2021
PET Imaging Estimates of Regional Acetylcholine Concentration Variation in Living Human Brain
Smart K, Naganawa M, Baldassarri SR, Nabulsi N, Ropchan J, Najafzadeh S, Gao H, Navarro A, Barth V, Esterlis I, Cosgrove KP, Huang Y, Carson RE, Hillmer AT. PET Imaging Estimates of Regional Acetylcholine Concentration Variation in Living Human Brain. Cerebral Cortex 2021, 31: 2787-2798. PMID: 33442731, PMCID: PMC8355478, DOI: 10.1093/cercor/bhaa387.Peer-Reviewed Original ResearchConceptsACh concentrationHuman volunteersHigh ACh concentrationsMuscarinic antagonist scopolamineHealthy human volunteersHuman brainCholinergic receptorsNicotine challengeAntagonist scopolaminePreclinical studiesStriatal regionsPET scansEndogenous neurotransmittersNeuropsychiatric diseasesNonhuman primatesWhole-brain imagesDrug occupancyNicotinic ligandsClinical populationsBrainAcetylcholineDistinct functional rolesStriatumVolunteersFunctional role
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 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
1998
Muscarinic Cholinergic Receptor Measurements With [18F]FP-TZTP: Control and Competition Studies
Carson R, Kiesewetter D, Jagoda E, Der M, Herscovitch P, Eckelman W. Muscarinic Cholinergic Receptor Measurements With [18F]FP-TZTP: Control and Competition Studies. Cerebrovascular And Brain Metabolism Reviews 1998, 18: 1130-1142. PMID: 9778190, DOI: 10.1097/00004647-199810000-00010.Peer-Reviewed Original ResearchMeSH KeywordsAcetylcholineAnesthesiaAnesthetics, InhalationAnimalsBinding, CompetitiveBlood ProteinsBrainCholinesterase InhibitorsChromatography, Thin LayerFluorine RadioisotopesIsofluraneKineticsMacaca mulattaModels, NeurologicalPhysostigminePyridinesReceptors, MuscarinicThiazolesTomography, Emission-ComputedConceptsCholinergic receptorsBasal gangliaMuscarinic cholinergic receptorsPositron emission tomography studyM2 cholinergic receptorsMuscarinic cholinergic ligandEmission tomography studiesPositron emission tomographyBrain acetylcholineIntravenous infusionMuscarinic receptorsHigh AChE activityControl studyML xSubcortical regionsAlzheimer's diseaseGray matterCortical regionsEmission tomographyRhesus monkeysArterial input functionTomography studyCholinergic ligandsTracer injectionAChE activity