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