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
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 activity
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