2019
Novel Kappa Opioid Receptor Agonist as Improved PET Radiotracer: Development and in Vivo Evaluation
Li S, Zheng M, Naganawa M, Gao H, Pracitto R, Shirali A, Lin SF, Teng JK, Ropchan J, Huang Y. Novel Kappa Opioid Receptor Agonist as Improved PET Radiotracer: Development and in Vivo Evaluation. Molecular Pharmaceutics 2019, 16: 1523-1531. PMID: 30726092, DOI: 10.1021/acs.molpharmaceut.8b01209.Peer-Reviewed Original ResearchConceptsKappa-opioid receptorsAgonist radiotracerOpioid receptorsNovel kappa-opioid receptor agonistKappa-opioid receptor agonistFast tissue kineticsNonselective opioid receptorTissue kineticsOpioid receptor agonistsDose-dependent mannerMultilinear analysis-1 (MA1) methodHigh specific bindingSpecific bindingAgonist tracersHigh binding regionsReceptor agonistRegional time-activity curvesSpecific binding signalsTime-activity curvesArterial activityImproved imaging propertiesRhesus monkeysDrug abusePET radiotracersParent fraction
2007
High Occupancy of Sigma-1 Receptors in the Human Brain after Single Oral Administration of Fluvoxamine: A Positron Emission Tomography Study Using [11C]SA4503
Ishikawa M, Ishiwata K, Ishii K, Kimura Y, Sakata M, Naganawa M, Oda K, Miyatake R, Fujisaki M, Shimizu E, Shirayama Y, Iyo M, Hashimoto K. High Occupancy of Sigma-1 Receptors in the Human Brain after Single Oral Administration of Fluvoxamine: A Positron Emission Tomography Study Using [11C]SA4503. Biological Psychiatry 2007, 62: 878-883. PMID: 17662961, DOI: 10.1016/j.biopsych.2007.04.001.Peer-Reviewed Original ResearchConceptsSelective serotonin reuptake inhibitorsSigma-1 receptorMechanism of actionPositron emission tomography studySerotonin reuptake inhibitorsHuman brainHealthy male volunteersSingle oral administrationEmission tomography studiesSelective sigma-1 receptor ligandSigma-1 receptor ligandsDose-dependent mannerReuptake inhibitorsSingle doseTherapeutic dosesOral administrationMale volunteersArterial bloodPET scansPsychiatric diseasesFluvoxamineGene polymorphismsBrain regionsFunctional polymorphismsTomography study