2020
First-in-Human Assessment of 11C-LSN3172176, an M1 Muscarinic Acetylcholine Receptor PET Radiotracer
Naganawa M, Nabulsi N, Henry S, Matuskey D, Lin SF, Slieker L, Schwarz AJ, Kant N, Jesudason C, Ruley K, Navarro A, Gao H, Ropchan J, Labaree D, Carson RE, Huang Y. First-in-Human Assessment of 11C-LSN3172176, an M1 Muscarinic Acetylcholine Receptor PET Radiotracer. Journal Of Nuclear Medicine 2020, 62: 553-560. PMID: 32859711, PMCID: PMC8049371, DOI: 10.2967/jnumed.120.246967.Peer-Reviewed Original ResearchConceptsSimplified reference tissue modelM1 receptorsHealthy subjectsMuscarinic acetylcholine receptor subtype M1Distribution volumePET radiotracersAbsolute test-retest variabilityExcellent test-retest reproducibilityReference tissue model 2Total distribution volumeSuitable reference regionTest-retest reproducibilityTest-retest variabilityReference regionTest-retest protocolNondisplaceable distribution volumeReference tissue modelTest-retest studySubtypes M1Preclinical studiesRegional time-activity curvesAcetylcholine concentrationHuman studiesReceptor occupancyTime-activity curves
2019
Synthesis and in vivo evaluation of [18F]UCB-J for PET imaging of synaptic vesicle glycoprotein 2A (SV2A)
Li S, Cai Z, Zhang W, Holden D, Lin SF, Finnema SJ, Shirali A, Ropchan J, Carre S, Mercier J, Carson RE, Nabulsi N, Huang Y. Synthesis and in vivo evaluation of [18F]UCB-J for PET imaging of synaptic vesicle glycoprotein 2A (SV2A). European Journal Of Nuclear Medicine And Molecular Imaging 2019, 46: 1952-1965. PMID: 31175396, PMCID: PMC6810698, DOI: 10.1007/s00259-019-04357-w.Peer-Reviewed Original ResearchConceptsSynaptic vesicle glycoprotein 2AHigh specific binding signalsNonhuman primatesPET imagingHigh brain uptakeRegional distribution volumesBrain uptakeSynaptic densityOne-tissue compartment modelExcellent imaging agentRegional time-activity curvesVivo biomarkersArterial samplesSpecific binding signalsPsychiatric diseasesTime-activity curvesAlzheimer's diseaseDistribution volumeNeuropsychiatric disordersRadioactive metabolitesRhesus monkeysPET radiotracersVivo evaluationDiseaseImaging agentEvaluation 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
2017
A modification to improve the reliability of [11C]CN− production in the GE radiochemistry system
Labaree DC, Ropchan JR, Nabulsi N, Huang Y. A modification to improve the reliability of [11C]CN− production in the GE radiochemistry system. Journal Of Labelled Compounds And Radiopharmaceuticals 2017, 60: 592-595. PMID: 28833348, DOI: 10.1002/jlcr.3540.Peer-Reviewed Original ResearchEvaluation 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 1
2016
Synthesis 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
2013
Determination of In Vivo Bmax and Kd for 11C-GR103545, an Agonist PET Tracer for κ-Opioid Receptors: A Study in Nonhuman Primates
Tomasi G, Nabulsi N, Zheng MQ, Weinzimmer D, Ropchan J, Blumberg L, Brown-Proctor C, Ding YS, Carson RE, Huang Y. Determination of In Vivo Bmax and Kd for 11C-GR103545, an Agonist PET Tracer for κ-Opioid Receptors: A Study in Nonhuman Primates. Journal Of Nuclear Medicine 2013, 54: 600-608. PMID: 23424192, PMCID: PMC3775350, DOI: 10.2967/jnumed.112.112672.Peer-Reviewed Original Research
2010
[11C]GR103545: novel one-pot radiosynthesis with high specific activity
Nabulsi NB, Zheng MQ, Ropchan J, Labaree D, Ding YS, Blumberg L, Huang Y. [11C]GR103545: novel one-pot radiosynthesis with high specific activity. Nuclear Medicine And Biology 2010, 38: 215-221. PMID: 21315277, DOI: 10.1016/j.nucmedbio.2010.08.014.Peer-Reviewed Original Research