Featured Publications
Quantification of Amphetamine-Induced Changes in [11C] Raclopride Binding with Continuous Infusion
Carson R, Breier* A, de Bartolomeis* A, Saunders† R, Su* T, Schmall B, Der M, Pickar* D, Eckelman W. Quantification of Amphetamine-Induced Changes in [11C] Raclopride Binding with Continuous Infusion. Cerebrovascular And Brain Metabolism Reviews 1997, 17: 437-447. PMID: 9143226, DOI: 10.1097/00004647-199704000-00009.Peer-Reviewed Original Research
2023
Evaluation of a First PET Tracer Suitable for Imaging the Sigma‑2 Receptor in the Brain of Nonhuman Primates
Alluri S, Zheng M, Holden D, Zhang Y, Zhang L, Felchner Z, Li S, Ropchan J, Carson R, Jia H, Huang Y. Evaluation of a First PET Tracer Suitable for Imaging the Sigma‑2 Receptor in the Brain of Nonhuman Primates. Molecular Pharmaceutics 2023, 21: 194-200. PMID: 38013422, DOI: 10.1021/acs.molpharmaceut.3c00750.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBrainMacaca mulattaNeoplasmsPositron-Emission TomographyPrimatesRadiopharmaceuticalsConceptsAlzheimer's diseaseLimited brain uptakeNonhuman primate brainCentral nervous systemPotential therapeutic targetPositron emission tomography (PET) imagingEmission Tomography ImagingTransmembrane protein 97Sigma-2 receptorsFirst PET tracerBrain penetrantBrain uptakeTherapeutic targetNervous systemPrimate brainNeurological disordersPET tracersNonhuman primatesTomography imagingProtein 97CancerDiseaseBrainCell typesReceptors
2022
Imaging the fetal nonhuman primate brain with SV2A positron emission tomography (PET)
Rossano S, Toyonaga T, Berg E, Lorence I, Fowles K, Nabulsi N, Ropchan J, Li S, Ye Y, Felchner Z, Kukis D, Huang Y, Benveniste H, Tarantal AF, Groman S, Carson RE. Imaging the fetal nonhuman primate brain with SV2A positron emission tomography (PET). European Journal Of Nuclear Medicine And Molecular Imaging 2022, 49: 3679-3691. PMID: 35633376, PMCID: PMC9826644, DOI: 10.1007/s00259-022-05825-6.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBrainMacaca mulattaMembrane GlycoproteinsNerve Tissue ProteinsPositron-Emission TomographyConceptsPositron emission tomographySynaptic densityFetal brainThird trimesterEmission tomographyBrain developmentGravid rhesus monkeysPost-mortem brain tissueEarly neonatal periodNonhuman primate brainLate gestational periodSubset of subjectsPostnatal brain developmentPost-mortem samplesGestational ageNeonatal periodPregnant monkeysSynapse numberGestational periodPrimary motorPrimate brainBrain growthSubcortical regionsBrain tissueCortical regionsComparison of three novel radiotracers for GluN2B-containing NMDA receptors in non-human primates: (R)-[11C]NR2B-Me, (R)-[18F]of-Me-NB1, and (S)-[18F]of-NB1
Smart K, Zheng MQ, Ahmed H, Fang H, Xu Y, Cai L, Holden D, Kapinos M, Haider A, Felchner Z, Ropchan JR, Tamagnan G, Innis RB, Pike VW, Ametamey SM, Huang Y, Carson RE. Comparison of three novel radiotracers for GluN2B-containing NMDA receptors in non-human primates: (R)-[11C]NR2B-Me, (R)-[18F]of-Me-NB1, and (S)-[18F]of-NB1. Cerebrovascular And Brain Metabolism Reviews 2022, 42: 1398-1409. PMID: 35209743, PMCID: PMC9274863, DOI: 10.1177/0271678x221084416.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBrainMacaca mulattaPositron-Emission TomographyRadiopharmaceuticalsReceptors, N-Methyl-D-AspartateConceptsNon-human primatesNMDA receptorsML/GluN2B-containing NMDA receptorsFree fractionRegional non-displaceable binding potentialsNon-displaceable binding potentialGood brain uptakeAdult rhesus macaquesBrain uptakeOne-tissue compartment modelTime-activity curvesNovel radiotracersGray matterNeuropsychiatric disordersSelective radiotracerDisplaceable bindingRhesus macaquesTissue distributionAcceptable profilePotential translationRadiotracerCerebellumFurther investigationReceptors
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
2019
Evaluation of 11C-LSN3172176 as a Novel PET Tracer for Imaging M1 Muscarinic Acetylcholine Receptors in Nonhuman Primates
Nabulsi NB, Holden D, Zheng MQ, Bois F, Lin SF, Najafzadeh S, Gao H, Ropchan J, Lara-Jaime T, Labaree D, Shirali A, Slieker L, Jesudason C, Barth V, Navarro A, Kant N, Carson RE, Huang Y. Evaluation of 11C-LSN3172176 as a Novel PET Tracer for Imaging M1 Muscarinic Acetylcholine Receptors in Nonhuman Primates. Journal Of Nuclear Medicine 2019, 60: 1147-1153. PMID: 30733324, DOI: 10.2967/jnumed.118.222034.Peer-Reviewed Original ResearchConceptsMuscarinic acetylcholine receptorsAcetylcholine receptorsNonhuman primatesM1 muscarinic acetylcholine receptorBrain time-activity curvesRich brain regionsArterial blood samplingNovel PET tracersSuitable reference regionRegional distribution volumesReference regionDevelopment of drugsBrain uptakeGlobus pallidusDistribution volume valuesNucleus accumbensBlood samplingPET scansTime-activity curvesCognitive impairmentAlzheimer's diseaseBrain regionsDistribution volumeSelective radiotracerRhesus monkeys
2018
Synthesis and in Vivo Evaluation of a Novel PET Radiotracer for Imaging of Synaptic Vesicle Glycoprotein 2A (SV2A) in Nonhuman Primates
Li S, Cai Z, Wu X, Holden D, Pracitto R, Kapinos M, Gao H, Labaree D, Nabulsi N, Carson RE, Huang Y. Synthesis and in Vivo Evaluation of a Novel PET Radiotracer for Imaging of Synaptic Vesicle Glycoprotein 2A (SV2A) in Nonhuman Primates. ACS Chemical Neuroscience 2018, 10: 1544-1554. PMID: 30396272, PMCID: PMC6810685, DOI: 10.1021/acschemneuro.8b00526.Peer-Reviewed Original ResearchConceptsSynaptic vesicle glycoprotein 2AStandardized uptake valuePET radiotracersNonhuman primatesAlterations of synapsesC-UCBPeak standardized uptake valueVivo evaluationHigh brain uptakeNovel PET radiotracersBrain uptakeSynaptic densityExcellent radiotracerPsychiatric disordersUptake valueCingulate cortexAlzheimer's diseaseBrain disordersNovel radiotracersRhesus monkeysNeurodegenerative diseasesTissue kineticsDiseaseAttractive imaging propertiesLevetiracetam
2017
Evaluation of the Lysophosphatidic Acid Receptor Type 1 Radioligand 11C-BMT-136088 for Lung Imaging in Rhesus Monkeys
Gallezot JD, Nabulsi NB, Holden D, Lin SF, Labaree D, Ropchan J, Najafzadeh S, Donnelly DJ, Cao K, Bonacorsi S, Seiders J, Roppe J, Hayes W, Huang Y, Du S, Carson RE. Evaluation of the Lysophosphatidic Acid Receptor Type 1 Radioligand 11C-BMT-136088 for Lung Imaging in Rhesus Monkeys. Journal Of Nuclear Medicine 2017, 59: 327-333. PMID: 28864634, DOI: 10.2967/jnumed.117.195073.Peer-Reviewed Original ResearchConceptsMultilinear analysis 1Rhesus monkeysHighest organ doseLung tissue injuryLung regionsΜSv/MBqPlasma free fractionReceptor type 1Test-retest scansTest-retest variabilityVivo dissociationMolecule lysophosphatidic acidRight lung regionsML of plasmaNondisplaceable volumePulmonary fibrosisLung fibrosisVascular leakageInfusion protocolPlasma concentrationsTissue injuryDrug doseNormal healingOrgan doseType 1PET imaging of α7 nicotinic acetylcholine receptors: a comparative study of [18F]ASEM and [18F]DBT-10 in nonhuman primates, and further evaluation of [18F]ASEM in humans
Hillmer AT, Li S, Zheng MQ, Scheunemann M, Lin SF, Nabulsi N, Holden D, Pracitto R, Labaree D, Ropchan J, Teodoro R, Deuther-Conrad W, Esterlis I, Cosgrove KP, Brust P, Carson RE, Huang Y. PET imaging of α7 nicotinic acetylcholine receptors: a comparative study of [18F]ASEM and [18F]DBT-10 in nonhuman primates, and further evaluation of [18F]ASEM in humans. European Journal Of Nuclear Medicine And Molecular Imaging 2017, 44: 1042-1050. PMID: 28120003, PMCID: PMC5400702, DOI: 10.1007/s00259-017-3621-8.Peer-Reviewed Original Research
2016
First-in-Human Assessment of the Novel PDE2A PET Radiotracer 18F-PF-05270430
Naganawa M, Waterhouse RN, Nabulsi N, Lin SF, Labaree D, Ropchan J, Tarabar S, DeMartinis N, Ogden A, Banerjee A, Huang Y, Carson RE. First-in-Human Assessment of the Novel PDE2A PET Radiotracer 18F-PF-05270430. Journal Of Nuclear Medicine 2016, 57: 1388-1395. PMID: 27103022, PMCID: PMC5093918, DOI: 10.2967/jnumed.115.166850.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsAzabicyclo CompoundsAzetidinesBrainComputer SimulationCyclic Nucleotide Phosphodiesterases, Type 2Feasibility StudiesFemaleHumansIsotope LabelingMacaca mulattaMaleMetabolic Clearance RateModels, BiologicalMolecular ImagingOrgan SpecificityPilot ProjectsPositron-Emission TomographyRadiopharmaceuticalsReproducibility of ResultsSensitivity and SpecificityTissue DistributionConceptsTest-retest variabilityHuman studiesPET ligandWhite matterNeocortical regionsMultilinear analysis 1MSv/MBqHealthy male subjectsDetectable pharmacologic effectsAppropriate tracer kinetic modelsTest-retest protocolAdverse eventsBrain uptakePharmacologic effectsRegional time-activity curvesTarget doseTime-activity curvesTracer uptakeMale subjectsWhole brainBrain regionsEffective doseCritical organsPET radiotracersNonhuman primatesSynthesis and Preclinical Evaluation of 11C-UCB-J as a PET Tracer for Imaging the Synaptic Vesicle Glycoprotein 2A in the Brain
Nabulsi N, Mercier J, Holden D, Carré S, Najafzadeh S, Vandergeten MC, Lin SF, Deo A, Price N, Wood M, Lara-Jaime T, Montel F, Laruelle M, Carson RE, Hannestad J, Huang Y. Synthesis and Preclinical Evaluation of 11C-UCB-J as a PET Tracer for Imaging the Synaptic Vesicle Glycoprotein 2A in the Brain. Journal Of Nuclear Medicine 2016, 57: 777-784. PMID: 26848175, DOI: 10.2967/jnumed.115.168179.Peer-Reviewed Original ResearchConceptsSynaptic vesicle glycoprotein 2AWhole-body biodistributionPET radiotracersNonhuman primatesDose-limiting organHigher free fractionGray matter regionsBaseline VTNondisplaceable distribution volumeAntiepileptic drugsVitro inhibition constantSynaptic densityPreclinical evaluationMonkey brainDistribution volumeArterial samplingEndocrine cellsRegional volumesMatter regionsRhesus macaquesPET tracersUCBFree fractionBrainTarget occupancy
2015
Brivaracetam, a selective high‐affinity synaptic vesicle protein 2A (SV2A) ligand with preclinical evidence of high brain permeability and fast onset of action
Nicolas JM, Hannestad J, Holden D, Kervyn S, Nabulsi N, Tytgat D, Huang Y, Chanteux H, Staelens L, Matagne A, Mathy FX, Mercier J, Stockis A, Carson RE, Klitgaard H. Brivaracetam, a selective high‐affinity synaptic vesicle protein 2A (SV2A) ligand with preclinical evidence of high brain permeability and fast onset of action. Epilepsia 2015, 57: 201-209. PMID: 26663401, DOI: 10.1111/epi.13267.Peer-Reviewed Original ResearchConceptsFaster onsetAcute seizuresHigh-affinity synaptic vesicle protein 2A ligandNonhuman primate PET studyAudiogenic seizure miceRapid brain entryOnset of actionSingle oral dosingHigh brain permeabilityBlood-brain barrier permeability (BBBP) valuesPrimate PET studyAudiogenic miceBrain entryCaco-2 cellsSeizure micePreclinical evidenceAntiepileptic drugsSusceptible miceBrain levelsBrain penetrationPreclinical dataBrain kineticsOral dosingSingle dosingClinical studies
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
2012
In Vivo Imaging of Endogenous Pancreatic β-Cell Mass in Healthy and Type 1 Diabetic Subjects Using 18F-Fluoropropyl-Dihydrotetrabenazine and PET
Normandin MD, Petersen KF, Ding YS, Lin SF, Naik S, Fowles K, Skovronsky DM, Herold KC, McCarthy TJ, Calle RA, Carson RE, Treadway JL, Cline GW. In Vivo Imaging of Endogenous Pancreatic β-Cell Mass in Healthy and Type 1 Diabetic Subjects Using 18F-Fluoropropyl-Dihydrotetrabenazine and PET. Journal Of Nuclear Medicine 2012, 53: 908-916. PMID: 22573821, PMCID: PMC3737743, DOI: 10.2967/jnumed.111.100545.Peer-Reviewed Original ResearchConceptsType 1 diabetes mellitusVesicular monoamine transporter type 2Pancreatic β-cell massStandardized uptake valueΒ-cell massDiabetes mellitusUptake valueType 1 diabetic subjectsΒ-cell densityHealthy control subjectsInsulin secretion capacityΒ-cell functionPathophysiology of diabetesTransporter type 2Nondisplaceable uptakeDiabetic subjectsControl subjectsDisease progressionClinical assessmentVMAT2 bindingRenal cortexTotal pancreasDTBZ PETEarly diagnosisInjected dose
2000
Opiate receptor avidity is increased in rhesus monkeys following unilateral optic tract lesion combined with transections of corpus callosum and hippocampal and anterior commissures
Cohen R, Carson R, Saunders R, Doudet D. Opiate receptor avidity is increased in rhesus monkeys following unilateral optic tract lesion combined with transections of corpus callosum and hippocampal and anterior commissures. Brain Research 2000, 879: 1-6. PMID: 11010998, DOI: 10.1016/s0006-8993(00)02528-2.Peer-Reviewed Original ResearchConceptsOpiate receptor avidityPositron emission tomographyReceptor avidityAnterior commissureCorpus callosumKappa-opiate receptor antagonistUnilateral optic tract lesionRhesus monkeysOptic tract lesionsBrain functional activitySplit animalsIpsilateral changesOptic tractTract lesionsUnilateral lesioningPosterior putamenReceptor antagonistHealthy monkeysLateral cortexOccipital cortexMedial cortexVisual deprivationEmission tomographyTransectionCommissurePET evaluation of [18F]FCWAY, an analog of the 5-HT1A receptor antagonist, WAY-100635
Carson R, Lang L, Watabe H, Der M, Adams H, Jagoda E, Herscovitch P, Eckelman W. PET evaluation of [18F]FCWAY, an analog of the 5-HT1A receptor antagonist, WAY-100635. Nuclear Medicine And Biology 2000, 27: 493-497. PMID: 10962257, DOI: 10.1016/s0969-8051(00)00118-9.Peer-Reviewed Original ResearchKinetic Analysis of the 5-HT2A Ligand [11C]MDL 100,907
Watabe H, Channing M, Der M, Adams H, Jagoda E, Herscovitch P, Eckelman W, Carson R. Kinetic Analysis of the 5-HT2A Ligand [11C]MDL 100,907. Cerebrovascular And Brain Metabolism Reviews 2000, 20: 899-909. PMID: 10894173, DOI: 10.1097/00004647-200006000-00002.Peer-Reviewed Original ResearchThe Suitability of [11C]-α-Methyl-L-tryptophan as a Tracer for Serotonin Synthesis: Studies With Dual Administration of [11C] and [14C] Labeled Tracer
Shoaf S, Carson R, Hommer D, Williams W, Higley J, Schmall B, Herscovitch P, Eckelman W, Linnoila M. The Suitability of [11C]-α-Methyl-L-tryptophan as a Tracer for Serotonin Synthesis: Studies With Dual Administration of [11C] and [14C] Labeled Tracer. Cerebrovascular And Brain Metabolism Reviews 2000, 20: 244-252. PMID: 10698060, DOI: 10.1097/00004647-200002000-00004.Peer-Reviewed Original ResearchConceptsPositron emission tomographySerotonin synthesisOverdose of phenobarbitalBrain serotonin synthesis rateIsoflurane-anesthetized rhesus monkeysSerotonin synthesis rateBrain concentrationsSecond doseBrain samplesEmission tomographyRhesus monkeysDual administrationTryptophan uptakePatlak plotSerotoninMinimal conversionAdministrationMonkeysSynthesis rateL-tryptophanPET imagesPET dataTotal countOverdoseExternal quantification
1999
Opiate receptor avidity is reduced bilaterally in rhesus monkeys unilaterally lesioned with MPTP
Cohen R, Carson R, Wyatt R, Doudet D. Opiate receptor avidity is reduced bilaterally in rhesus monkeys unilaterally lesioned with MPTP. Synapse 1999, 33: 282-288. PMID: 10421709, DOI: 10.1002/(sici)1098-2396(19990915)33:4<282::aid-syn5>3.0.co;2-5.Peer-Reviewed Original ResearchMeSH Keywords1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridineAnimalsBasal GangliaBrainCerebellumCerebral CortexDihydroxyphenylalanineFluorine RadioisotopesFunctional LateralityInfusions, ParenteralLimbic SystemMacaca mulattaNaltrexoneNarcotic AntagonistsOrgan SpecificityReceptors, OpioidReceptors, Opioid, kappaReceptors, Opioid, muTomography, Emission-ComputedConceptsOpiate receptor avidityPositron emission tomographyReceptor avidityKappa-opiate receptor antagonistInitial clinical manifestationBasal ganglia functionBasal ganglia circuitsParkinsonian animalsParkinsonian symptomsAnterior putamenClinical manifestationsDopamine innervationGanglia functionReceptor antagonistInternal carotidGanglia circuitsTreatment responsivenessOpiate pathwaysParkinson's diseaseNormal controlsMild lossEmission tomographyRhesus monkeysPET studiesMPTP
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