2014
Evaluation of the agonist PET radioligand [11C]GR103545 to image kappa opioid receptor in humans: Kinetic model selection, test–retest reproducibility and receptor occupancy by the antagonist PF-04455242
Naganawa M, Jacobsen LK, Zheng MQ, Lin SF, Banerjee A, Byon W, Weinzimmer D, Tomasi G, Nabulsi N, Grimwood S, Badura LL, Carson RE, McCarthy TJ, Huang Y. Evaluation of the agonist PET radioligand [11C]GR103545 to image kappa opioid receptor in humans: Kinetic model selection, test–retest reproducibility and receptor occupancy by the antagonist PF-04455242. NeuroImage 2014, 99: 69-79. PMID: 24844744, PMCID: PMC4140089, DOI: 10.1016/j.neuroimage.2014.05.033.Peer-Reviewed Original ResearchConceptsKappa-opioid receptorsTest-retest reproducibilityTest-retest variabilityAbsolute test-retest variabilityPF-04455242Time-activity curvesIntra-class coefficientOpioid receptorsRegional time-activity curvesMetabolite-corrected arterial input functionHuman positron emission tomography studiesPositron emission tomography studySelective KOR antagonistEmission tomography studiesReceptor occupancy studiesSuitable reference regionHalf maximal inhibitory concentrationAgonist tracersRegional VTAgonist PET radioligandOral doseKOR antagonistsMaximal inhibitory concentrationOral administrationPreclinical models
2012
Affinity and selectivity of [11C]‐(+)‐PHNO for the D3 and D2 receptors in the rhesus monkey brain in vivo
Gallezot J, Beaver JD, Gunn RN, Nabulsi N, Weinzimmer D, Singhal T, Slifstein M, Fowles K, Ding Y, Huang Y, Laruelle M, Carson RE, Rabiner EA. Affinity and selectivity of [11C]‐(+)‐PHNO for the D3 and D2 receptors in the rhesus monkey brain in vivo. Synapse 2012, 66: 489-500. PMID: 22213512, DOI: 10.1002/syn.21535.Peer-Reviewed Original ResearchConceptsHuman positron emission tomography studiesPositron emission tomography studyRhesus monkey brainEmission tomography studiesDopamine D2 receptorsRegional binding potentialDopamine D3 receptorAnesthetized primatePHNO signalFuture PET studiesInfusion paradigmD2 receptorsMonkey brainPrimate brainVivo affinityRhesus monkeysPET studiesTomography studyD2RPHNOBrainReceptorsD3RRegional fractionHuman brain