2017
Novel 18F-Labeled κ-Opioid Receptor Antagonist as PET Radiotracer: Synthesis and In Vivo Evaluation of 18F-LY2459989 in Nonhuman Primates
Li S, Cai Z, Zheng MQ, Holden D, Naganawa M, Lin SF, Ropchan J, Labaree D, Kapinos M, Lara-Jaime T, Navarro A, Huang Y. Novel 18F-Labeled κ-Opioid Receptor Antagonist as PET Radiotracer: Synthesis and In Vivo Evaluation of 18F-LY2459989 in Nonhuman Primates. Journal Of Nuclear Medicine 2017, 59: 140-146. PMID: 28747521, PMCID: PMC5750518, DOI: 10.2967/jnumed.117.195586.Peer-Reviewed Original ResearchConceptsPET radiotracersNonhuman primatesTime-activity curvesHigh specific binding signalsΚ-opioid receptor antagonistCentral nervous system disordersFast tissue kineticsBrain time-activity curvesCaudate/putamenNervous system disordersΚ-opioid receptorsRegional binding potentialPeak uptake timeRegional distribution volumesAntagonist radiotracersReceptor antagonistFrontal cortexNovel 18FRegional time-activity curvesSystem disordersNovel radioligandPET scansSpecific binding signalsTemporal cortexMonkey brain
2015
PET imaging evaluation of [18F]DBT-10, a novel radioligand specific to α7 nicotinic acetylcholine receptors, in nonhuman primates
Hillmer AT, Zheng MQ, Li S, Scheunemann M, Lin SF, Holden D, Labaree D, Ropchan J, Teodoro R, Deuther-Conrad W, Carson RE, Brust P, Huang Y. PET imaging evaluation of [18F]DBT-10, a novel radioligand specific to α7 nicotinic acetylcholine receptors, in nonhuman primates. European Journal Of Nuclear Medicine And Molecular Imaging 2015, 43: 537-547. PMID: 26455500, PMCID: PMC4733418, DOI: 10.1007/s00259-015-3209-0.Peer-Reviewed Original ResearchConceptsPurposePositron emission tomographyDose-dependent blockadeStandardized uptake valueΑ7 nicotinic acetylcholine receptorNonhuman primatesPeak standardized uptake valueBaseline PET scanParent fractionEx vivo analysisPlasma free fractionNicotinic acetylcholine receptorsTotal distribution volumeBrain tissue samplesRegional rank orderTwo-tissue compartment modelSpecific radioligandFrontal cortexOccipital cortexNovel radioligandPET scansArterial plasmaAcetylcholine receptorsUptake valueAlzheimer's diseaseBrain tissue
2014
Relationship Between Glycine Transporter 1 Inhibition as Measured with Positron Emission Tomography and Changes in Cognitive Performances in Nonhuman Primates
Castner SA, Murthy NV, Ridler K, Herdon H, Roberts BM, Weinzimmer DP, Huang Y, Zheng MQ, Rabiner EA, Gunn RN, Carson RE, Williams GV, Laruelle M. Relationship Between Glycine Transporter 1 Inhibition as Measured with Positron Emission Tomography and Changes in Cognitive Performances in Nonhuman Primates. Neuropsychopharmacology 2014, 39: 2742-2749. PMID: 24487737, PMCID: PMC4200505, DOI: 10.1038/npp.2014.4.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBenzamidesBrainCarbon RadioisotopesCentral Nervous System AgentsExcitatory Amino Acid AntagonistsFemaleGlycine Plasma Membrane Transport ProteinsKetamineMacaca mulattaMaleMemory, Short-TermNeuropsychological TestsN-MethylaspartatePositron-Emission TomographyRadiopharmaceuticalsSpatial MemoryTetrahydronaphthalenesConceptsOrg 25935GlyT-1 inhibitorsNMDA hypofunctionN-methyl-D-aspartate receptorsPotential therapeutic effectsTreatment of schizophreniaPositron emission tomography (PET) radiotracerPositron emission tomographyNMDA transmissionGlutamatergic transmissionControl conditionKetamine administrationNMDA receptorsTherapeutic effectExtracellular glycineExtracellular levelsGlyT-1Emission tomographyMemory deficitsRhesus monkeysTomography radiotracerNonhuman primatesLines of evidenceHypofunctionCognitive performance