2024
Novel 18F‑Labeled Benzimidazolone-Based Radioligands as Highly Selective Sigma‑2 Receptor Probes for Tumor Imaging
Wang J, Wang T, Mou T, Yang T, Gao X, An X, Hu B, Zhang J, Zhang X, Deuther-Conrad W, Huang Y, Jia H. Novel 18F‑Labeled Benzimidazolone-Based Radioligands as Highly Selective Sigma‑2 Receptor Probes for Tumor Imaging. Journal Of Medicinal Chemistry 2024, 67: 17392-17406. DOI: 10.1021/acs.jmedchem.4c01315.Peer-Reviewed Original ResearchSmall-animal PET/CTS2 receptorsAnimal PET/CTHigh subtype selectivityGlioma modelCo-administrationPET/CTLung cancerGlioma xenograftsBlocking studiesU87MG xenograftsA549 lung cancerCompound 4U87MG glioma xenograftsTumorTumor imagingReceptorsSubtype selectivityXenograftsRadiochemical yieldRadioligandSigma-2Active uptakeMolar activityU87MG
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 ResearchConceptsAlzheimer'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 typesReceptorsDevelopment of a Highly Specific 18F‑Labeled Radioligand for Imaging of the Sigma‑2 Receptor in Brain Tumors
Wang T, Wang J, Chen L, Zhang X, Mou T, An X, Zhang J, Zhang X, Deuther-Conrad W, Huang Y, Jia H. Development of a Highly Specific 18F‑Labeled Radioligand for Imaging of the Sigma‑2 Receptor in Brain Tumors. Journal Of Medicinal Chemistry 2023, 66: 12840-12857. PMID: 37704582, DOI: 10.1021/acs.jmedchem.3c00735.Peer-Reviewed Original ResearchMicro-PET/CT imagingSigma-2 receptorsTumor uptakeCT imagingClear tumor visualizationGlioma xenograft modelU87MG glioma xenograftsHigh subtype selectivityHigh tumor uptakeHigh specific bindingGlioma xenograftsBrain tumorsXenograft modelTumor visualizationSubtype selectivityReceptorsTumorsRadioligandSpecific bindingGBq/ImagingRadiochemical purityNanomolar affinity
2022
Synthesis and characterization of the two enantiomers of a chiral sigma-1 receptor radioligand: (S)-(+)- and (R)-(-)-[18F]FBFP
Wang T, Zhang Y, Zhang X, Chen L, Zheng M, Zhang J, Brust P, Deuther-Conrad W, Huang Y, Jia H. Synthesis and characterization of the two enantiomers of a chiral sigma-1 receptor radioligand: (S)-(+)- and (R)-(-)-[18F]FBFP. Chinese Chemical Letters 2022, 33: 3543-3548. DOI: 10.1016/j.cclet.2022.03.099.Peer-Reviewed Original ResearchIodonium ylide precursorsMicro-positron emission tomographyHigh brain uptakeBrain uptakeICR miceBrain kineticsBlood ratioReceptor radiotracerReceptor radioligandEmission tomographyFurther evaluationFast clearanceComparable high affinityReceptorsBrainUnlabeled compoundsVivo stabilitySuperior imaging propertiesMolar activityHigh affinityAgonistsAntagonistRatsMiceRadioligand
2001
Imaging Human Mesolimbic Dopamine Transmission With Positron Emission Tomography: I. Accuracy and Precision of D2 Receptor Parameter Measurements in Ventral Striatum
Mawlawi O, Martinez D, Slifstein M, Broft A, Chatterjee R, Hwang D, Huang Y, Simpson N, Ngo K, Van Heertum R, Laruelle M. Imaging Human Mesolimbic Dopamine Transmission With Positron Emission Tomography: I. Accuracy and Precision of D2 Receptor Parameter Measurements in Ventral Striatum. Cerebrovascular And Brain Metabolism Reviews 2001, 21: 1034-1057. PMID: 11524609, DOI: 10.1097/00004647-200109000-00002.Peer-Reviewed Original ResearchConceptsPositron emission tomographyVentral striatumDopamine transmissionReceptor measurementsEmission tomographyMesolimbic dopamine transmissionHigh-resolution magnetic resonanceNonspecific partition coefficientDrugs of abuseDorsal putamenPostmortem studiesVentral putamenDorsal caudateVentral caudateNucleus accumbensConstant infusion methodReceptor availabilityPsychotic statesStriatumReceptorsPutamenCaudateSpecific bindingInfusion methodTomographyVulnerability of positron emission tomography radiotracers to endogenous competition. New insights.
Laruelle M, Huang Y. Vulnerability of positron emission tomography radiotracers to endogenous competition. New insights. Quarterly Journal Of Nuclear Medicine And Molecular Imaging 2001, 45: 124-38. PMID: 11476162.Peer-Reviewed Original ResearchConceptsTransmitter levelsSynaptic dopamine concentrationsPositron emission tomographyDA transmissionD2 receptorsNeurotransmitter systemsPharmacological challengeDevelopment of PETSynaptic transmitter levelsEmission tomographyDopamine concentrationsAcute fluctuationsReceptor traffickingHuman brainRadioligandImaging techniquesVivoEndogenous competitionPETBinding competitionNeurotransmittersBrainReceptors
1998
Chapter 44 Characterization of the Radiolabeled Metabolites of [18F]Altanserin Implications for Kinetic Modeling
Lopresti B, Holt D, Mason N, Huang Y, Ruszkiewicz J, Perevuznik J, Price J, Smith G, Davis J, Mathis C. Chapter 44 Characterization of the Radiolabeled Metabolites of [18F]Altanserin Implications for Kinetic Modeling. 1998, 293-298. DOI: 10.1016/b978-012161340-2/50046-9.Peer-Reviewed Original ResearchVivo positron emission tomography (PET) imaging studiesPositron emission tomography (PET) imaging studiesTomography Imaging StudyPostmortem brain studiesSerotonergic abnormalitiesSerotonergic dysfunctionMajor depressionRadiolabeled metabolitesTherapeutic efficacyAlzheimer's diseaseImaging studiesNeurodegenerative disordersPET studiesReceptorsBrain studiesVivo propertiesDiseaseRadioligandDisordersDysfunctionAltanserinAbnormalitiesNonspecific bindingSchizophrenia