2019
Kappa-opioid receptors, dynorphin, and cocaine addiction: a positron emission tomography study
Martinez D, Slifstein M, Matuskey D, Nabulsi N, Zheng MQ, Lin SF, Ropchan J, Urban N, Grassetti A, Chang D, Salling M, Foltin R, Carson RE, Huang Y. Kappa-opioid receptors, dynorphin, and cocaine addiction: a positron emission tomography study. Neuropsychopharmacology 2019, 44: 1720-1727. PMID: 31026862, PMCID: PMC6785004, DOI: 10.1038/s41386-019-0398-4.Peer-Reviewed Original ResearchConceptsCocaine use disorderStress-induced relapsePositron emission tomographyCocaine bingeKappa-opioid receptor/dynorphin systemKOR selective agonistPositron emission tomography studyKappa-opioid receptorsCold pressor testCocaine self-administration sessionsEmission tomography studiesSelf-administration sessionsStress-induced cocaineEndogenous dynorphinDynorphin systemHealthy controlsPressor testSelective agonistPET scansAnimal studiesKOR bindingReceptor availabilitySignificant associationBrain regionsEmission tomography
2017
Quantification of Tumor Hypoxic Fractions Using Positron Emission Tomography with [18F]Fluoromisonidazole ([18F]FMISO) Kinetic Analysis and Invasive Oxygen Measurements
Kelada OJ, Rockwell S, Zheng MQ, Huang Y, Liu Y, Booth CJ, Decker RH, Oelfke U, Carson RE, Carlson DJ. Quantification of Tumor Hypoxic Fractions Using Positron Emission Tomography with [18F]Fluoromisonidazole ([18F]FMISO) Kinetic Analysis and Invasive Oxygen Measurements. Molecular Imaging And Biology 2017, 19: 893-902. PMID: 28409339, PMCID: PMC5640490, DOI: 10.1007/s11307-017-1083-9.Peer-Reviewed Original ResearchConceptsPositron emission tomographyTumor hypoxic fractionHypoxic fractionEmission tomographyLung cancer radiotherapy patientsPO2 measurementsAbsolute tumor volumeC miceDirect pO2 measurementsBlood ratioClinical impactTumor volumeHypoxia quantificationSubcutaneous tumorsPurposeThe purposeTracer kinetic modelingRadiotherapy patientsPET imagingPatientsPO2 valuesScansPatlak modelTomographyTwo-compartmentTBR
2015
Receptor Occupancy of the κ-Opioid Antagonist LY2456302 Measured with Positron Emission Tomography and the Novel Radiotracer 11C-LY2795050
Naganawa M, Dickinson GL, Zheng MQ, Henry S, Vandenhende F, Witcher J, Bell R, Nabulsi N, Lin SF, Ropchan J, Neumeister A, Ranganathan M, Tauscher J, Huang Y, Carson RE. Receptor Occupancy of the κ-Opioid Antagonist LY2456302 Measured with Positron Emission Tomography and the Novel Radiotracer 11C-LY2795050. Journal Of Pharmacology And Experimental Therapeutics 2015, 356: 260-266. PMID: 26628406, PMCID: PMC4727157, DOI: 10.1124/jpet.115.229278.Peer-Reviewed Original ResearchConceptsHours postdosePositron emission tomographyReceptor occupancyEmission tomographySerious adverse eventsSingle oral dosesImportant therapeutic roleΚ-opioid receptorsSubstance abuse disordersFurther clinical testingHealthy human subjectsMultilinear analysis-1 (MA1) methodAntagonist radiotracersAdverse eventsOral dosesBrain penetrationTherapeutic rolePlasma concentrationsAbuse disordersEthanol consumptionLY2456302Clinical testingNovel radiotracersAlcohol dependenceDistribution volumeA Promising PET Tracer for Imaging of α7 Nicotinic Acetylcholine Receptors in the Brain: Design, Synthesis, and in Vivo Evaluation of a Dibenzothiophene-Based Radioligand
Teodoro R, Scheunemann M, Deuther-Conrad W, Wenzel B, Fasoli FM, Gotti C, Kranz M, Donat CK, Patt M, Hillmer A, Zheng MQ, Peters D, Steinbach J, Sabri O, Huang Y, Brust P. A Promising PET Tracer for Imaging of α7 Nicotinic Acetylcholine Receptors in the Brain: Design, Synthesis, and in Vivo Evaluation of a Dibenzothiophene-Based Radioligand. Molecules 2015, 20: 18387-18421. PMID: 26473809, PMCID: PMC6332508, DOI: 10.3390/molecules201018387.Peer-Reviewed Original ResearchMeSH KeywordsAlpha7 Nicotinic Acetylcholine ReceptorAnimalsAza CompoundsBrainBrain MappingFluorine RadioisotopesHaplorhiniHumansHydrogen BondingKineticsLigandsOxidesPiperazinesPositron-Emission TomographyProtein BindingRadiopharmaceuticalsRatsReceptors, Serotonin, 5-HT3Structure-Activity RelationshipSwineThiophenesTissue DistributionConceptsStructure-activity relationshipsCationic centerPositron emission tomographyHydrogen bond acceptor functionalitiesNicotinic acetylcholine receptorsAcceptor functionalitiesAcetylcholine receptorsNew ligandsDibenzothiophene dioxideΑ7 nicotinic acetylcholine receptorCompound 7Promising PET tracerNew basic structureRadioligand displacement studiesTwo-tissue compartment modelLigandsEmission tomographyPET radioligandKinetic analysisFurther evaluationDynamic positron emission tomographyPET tracersInitial evaluationVivo evaluationBrain
2014
Relationship 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
Elevated brain cannabinoid CB1 receptor availability in post-traumatic stress disorder: a positron emission tomography study
Neumeister A, Normandin MD, Pietrzak RH, Piomelli D, Zheng MQ, Gujarro-Anton A, Potenza MN, Bailey CR, Lin SF, Najafzadeh S, Ropchan J, Henry S, Corsi-Travali S, Carson RE, Huang Y. Elevated brain cannabinoid CB1 receptor availability in post-traumatic stress disorder: a positron emission tomography study. Molecular Psychiatry 2013, 18: 1034-1040. PMID: 23670490, PMCID: PMC3752332, DOI: 10.1038/mp.2013.61.Peer-Reviewed Original ResearchMeSH KeywordsAdultAmidesAnalysis of VarianceArachidonic AcidsBrainEndocannabinoidsEthanolaminesFemaleGlyceridesHumansHydrocortisoneImidazolesLogistic ModelsMalePalmitic AcidsPiperidinesPolyunsaturated AlkamidesPyrazolesRadionuclide ImagingReceptor, Cannabinoid, CB1Stress Disorders, Post-TraumaticYoung AdultConceptsPost-traumatic stress disorderVolume of distributionCB1 receptor availabilityPositron emission tomographyHC groupReceptor availabilityTC groupCannabinoid type 1 receptorStress disorderPositron emission tomography studyEvidence-based pharmacotherapyEtiology of PTSDType 1 receptorEmission tomography studiesAnandamide concentrationsElevated brainPeripheral levelsHealthy controlsCB1 receptorsUntreated individualsPET scansAnimal modelsCortisol levelsLifetime historyEmission tomography
2010
Development of effective PET and SPECT imaging agents for the serotonin transporter: has a twenty-year journey reached its destination?
Huang Y, Zheng MQ, Gerdes JM. Development of effective PET and SPECT imaging agents for the serotonin transporter: has a twenty-year journey reached its destination? Current Topics In Medicinal Chemistry 2010, 10: 1499-526. PMID: 20583995, DOI: 10.2174/156802610793176792.Peer-Reviewed Original ResearchConceptsChemical scaffoldsPositron emission tomographySerotonin transporterTwenty-year journeyImaging tracerFunction of SERTRelated compoundsNon-specific bindingSingle photon emissionRadiotracer developmentSpecific binding signalsPromising radiotracerAlzheimer's diseaseEmission tomographyNeurodegenerative disordersNeuropsychiatric disordersSPECT radiotracerSubstance abusePharmacological propertiesDiseaseScaffoldsTerms of tissueSPECTDiarylsulfidesVivo