2015
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
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
Parametric Imaging and Test–Retest Variability of 11C-(+)-PHNO Binding to D2/D3 Dopamine Receptors in Humans on the High-Resolution Research Tomograph PET Scanner
Gallezot JD, Zheng MQ, Lim K, Lin SF, Labaree D, Matuskey D, Huang Y, Ding YS, Carson RE, Malison RT. Parametric Imaging and Test–Retest Variability of 11C-(+)-PHNO Binding to D2/D3 Dopamine Receptors in Humans on the High-Resolution Research Tomograph PET Scanner. Journal Of Nuclear Medicine 2014, 55: 960-966. PMID: 24732151, PMCID: PMC4201637, DOI: 10.2967/jnumed.113.132928.Peer-Reviewed Original Research
2013
Quantitative Analysis of [11C]-Erlotinib PET Demonstrates Specific Binding for Activating Mutations of the EGFR Kinase Domain
Petrulli JR, Sullivan JM, Zheng MQ, Bennett DC, Charest J, Huang Y, Morris ED, Contessa JN. Quantitative Analysis of [11C]-Erlotinib PET Demonstrates Specific Binding for Activating Mutations of the EGFR Kinase Domain. Neoplasia 2013, 15: 1347-1353. PMID: 24403856, PMCID: PMC3884525, DOI: 10.1593/neo.131666.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsCarbon RadioisotopesCatalytic DomainCell Line, TumorDrug Evaluation, PreclinicalErbB ReceptorsErlotinib HydrochlorideGene ExpressionHumansMiceMice, NudeMutation, MissenseNeoplasm TransplantationPhosphorylationPositron-Emission TomographyProtein BindingProtein Processing, Post-TranslationalQuinazolinesRadiopharmaceuticalsConceptsNon-small cell lung cancerEpidermal growth factor receptorPositron emission tomographyMutant non-small cell lung cancerNovel clinical methodologyCell lung cancerMutations of EGFREGFR mutation statusDomain mutationsHuman cancer xenograftsKinase domain mutationsConstitutive EGFR phosphorylationMultiple tumor typesPET scan analysisMolecular imaging approachesExtracellular domain mutationsWild-type epidermal growth factor receptorSimplified reference tissue modelGrowth factor receptorReference tissue modelNSCLC xenograftsLung cancerCancer xenograftsMalignant gliomasClinical utilityImaging 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 imagingBPNDReceptors