2014
Evaluation of [18F]-(-)-norchlorofluorohomoepibatidine ([18F]-(-)-NCFHEB) as a PET radioligand to image the nicotinic acetylcholine receptors in non-human primates
Bois F, Gallezot JD, Zheng MQ, Lin SF, Esterlis I, Cosgrove KP, Carson RE, Huang Y. Evaluation of [18F]-(-)-norchlorofluorohomoepibatidine ([18F]-(-)-NCFHEB) as a PET radioligand to image the nicotinic acetylcholine receptors in non-human primates. Nuclear Medicine And Biology 2014, 42: 570-577. PMID: 25858513, PMCID: PMC4441617, DOI: 10.1016/j.nucmedbio.2014.08.003.Peer-Reviewed Original ResearchConceptsRhesus monkeysGood test-retest reproducibilityML/Plasma free fractionReceptor binding profileNicotinic acetylcholine receptorsTest-retest reproducibilityNon-human primatesReceptor radiotracerΑ4β2 receptorsFrontal cortexPET examinationsMonkey brainAcetylcholine receptorsBrain regionsDistribution volumePET radioligandMultilinear analysis methodPharmacokinetic propertiesEnd of synthesisNon-displaceable distribution volumeFree fractionPET measurementsMonkeysAn 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 purityRelationship Between Glycine Transporter 1 Inhibition as Measured with Positron Emission Tomography and Changes in Cognitive Performances in Nonhuman Primates
Castner SA, Murthy NV, Ridler K, Herdon H, Roberts BM, Weinzimmer DP, Huang Y, Zheng MQ, Rabiner EA, Gunn RN, Carson RE, Williams GV, Laruelle M. Relationship Between Glycine Transporter 1 Inhibition as Measured with Positron Emission Tomography and Changes in Cognitive Performances in Nonhuman Primates. Neuropsychopharmacology 2014, 39: 2742-2749. PMID: 24487737, PMCID: PMC4200505, DOI: 10.1038/npp.2014.4.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBenzamidesBrainCarbon RadioisotopesCentral Nervous System AgentsExcitatory Amino Acid AntagonistsFemaleGlycine Plasma Membrane Transport ProteinsKetamineMacaca mulattaMaleMemory, Short-TermNeuropsychological TestsN-MethylaspartatePositron-Emission TomographyRadiopharmaceuticalsSpatial MemoryTetrahydronaphthalenesConceptsOrg 25935GlyT-1 inhibitorsNMDA hypofunctionN-methyl-D-aspartate receptorsPotential therapeutic effectsTreatment of schizophreniaPositron emission tomography (PET) radiotracerPositron emission tomographyNMDA transmissionGlutamatergic transmissionControl conditionKetamine administrationNMDA receptorsTherapeutic effectExtracellular glycineExtracellular levelsGlyT-1Emission tomographyMemory deficitsRhesus monkeysTomography radiotracerNonhuman primatesLines of evidenceHypofunctionCognitive performance
2013
Imaging Nicotine- and Amphetamine-Induced Dopamine Release in Rhesus Monkeys with [11C]PHNO vs [11C]raclopride PET
Gallezot JD, Kloczynski T, Weinzimmer D, Labaree D, Zheng MQ, Lim K, Rabiner EA, Ridler K, Pittman B, Huang Y, Carson RE, Morris ED, Cosgrove KP. Imaging Nicotine- and Amphetamine-Induced Dopamine Release in Rhesus Monkeys with [11C]PHNO vs [11C]raclopride PET. Neuropsychopharmacology 2013, 39: 866-874. PMID: 24220025, PMCID: PMC3924521, DOI: 10.1038/npp.2013.286.Peer-Reviewed Original ResearchConceptsAmphetamine-induced DA releaseD2/D3 receptorsDA releaseD3 receptorsRhesus monkeysAmphetamine-Induced Dopamine ReleaseDopamine D2/D3 receptorsHuman tobacco smokersAmphetamine-induced changesClinical neuroimaging studiesAdult rhesus monkeysPositron emission tomography (PET) imagingEmission Tomography ImagingLow-affinity receptorsNon-human primatesTobacco smokersSubstantia nigraGlobus pallidusDopamine releaseNucleus accumbensNicotineNeuroimaging studiesTomography imagingBPNDReceptorsDetermination 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