2016
Imaging of cerebral α4β2* nicotinic acetylcholine receptors with (−)-[18F]Flubatine PET: Implementation of bolus plus constant infusion and sensitivity to acetylcholine in human brain
Hillmer AT, Esterlis I, Gallezot JD, Bois F, Zheng MQ, Nabulsi N, Lin SF, Papke RL, Huang Y, Sabri O, Carson RE, Cosgrove KP. Imaging of cerebral α4β2* nicotinic acetylcholine receptors with (−)-[18F]Flubatine PET: Implementation of bolus plus constant infusion and sensitivity to acetylcholine in human brain. NeuroImage 2016, 141: 71-80. PMID: 27426839, PMCID: PMC5026941, DOI: 10.1016/j.neuroimage.2016.07.026.Peer-Reviewed Original ResearchMeSH KeywordsAcetylcholineAdultBenzamidesBrainBridged Bicyclo Compounds, HeterocyclicComputer SimulationHumansImage Interpretation, Computer-AssistedInfusions, IntraventricularMetabolic Clearance RateMiddle AgedModels, NeurologicalMolecular ImagingNeurotransmitter AgentsPositron-Emission TomographyRadiopharmaceuticalsReceptors, NicotinicReproducibility of ResultsSensitivity and SpecificityTissue DistributionYoung AdultConceptsGray matter regions
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 measurementsMonkeysEvaluation of the sensitivity of the novel α4β2* nicotinic acetylcholine receptor PET radioligand 18F‐(‐)‐NCFHEB to increases in synaptic acetylcholine levels in rhesus monkeys
Gallezot J, Esterlis I, Bois F, Zheng M, Lin S, Kloczynski T, Krystal JH, Huang Y, Sabri O, Carson RE, Cosgrove KP. Evaluation of the sensitivity of the novel α4β2* nicotinic acetylcholine receptor PET radioligand 18F‐(‐)‐NCFHEB to increases in synaptic acetylcholine levels in rhesus monkeys. Synapse 2014, 68: 556-564. PMID: 25043426, PMCID: PMC4224280, DOI: 10.1002/syn.21767.Peer-Reviewed Original ResearchConceptsSynaptic acetylcholine concentrationPositron emission tomographyAcetylcholine concentrationRhesus monkeysInfusion of physostigmineSynaptic acetylcholine levelsDose-dependent reductionNicotinic acetylcholine receptorsAcetylcholine levelsBolus injectionAcetylcholine receptorsAcetylcholine dynamicsNew radioligandEmission tomographyArterial input functionAcetylcholinesterase inhibitorsRadioligandThalamusPhysostigmineDonepezilΑ4β2Promising tracerBaselineMonkeysShort scan duration
2009
Decrease of Nicotinic Receptors in the Nigrostriatal System in Parkinson's Disease
Kas A, Bottlaender M, Gallezot JD, Vidailhet M, Villafane G, Grégoire MC, Coulon C, Valette H, Dollé F, Ribeiro MJ, Hantraye P, Remy P. Decrease of Nicotinic Receptors in the Nigrostriatal System in Parkinson's Disease. Cerebrovascular And Brain Metabolism Reviews 2009, 29: 1601-1608. PMID: 19491921, DOI: 10.1038/jcbfm.2009.74.Peer-Reviewed Original ResearchConceptsParkinson's diseasePositron emission tomographyDistribution volumeDopaminergic functionPD severityCerebral nicotinic acetylcholine receptorsStriatal dopaminergic functionNicotinic acetylcholine receptorsNAChR densityNeuroprotective actionNigrostriatal systemClinical scoresPD patientsSubstantia nigraHealthy controlsPD groupPostmortem studiesLower incidenceNicotinic receptorsPET markersPET scansPD stagesAcetylcholine receptorsEmission tomographyDisease
2007
Quantification of Cerebral Nicotinic Acetylcholine Receptors by PET Using 2-[18F]Fluoro-A-85380 and the Multiinjection Approach
Gallezot JD, Bottlaender MA, Delforge J, Valette H, Saba W, Dollé F, Coulon CM, Ottaviani MP, Hinnen F, Syrota A, Grégoire MC. Quantification of Cerebral Nicotinic Acetylcholine Receptors by PET Using 2-[18F]Fluoro-A-85380 and the Multiinjection Approach. Cerebrovascular And Brain Metabolism Reviews 2007, 28: 172-189. PMID: 17519978, DOI: 10.1038/sj.jcbfm.9600505.Peer-Reviewed Original Research
2005
In vivo imaging of human cerebral nicotinic acetylcholine receptors with 2-18F-fluoro-A-85380 and PET.
Gallezot JD, Bottlaender M, Grégoire MC, Roumenov D, Deverre JR, Coulon C, Ottaviani M, Dollé F, Syrota A, Valette H. In vivo imaging of human cerebral nicotinic acetylcholine receptors with 2-18F-fluoro-A-85380 and PET. Journal Of Nuclear Medicine 2005, 46: 240-7. PMID: 15695782.Peer-Reviewed Original ResearchConceptsNicotinic acetylcholine receptorsLogan graphical analysisPET scansTime-activity curvesAcetylcholine receptorsStudy durationCerebral nicotinic acetylcholine receptorsDistribution of nAChRsVolume of distributionDynamic PET scansHuman brainIntravenous injectionFrontal cortexOccipital cortexHuman volunteersPET radioligandCompartment modelCompartmental kinetic analysisLogan analysisVolume of interest