2022
Drug characteristics derived from kinetic modeling: combined 11C-UCB-J human PET imaging with levetiracetam and brivaracetam occupancy of SV2A
Naganawa M, Gallezot J, Finnema S, Maguire R, Mercier J, Nabulsi N, Kervyn S, Henry S, Nicolas J, Huang Y, Chen M, Hannestad J, Klitgaard H, Stockis A, Carson R. Drug characteristics derived from kinetic modeling: combined 11C-UCB-J human PET imaging with levetiracetam and brivaracetam occupancy of SV2A. EJNMMI Research 2022, 12: 71. PMID: 36346513, PMCID: PMC9643320, DOI: 10.1186/s13550-022-00944-5.Peer-Reviewed Original ResearchTime-activity curvesBrain entryDrug concentrationsNon-human primate brainAnti-seizure activitySynaptic vesicle glycoprotein 2APlasma drug concentrationsPrevious human studiesBackgroundAntiepileptic drugsHealthy subjectsBlood samplesHuman studiesLevetiracetamPrimate brainEmission tomography dataBrivaracetamDistribution volumeArterial input functionBrainDrug characteristicsPositron emission tomography dataDrug entryFree fractionDrugsKinetic parameters k1Imaging 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 ResearchConceptsPositron 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 regions
2021
A metabolically stable PET tracer for imaging synaptic vesicle protein 2A: synthesis and preclinical characterization of [18F]SDM-16
Zheng C, Holden D, Zheng MQ, Pracitto R, Wilcox KC, Lindemann M, Felchner Z, Zhang L, Tong J, Fowles K, Finnema SJ, Nabulsi N, Carson RE, Huang Y, Cai Z. A metabolically stable PET tracer for imaging synaptic vesicle protein 2A: synthesis and preclinical characterization of [18F]SDM-16. European Journal Of Nuclear Medicine And Molecular Imaging 2021, 49: 1482-1496. PMID: 34761284, PMCID: PMC8940841, DOI: 10.1007/s00259-021-05597-5.Peer-Reviewed Original ResearchConceptsTest-retest variabilityVolume of distributionCentral nervous systemTime-activity curvesPET tracersCentrum semiovaleSynaptic vesicle protein 2AAbsolute test-retest variabilityWhole central nervous systemNonhuman primate brainPlasma free fractionBrain PET scansHigh specific bindingSpecific bindingNondisplaceable volumePlasma input functionNHP brainOne-tissue compartment modelArterial bloodRegional time-activity curvesPET scansNervous systemPrimate brainMonkey brainPreclinical characterization
2020
Synthesis and Preclinical Evaluation of an 18F‑Labeled Synaptic Vesicle Glycoprotein 2A PET Imaging Probe: [18F]SynVesT‑2
Cai Z, Li S, Zhang W, Pracitto R, Wu X, Baum E, Finnema SJ, Holden D, Toyonaga T, Lin SF, Lindemann M, Shirali A, Labaree DC, Ropchan J, Nabulsi N, Carson RE, Huang Y. Synthesis and Preclinical Evaluation of an 18F‑Labeled Synaptic Vesicle Glycoprotein 2A PET Imaging Probe: [18F]SynVesT‑2. ACS Chemical Neuroscience 2020, 11: 592-603. PMID: 31961649, DOI: 10.1021/acschemneuro.9b00618.Peer-Reviewed Original ResearchConceptsPET imaging probeHigh specific binding signalsNon-human primate brainSynaptic vesicle glycoprotein 2ATraumatic brain injuryPost-traumatic stress disorderMultiple sclerosisBrain injuryParkinson's diseasePreclinical evaluationSpecific binding signalsPrimate brainAlzheimer's diseaseNeuropsychiatric diseasesPresynaptic vesiclesStress disorderDiseaseImaging probeTransmembrane glycoproteinSclerosisPrognosisEpilepsyInjuryStrokeSV2A
2014
Phosphodiesterase 10A PET Radioligand Development Program: From Pig to Human
Plisson C, Weinzimmer D, Jakobsen S, Natesan S, Salinas C, Lin SF, Labaree D, Zheng MQ, Nabulsi N, Marques TR, Kapur S, Kawanishi E, Saijo T, Gunn RN, Carson RE, Rabiner EA. Phosphodiesterase 10A PET Radioligand Development Program: From Pig to Human. Journal Of Nuclear Medicine 2014, 55: 595-601. PMID: 24614221, DOI: 10.2967/jnumed.113.131409.Peer-Reviewed Original ResearchConceptsMP-10Primate brainRadioligand candidatesBaseline PET studyFirst human administrationTissue kineticsNonhuman primate brainRegional binding potentialSelective PDE10A inhibitorDose-dependent mannerOutcome measuresPreclinical studiesBrain regionsFurther evaluationPET studiesPig brainPET tracersPDE10A inhibitorsBrainVivo studiesReference tissueHuman administrationHuman brainAdministrationGood radiochemical yield
2012
Affinity and selectivity of [11C]‐(+)‐PHNO for the D3 and D2 receptors in the rhesus monkey brain in vivo
Gallezot J, Beaver JD, Gunn RN, Nabulsi N, Weinzimmer D, Singhal T, Slifstein M, Fowles K, Ding Y, Huang Y, Laruelle M, Carson RE, Rabiner EA. Affinity and selectivity of [11C]‐(+)‐PHNO for the D3 and D2 receptors in the rhesus monkey brain in vivo. Synapse 2012, 66: 489-500. PMID: 22213512, DOI: 10.1002/syn.21535.Peer-Reviewed Original ResearchConceptsHuman positron emission tomography studiesPositron emission tomography studyRhesus monkey brainEmission tomography studiesDopamine D2 receptorsRegional binding potentialDopamine D3 receptorAnesthetized primatePHNO signalFuture PET studiesInfusion paradigmD2 receptorsMonkey brainPrimate brainVivo affinityRhesus monkeysPET studiesTomography studyD2RPHNOBrainReceptorsD3RRegional fractionHuman brain
2011
Assessing the sensitivity of [11C]p943, a novel 5‐HTIB radioligand, to endogenous serotonin release
Cosgrove KP, Kloczynski T, Nabulsi N, Weinzimmer D, Lin S, Staley JK, Bhagwagar Z, Carson RE. Assessing the sensitivity of [11C]p943, a novel 5‐HTIB radioligand, to endogenous serotonin release. Synapse 2011, 65: 1113-1117. PMID: 21484884, PMCID: PMC3149753, DOI: 10.1002/syn.20942.Peer-Reviewed Original ResearchConceptsFenfluramine-induced changesReceptor occupancyDoses of fenfluraminePositron emission tomography radioligandEndogenous serotonin releaseNonhuman primate brainSerotonin releaseLow doseHigh doseTomography radioligandPrimate brainRhesus monkeysFenfluramineRhesus macaquesPET imagingHuman brainBaboonsDoseDosesRadioligandBrainCurrent studyReceptors