2025
Correction: Quantifying VMAT2 target occupancy at effective valbenazine doses and comparing to a novel VMAT2 inhibitor: a translational PET study
Terry-Lorenzo R, Albrecht D, Crouch S, Wong R, Loewen G, Giri N, Skor H, Lin K, Sandiego C, Pajonas M, Rabiner E, Gunn R, Russell D, Haubenberger D. Correction: Quantifying VMAT2 target occupancy at effective valbenazine doses and comparing to a novel VMAT2 inhibitor: a translational PET study. Neuropsychopharmacology 2025, 50: 719-719. PMID: 39843851, PMCID: PMC11845734, DOI: 10.1038/s41386-025-02055-w.Peer-Reviewed Original ResearchQuantifying VMAT2 target occupancy at effective valbenazine doses and comparing to a novel VMAT2 inhibitor: a translational PET study
Terry-Lorenzo R, Albrecht D, Crouch S, Wong R, Loewen G, Giri N, Skor H, Lin K, Sandiego C, Pajonas M, Rabiner E, Gunn R, Russell D, Haubenberger D. Quantifying VMAT2 target occupancy at effective valbenazine doses and comparing to a novel VMAT2 inhibitor: a translational PET study. Neuropsychopharmacology 2025, 50: 1093-1101. PMID: 39757283, PMCID: PMC12089418, DOI: 10.1038/s41386-024-02046-3.Peer-Reviewed Original ResearchVesicular monoamine transporter type 2Treatment of tardive dyskinesiaPositron emission tomographyVesicular monoamine transporter type 2 inhibitorsTarget occupancyTreatment of chorea associated with Huntington's diseaseTreatment of TDChorea associated with Huntington's diseaseCentral nervous systemTardive dyskinesiaVMAT2 inhibitorsValbenazineClinical developmentEffect sizeAssociated with efficacyPET studiesEmission tomographyGold standard biomarkerDosing regimensClinical benefitDaily doseHuntington's diseaseActive metabolitePlasma concentrationsAcceptable dose
2021
Brain target occupancy of LY3372689, an inhibitor of the O‐GlcNAcase (OGA) enzyme, following administration of single and multiple doses to healthy volunteers
Kielbasa W, Shcherbinin S, Goldsmith P, Phipps K, Biglan K, Mancini M, Russell D, Constantinescu C, Gunn R, Nuthall H, Mergott D, Lowe S, Collins E. Brain target occupancy of LY3372689, an inhibitor of the O‐GlcNAcase (OGA) enzyme, following administration of single and multiple doses to healthy volunteers. Alzheimer's & Dementia 2021, 17 DOI: 10.1002/alz.057774.Peer-Reviewed Original ResearchHealthy volunteersEnzyme occupancyPET scansSingle doseMultiple-dose clinical studiesPost-dose intervalPositron emission tomography radioligandBaseline PET scanLonger clinical trialsTarget occupancyTau-related diseasesMultiple dosesMultiple dosingClinical trialsPlasma pharmacokineticsClinical studiesEfficacy trialsSD studiesDose selectionTomography radioligandEnzyme inhibitorsPotential treatmentAlzheimer's diseasePET studiesTarget engagement
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
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