2025
Novel F-18-labeled Tracers of Sympathetic Function for Improved Risk Stratification and Clinical Outcomes
Zohora F, Nazari M, Sinusas A. Novel F-18-labeled Tracers of Sympathetic Function for Improved Risk Stratification and Clinical Outcomes. Current Cardiology Reports 2025, 27: 61. PMID: 40009333, DOI: 10.1007/s11886-025-02197-9.Peer-Reviewed Original ResearchConceptsSudden cardiac deathImplantable cardioverter defibrillatorPositron emission tomographyImplantable cardioverter defibrillator placementMyocardial sympathetic denervationRisk stratificationSympathetic denervationIschemic heart diseaseHeart failurePrevention of sudden cardiac deathRisk stratification of patientsHeart diseaseOptimal risk stratificationLow ejection fractionStratification of patientsSympathetic nerve densityImprove risk stratificationHeart failure patientsPositron emission tomography radiotracersPredicting sudden cardiac deathPositron emission tomography tracersPrognostic benefitEjection fractionClinically practical approachNerve densityPET Imaging of Sphingosine-1-Phosphate Receptor 1 with [18F]TZ4877 in Nonhuman Primates
Gu J, Zheng M, Holden D, Fowles K, Qiu L, Felchner Z, Zhang L, Ropchan J, Gropler R, Carson R, Tu Z, Huang Y, Hillmer A. PET Imaging of Sphingosine-1-Phosphate Receptor 1 with [18F]TZ4877 in Nonhuman Primates. Molecular Imaging And Biology 2025, 27: 54-63. PMID: 39779653, DOI: 10.1007/s11307-024-01979-x.Peer-Reviewed Original ResearchConceptsSphingosine-1-phosphate receptor 1Absorbed radiation dose estimatesReceptor 1Nonhuman primatesFree fractionPlasma free fractionRadiation dose estimatesMetabolite-corrected input functionF-18 labeled radiotracersArterial blood samplesCritical organsPET/CT systemBolus injectionF-18Anesthetized nonhuman primatesDosimetry studiesHuman studiesDose estimatesVT/fPPET imaging dataS1PR1PET imagingInput functionBlood samplesPonesimodSelective Mu-Opioid Receptor Imaging Using 18F‑Labeled Carfentanils
Lee S, Pearson T, Dhaynaut M, MacDonagh A, Wey H, Wilks M, Roth B, Hooker J, Normandin M. Selective Mu-Opioid Receptor Imaging Using 18F‑Labeled Carfentanils. Journal Of Medicinal Chemistry 2025, 68: 1632-1644. PMID: 39772615, DOI: 10.1021/acs.jmedchem.4c02287.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBrainFentanylFluorine RadioisotopesHumansMaleMicePositron-Emission TomographyRadiopharmaceuticalsRatsReceptors, Opioid, muTissue DistributionConceptsMu-opioid receptorsPositron emission tomographyIn vivo PET scansCarbon-11Neurobiological studiesCopper-mediated radiofluorinationMu-opioidReceptor imagingPET scansBrain uptakeFavorable pharmacokineticsImaging evaluationHigh molar activityMass doseEmission tomographyHalf-life of fluorine-18Synthetic opioidsFluorine-18Half-lifeIn vitro binding assaysBinding assaysClinical research useMolar activityCarfentanilResearch useIn Vivo Head-to-Head Comparison of [18F]GTP1 with [18F]MK-6240 and [18F]PI-2620 in Alzheimer Disease
Olafson E, Tonietto M, Klein G, Teng E, Stephens A, Russell D, Pickthorn K, Bohorquez S. In Vivo Head-to-Head Comparison of [18F]GTP1 with [18F]MK-6240 and [18F]PI-2620 in Alzheimer Disease. Journal Of Nuclear Medicine 2025, 66: jnumed.124.268623. PMID: 39746756, PMCID: PMC11800736, DOI: 10.2967/jnumed.124.268623.Peer-Reviewed Original ResearchConceptsAlzheimer's diseaseAccumulation of tau neurofibrillary tanglesTau neurofibrillary tanglesOff-target regionsNeurofibrillary tanglesTau pathologyTau-PET signalTau PET tracersBinding profilesTau-PETMild ADNormal cognitionBraak regionsHead-to-head studiesAD patientsTauMagnitude of uptakeTracer bindingAlzheimerTarget region
2024
Comparative Kidney Uptake of Nanobody-Based PET Tracers Labeled with Various Fluorine-18-Labeled Prosthetic Groups
Olkowski C, Basuli F, Fernandes B, Ghaemi B, Shi J, Zhang H, Farber J, Escorcia F, Choyke P, Jacobson O. Comparative Kidney Uptake of Nanobody-Based PET Tracers Labeled with Various Fluorine-18-Labeled Prosthetic Groups. Molecular Pharmaceutics 2024, 22: 533-543. PMID: 39680709, DOI: 10.1021/acs.molpharmaceut.4c01101.Peer-Reviewed Original ResearchPlasma Glial Fibrillary Acid Protein and Phosphorated Tau 181 Association with Presynaptic Density-Dependent Tau Pathology at 18F-SynVesT-1 Brain PET Imaging.
Wu J, Li B, Wang J, Huang Q, Chen X, You Z, He K, Guo Q, Li S, Huang Y, Guo T, Dai W, Xiang W, Chen W, Yang D, Zhao J, Guan Y, Xie F. Plasma Glial Fibrillary Acid Protein and Phosphorated Tau 181 Association with Presynaptic Density-Dependent Tau Pathology at 18F-SynVesT-1 Brain PET Imaging. Radiology 2024, 313: e233019. PMID: 39560478, PMCID: PMC11605102, DOI: 10.1148/radiol.233019.Peer-Reviewed Original ResearchConceptsP-tau-181Alzheimer's diseaseAD-related pathologyAmyloid-bPhosphor-tauTau pathologySynaptic densityTau accumulationSynaptic lossTauTau-PETDecreased synaptic densityGlial fibrillary acidic proteinPlasma glial fibrillary acidic proteinCortical thicknessAcidic proteinFibrillary acidic proteinRuijin HospitalProspective studyRelationship of plasmaBlood assayBlood markersPET/MRIBrain PET imagingPET imagingIdentifying G6PC3 as a Potential Key Molecule in Hypoxic Glucose Metabolism of Glioblastoma Derived from the Depiction of 18F‐Fluoromisonidazole and 18F‐Fluorodeoxyglucose Positron Emission Tomography
Okamoto M, Yamaguchi S, Sawaya R, Echizenya S, Ishi Y, Kaneko S, Motegi H, Toyonaga T, Hirata K, Fujimura M. Identifying G6PC3 as a Potential Key Molecule in Hypoxic Glucose Metabolism of Glioblastoma Derived from the Depiction of 18F‐Fluoromisonidazole and 18F‐Fluorodeoxyglucose Positron Emission Tomography. BioMed Research International 2024, 2024: 2973407. PMID: 38449509, PMCID: PMC10917478, DOI: 10.1155/2024/2973407.Peer-Reviewed Original ResearchConceptsPositron emission tomographyF-FDGMRNA expressionOverall survivalGlucose metabolismF-FDG positron emission tomographyAssociated with poor overall survivalProtein expressionEmission tomographyGross total resectionPotential key moleculesFluorine-18 fluorodeoxyglucoseHypoxic conditionsDegree of glucose metabolismMolecular mechanisms of glucose metabolismAggressive primary brain tumorPoor overall survivalPrimary brain tumorKey moleculesTotal resectionPreoperative examinationIntratumoral hypoxiaPrognostic valuePoor prognosisBiomarkers of glioblastoma
2023
18F-Labeled o‑aminopyridyl alkynyl radioligands targeting colony-stimulating factor 1 receptor for neuroinflammation imaging
An X, Wang J, Tong L, Zhang X, Fu H, Zhang J, Xie H, Huang Y, Jia H. 18F-Labeled o‑aminopyridyl alkynyl radioligands targeting colony-stimulating factor 1 receptor for neuroinflammation imaging. Bioorganic & Medicinal Chemistry 2023, 83: 117233. PMID: 36933438, DOI: 10.1016/j.bmc.2023.117233.Peer-Reviewed Original ResearchConceptsBrain of lipopolysaccharideMale ICR miceModerate brain uptakeFactor 1 receptorColony-stimulating factor 1 receptorBrain uptakeICR miceGBq/Metabolic stability studiesID/Neuroinflammation imagingMouse brainBiodistribution studiesNanomolar inhibitory potencyReceptor ligandsMiceInhibitory potencySpecific bindingBrainCSF-1RRadiochemical purityMolar activityDetailed radiosynthesis of [18F]mG4P027 as a positron emission tomography radiotracer for mGluR4
Wang J, Moon S, Cleary M, Shoup T, Fakhri G, Zhang Z, Brownell A. Detailed radiosynthesis of [18F]mG4P027 as a positron emission tomography radiotracer for mGluR4. Journal Of Labelled Compounds And Radiopharmaceuticals 2023, 66: 34-40. PMID: 36593743, PMCID: PMC9985952, DOI: 10.1002/jlcr.4011.Peer-Reviewed Original Research
2021
In vivo imaging of mGlu5 receptor expression in humans with Fragile X Syndrome towards development of a potential biomarker
Mody M, Petibon Y, Han P, Kuruppu D, Ma C, Yokell D, Neelamegam R, Normandin M, Fakhri G, Brownell A. In vivo imaging of mGlu5 receptor expression in humans with Fragile X Syndrome towards development of a potential biomarker. Scientific Reports 2021, 11: 15897. PMID: 34354107, PMCID: PMC8342610, DOI: 10.1038/s41598-021-94967-y.Peer-Reviewed Original ResearchConceptsFragile X syndromeFragile X mental retardation proteinX syndromeLoss of fragile X mental retardation proteinMGlu5 receptor expressionMetabotropic glutamate subtype 5 receptorsDrug occupancy studiesSignificant group differencesFragile X mental retardationHealthy controlsAnterior cingulateMGluR5 availabilityVisuospatial processingMGlu5 receptorsOlfactory cortexBrain areasGroup differencesRetardation proteinGlutamate signalingImages of maleNeurodevelopmental disordersExcessive glutamate signalingGender-matched controlsDisordersMGluR5Effect of age on brain metabotropic glutamate receptor subtype 5 measured with [18F]FPEB PET
Mecca AP, Rogers K, Jacobs Z, McDonald JW, Michalak HR, DellaGioia N, Zhao W, Hillmer AT, Nabulsi N, Lim K, Ropchan J, Huang Y, Matuskey D, Esterlis I, Carson RE, van Dyck CH. Effect of age on brain metabotropic glutamate receptor subtype 5 measured with [18F]FPEB PET. NeuroImage 2021, 238: 118217. PMID: 34052464, PMCID: PMC8378132, DOI: 10.1016/j.neuroimage.2021.118217.Peer-Reviewed Original ResearchMeSH KeywordsAdolescentAdultAgedAged, 80 and overAgingBrain ChemistryFemaleFluorine RadioisotopesFluorodeoxyglucose F18Gray MatterHippocampusHumansMagnetic Resonance ImagingMaleMiddle AgedNeuroimagingOrgan SizePositron-Emission TomographyRadiopharmaceuticalsReceptor, Metabotropic Glutamate 5Young AdultConceptsMetabotropic glutamate receptor subtype 5MGluR5 availabilityMultiple brain regionsTissue lossSubtype 5Association cortexPrimary analysisBrain regionsAge-related molecular changesBrain glutamatergic systemBrain tissue lossNon-significant trendPartial volume correctionPositron emission tomographyBrain mGluR5Effect of ageAge-related declineGlutamatergic systemInverse associationTissue alterationsDistribution volumeEmission tomographyOlder ageCognitive functionExploratory analysisBinding characteristics of [18F]PI-2620 distinguish the clinically predicted tau isoform in different tauopathies by PET
Song M, Beyer L, Kaiser L, Barthel H, van Eimeren T, Marek K, Nitschmann A, Scheifele M, Palleis C, Respondek G, Kern M, Biechele G, Hammes J, Bischof G, Barbe M, Onur Ö, Jessen F, Saur D, Schroeter M, Rumpf J, Rullmann M, Schildan A, Patt M, Neumaier B, Barret O, Madonia J, Russell D, Stephens A, Mueller A, Roeber S, Herms J, Bötzel K, Danek A, Levin J, Classen J, Höglinger G, Bartenstein P, Villemagne V, Drzezga A, Seibyl J, Sabri O, Boening G, Ziegler S, Brendel M. Binding characteristics of [18F]PI-2620 distinguish the clinically predicted tau isoform in different tauopathies by PET. Cerebrovascular And Brain Metabolism Reviews 2021, 41: 2957-2972. PMID: 34044665, PMCID: PMC8545042, DOI: 10.1177/0271678x211018904.Peer-Reviewed Original ResearchAssessment of test-retest reproducibility of [18F]SynVesT-1, a novel radiotracer for PET imaging of synaptic vesicle glycoprotein 2A
Li S, Naganawa M, Pracitto R, Najafzadeh S, Holden D, Henry S, Matuskey D, Emery PR, Cai Z, Ropchan J, Nabulsi N, Carson RE, Huang Y. Assessment of test-retest reproducibility of [18F]SynVesT-1, a novel radiotracer for PET imaging of synaptic vesicle glycoprotein 2A. European Journal Of Nuclear Medicine And Molecular Imaging 2021, 48: 1327-1338. PMID: 33416954, DOI: 10.1007/s00259-020-05149-3.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBrainFluorine RadioisotopesGlycoproteinsPositron-Emission TomographyPyridinesPyrrolidinonesRadiopharmaceuticalsReproducibility of ResultsSynaptic VesiclesConceptsTest-retest reproducibilityTime-activity curvesBPND valuesNonhuman primatesAbsolute test-retest variabilitySynaptic vesicle glycoprotein 2AHigh brain uptakeNon-displaceable binding potentialExcellent test-retest reproducibilityGray matter areasHealthy human subjectsHigh uptakeTest-retest variabilityDynamic PET scanningTest-retest reliabilityBrain uptakeDistribution volume valuesCentrum semiovaleUrinary bladderOne-tissue compartment modelMaximum SUVPET scanningPET scansTracer uptakeBrain disorders
2020
Quantification of SV2A Binding in Rodent Brain Using [18F]SynVesT-1 and PET Imaging
Sadasivam P, Fang XT, Toyonaga T, Lee S, Xu Y, Zheng MQ, Spurrier J, Huang Y, Strittmatter SM, Carson RE, Cai Z. Quantification of SV2A Binding in Rodent Brain Using [18F]SynVesT-1 and PET Imaging. Molecular Imaging And Biology 2020, 23: 372-381. PMID: 33258040, PMCID: PMC8105262, DOI: 10.1007/s11307-020-01567-9.Peer-Reviewed Original ResearchConceptsBrain stemAlzheimer's diseaseMin postinjectionAnimal modelsAPP/PS1 miceReference regionStandardized uptake value ratioDynamic PET imaging dataUptake value ratioRodent brain tissueStatic PET scansDifferent imaging windowsPET imaging dataWild-type controlsReference tissue modelPS1 miceAD pathogenesisTherapeutic effectMouse modelRodent modelsLittermate controlsPET scansRodent brainPreclinical imaging studiesTherapeutic drug efficacyEvaluation of the potassium channel tracer [18F]3F4AP in rhesus macaques
Guehl N, Ramos-Torres K, Linnman C, Moon S, Dhaynaut M, Wilks M, Han P, Ma C, Neelamegam R, Zhou Y, Popko B, Correia J, Reich D, Fakhri G, Herscovitch P, Normandin M, Brugarolas P. Evaluation of the potassium channel tracer [18F]3F4AP in rhesus macaques. Cerebrovascular And Brain Metabolism Reviews 2020, 41: 1721-1733. PMID: 33090071, PMCID: PMC8221756, DOI: 10.1177/0271678x20963404.Peer-Reviewed Original ResearchMeSH KeywordsAminopyridinesAnimalsBrain InjuriesFluorine RadioisotopesMacaca mulattaMalePositron-Emission TomographyPotassium ChannelsRadioactive TracersRadiopharmaceuticalsConceptsFocal brain injuryMyelin repair therapyContributions of demyelinationDrivers of disabilityImaging demyelinationBrain injuryMeasurements of molecular changesTool's sensitivity to changesLower myelin contentDemyelinating lesionsNeuronal conductionImpaired conductionDemyelinationBrain penetrationGold standardRhesus macaquesInjured areaMultiple sclerosisMolecular changesMyelin sheathNeurological diseasesHigh metabolic stabilityMRI methodsMRIInjuryPositron Emission Tomography Imaging Evaluation of a Novel 18F‑Labeled Sigma‑1 Receptor Radioligand in Cynomolgus Monkeys
Jia H, Cai Z, Holden D, He Y, Lin SF, Li S, Baum E, Shirali A, Kapinos M, Gao H, Ropchan J, Huang Y. Positron Emission Tomography Imaging Evaluation of a Novel 18F‑Labeled Sigma‑1 Receptor Radioligand in Cynomolgus Monkeys. ACS Chemical Neuroscience 2020, 11: 1673-1681. PMID: 32356969, DOI: 10.1021/acschemneuro.0c00171.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBrainFluorine RadioisotopesMacaca fascicularisPositron-Emission TomographyRadiopharmaceuticalsReceptors, sigmaA Novel Radioligand Reveals Tissue Specific Pharmacological Modulation of Glucocorticoid Receptor Expression with Positron Emission Tomography
Huang Y, Zhao N, Wang Y, Truillet C, Wei J, Blecha J, VanBrocklin H, Seo Y, Sayeed M, Feldman B, Aggarwal R, Behr S, Shao H, Wilson D, Villanueva-Meyer J, Gestwicki J, Evans M. A Novel Radioligand Reveals Tissue Specific Pharmacological Modulation of Glucocorticoid Receptor Expression with Positron Emission Tomography. ACS Chemical Biology 2020, 15: 1381-1391. PMID: 32255605, PMCID: PMC8031368, DOI: 10.1021/acschembio.9b01043.Peer-Reviewed Original ResearchConceptsPositron emission tomographyBind GRGlucocorticoid receptorEmission tomographyGR agonist dexamethasoneGlucocorticoid receptor expressionGR modulatorsAdipose tissue of miceGR expression levelsTissues of miceReceptor expressionAgonist dexamethasoneArylboronic acid pinacol estersGR expressionKnockout miceGR signalingNuclear hormone receptorsPharmacological modulationHormone receptorsSevere diseaseAdipose tissueTissue levelsDecay corrected radiochemical yieldMiceHistorical screeningSynthesis and Characterization of Fluorine-18-Labeled N‑(4-Chloro-3-((fluoromethyl‑d 2)thio)phenyl)picolinamide for Imaging of mGluR4 in Brain
Wang J, Qu X, Shoup T, Yuan G, Afshar S, Pan C, Zhu A, Choi J, Kang H, Poutiainen P, Fakhri G, Zhang Z, Brownell A. Synthesis and Characterization of Fluorine-18-Labeled N‑(4-Chloro-3-((fluoromethyl‑d 2)thio)phenyl)picolinamide for Imaging of mGluR4 in Brain. Journal Of Medicinal Chemistry 2020, 63: 3381-3389. PMID: 32081008, PMCID: PMC7261135, DOI: 10.1021/acs.jmedchem.0c00201.Peer-Reviewed Original ResearchConceptsDrug-like propertiesMethylthio analoguePotential ligandsMetabolic stabilityPositron emission tomographyRadiochemical yieldMolar activityDose-dependent blocking effectPositron emission tomography imaging studiesMethylthioPAM activityBrain regionsMale Sprague Dawley ratsLigandEx vivo biodistribution studiesRadiosynthesisSprague Dawley ratsBrainMGluR4SynthesisAnaloguesEmission tomographyImaging studies
2019
Positron-Emission Tomographic Imaging of a Fluorine 18–Radiolabeled Poly(ADP-Ribose) Polymerase 1 Inhibitor Monitors the Therapeutic Efficacy of Talazoparib in SCLC Patient–Derived Xenografts
Laird J, Lok B, Carney B, Kossatz S, de Stanchina E, Reiner T, Poirier J, Rudin C. Positron-Emission Tomographic Imaging of a Fluorine 18–Radiolabeled Poly(ADP-Ribose) Polymerase 1 Inhibitor Monitors the Therapeutic Efficacy of Talazoparib in SCLC Patient–Derived Xenografts. Journal Of Thoracic Oncology 2019, 14: 1743-1752. PMID: 31195178, PMCID: PMC6764879, DOI: 10.1016/j.jtho.2019.05.032.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsApoptosisCell ProliferationFemaleFluorine RadioisotopesHumansLung NeoplasmsMiceMice, Inbred NODMice, SCIDPhthalazinesPoly (ADP-Ribose) Polymerase-1Poly(ADP-ribose) Polymerase InhibitorsPositron-Emission TomographyRadiopharmaceuticalsSmall Cell Lung CarcinomaTumor Cells, CulturedXenograft Model Antitumor AssaysConceptsPatient-derived xenograftsPositron emission tomographicPARP inhibitorsTherapeutic efficacyTarget engagementPositron emission tomographic imagingDifferential therapeutic efficacyTumor radiotracer uptakeTumor growth inhibitionEnzyme-linked immunosorbentDose-dependent mannerFluorine-18Oral talazoparibMultiple dosesSingle dosesTotal tumorsPolymerase-1 (PARP-1) inhibitorsPET uptakeRadiotracer uptakeInhibitor of polyIndividual tumorsPET/Drug efficacyTalazoparib treatmentPromising therapeuticsSynthesis 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 agent
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