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
2007
High 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