2023
Development 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 affinity18F-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
1998
Stereoconservative synthesis of the enantiomerically pure precursors of [11C](+)‐McN 5652 and [11C](−)‐McN 5652
Huang Y, Mahmood K, Simpson N, Mason N, Mathis C. Stereoconservative synthesis of the enantiomerically pure precursors of [11C](+)‐McN 5652 and [11C](−)‐McN 5652. Journal Of Labelled Compounds And Radiopharmaceuticals 1998, 41: 9-17. DOI: 10.1002/(sici)1099-1344(199801)41:1<9::aid-jlcr47>3.0.co;2-8.Peer-Reviewed Original ResearchBenzoyl thioesterTartrate saltFinal productOne-pot deprotectionSynthetic routeConvenient precursorsReaction sequenceSynthesis yieldDetectable isomerizationPurification procedureThioestersThioethersKey stepSubsequent formationSpecific activityCi/High specific activitySaltHPLC analysisPrecursorsRadiochemical purityS-methylationDeprotectionIsomerizationRadiosynthesis