2019
Development 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 ResearchMeSH KeywordsAnimalsMacaca mulattaPiperazinePiperazinesPositron-Emission TomographyRadioactive TracersRadiochemistryReceptors, Opioid, kappaConceptsMultilinear 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
An Improved Antagonist Radiotracer for the κ-Opioid Receptor: Synthesis and Characterization of 11C-LY2459989
Zheng MQ, Kim SJ, Holden D, Lin SF, Need A, Rash K, Barth V, Mitch C, Navarro A, Kapinos M, Maloney K, Ropchan J, Carson RE, Huang Y. An Improved Antagonist Radiotracer for the κ-Opioid Receptor: Synthesis and Characterization of 11C-LY2459989. Journal Of Nuclear Medicine 2014, 55: 1185-1191. PMID: 24854795, PMCID: PMC4826283, DOI: 10.2967/jnumed.114.138701.Peer-Reviewed Original ResearchConceptsHigh specific binding signalsΚ-opioid receptorsSpecific binding signalsPET radioligandRhesus monkeysPromising PET imaging agentSelective KOR antagonistNovel PET radioligandFavorable pharmacokinetic propertiesPET imaging agentMultilinear analysis-1 (MA1) methodAntagonist radiotracersKOR antagonistsPeripheral metabolismGlobus pallidusOpioid receptorsTracer candidatesFrontal cortexArterial input function measurementTemporal cortexCingulate cortexNeuropsychiatric diseasesPharmacokinetic propertiesFull antagonistHigh radiochemical purity
2013
Determination of the In Vivo Selectivity of a New κ-Opioid Receptor Antagonist PET Tracer 11C-LY2795050 in the Rhesus Monkey
Kim SJ, Zheng MQ, Nabulsi N, Labaree D, Ropchan J, Najafzadeh S, Carson RE, Huang Y, Morris ED. Determination of the In Vivo Selectivity of a New κ-Opioid Receptor Antagonist PET Tracer 11C-LY2795050 in the Rhesus Monkey. Journal Of Nuclear Medicine 2013, 54: 1668-1674. PMID: 23918735, PMCID: PMC5824998, DOI: 10.2967/jnumed.112.118877.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBenzamidesBrainComputer SimulationImage Interpretation, Computer-AssistedMacaca mulattaMetabolic Clearance RateModels, BiologicalPositron-Emission TomographyPyrrolidinesRadiopharmaceuticalsReceptors, Opioid, kappaReproducibility of ResultsSensitivity and SpecificityTissue DistributionSynthesis and Evaluation of 11C-LY2795050 as a κ-Opioid Receptor Antagonist Radiotracer for PET Imaging
Zheng MQ, Nabulsi N, Kim SJ, Tomasi G, Lin SF, Mitch C, Quimby S, Barth V, Rash K, Masters J, Navarro A, Seest E, Morris ED, Carson RE, Huang Y. Synthesis and Evaluation of 11C-LY2795050 as a κ-Opioid Receptor Antagonist Radiotracer for PET Imaging. Journal Of Nuclear Medicine 2013, 54: 455-463. PMID: 23353688, PMCID: PMC3775344, DOI: 10.2967/jnumed.112.109512.Peer-Reviewed Original ResearchConceptsKappa-opioid receptorsAntagonist radiotracersSelective kappa opioid receptorPET imagingKOR knockout micePathophysiology of depressionSelective KOR antagonistRadioligand competition binding assaysEx vivo analysisDose-dependent mannerFavorable pharmacokinetic propertiesFull antagonist activityKOR antagonistsPeripheral metabolismKOR agonistsTracer candidatesLY2795050Sprague-DawleyAntagonist tracersKnockout miceSpecific binding signalsCompetition binding assaysRhesus monkeysPharmacokinetic propertiesAntagonist activity