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
2019
Development and In Vivo Evaluation of a κ-Opioid Receptor Agonist as a PET Radiotracer with Superior Imaging Characteristics
Li S, Zheng MQ, Naganawa M, Kim S, Gao H, Kapinos M, Labaree D, Huang Y. Development and In Vivo Evaluation of a κ-Opioid Receptor Agonist as a PET Radiotracer with Superior Imaging Characteristics. Journal Of Nuclear Medicine 2019, 60: 1023-1030. PMID: 30630942, PMCID: PMC6604690, DOI: 10.2967/jnumed.118.220517.Peer-Reviewed Original ResearchConceptsMultilinear analysis 1Κ-opioid receptor agonistCentral nervous system diseaseNervous system diseasesHigh specific bindingAgonist tracersGlobus pallidusReceptor abnormalitiesReceptor agonistFrontal cortexSystem diseasesPrimate brainReceptor occupancySuperior imaging characteristicsCingulate cortexAlzheimer's diseasePeak uptakeImaging characteristicsRhesus monkeysOptimal radiotracerPET studiesArterial input functionBlocking studiesPET radiotracersAnalysis 1
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