: A Positron Emission Tomography Study Using [11C]SA4503. Biological Psychiatry 2007, 62: 878-883. PMID: 17662961, DOI: 10.1016/j.biopsych.2007.04.001.Peer-Reviewed Original ResearchConceptsSelective serotonin reuptake inhibitorsSigma-1 receptorMechanism of actionPositron emission tomography studySerotonin reuptake inhibitorsHuman brainHealthy male volunteersSingle oral administrationEmission tomography studiesSelective sigma-1 receptor ligandSigma-1 receptor ligandsDose-dependent mannerReuptake inhibitorsSingle doseTherapeutic dosesOral administrationMale volunteersArterial bloodPET scansPsychiatric diseasesFluvoxamineGene polymorphismsBrain regionsFunctional polymorphismsTomography studyMapping 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