2013
Synthesis and Evaluation of 11C-LY2795050 as a κ-Opioid Receptor Antagonist Radiotracer for PET Imaging
Zheng MQ, Nabulsi N, Kim SJ, Tomasi G, Lin SF, Mitch C, Quimby S, Barth V, Rash K, Masters J, Navarro A, Seest E, Morris ED, Carson RE, Huang Y. Synthesis and Evaluation of 11C-LY2795050 as a κ-Opioid Receptor Antagonist Radiotracer for PET Imaging. Journal Of Nuclear Medicine 2013, 54: 455-463. PMID: 23353688, PMCID: PMC3775344, DOI: 10.2967/jnumed.112.109512.Peer-Reviewed Original ResearchConceptsKappa-opioid receptorsAntagonist radiotracersSelective kappa opioid receptorPET imagingKOR knockout micePathophysiology of depressionSelective KOR antagonistRadioligand competition binding assaysEx vivo analysisDose-dependent mannerFavorable pharmacokinetic propertiesFull antagonist activityKOR antagonistsPeripheral metabolismKOR agonistsTracer candidatesLY2795050Sprague-DawleyAntagonist tracersKnockout miceSpecific binding signalsCompetition binding assaysRhesus monkeysPharmacokinetic propertiesAntagonist activity
2005
[11C]Glycylsarcosine: synthesis and in vivo evaluation as a PET tracer of PepT2 transporter function in kidney of PepT2 null and wild-type mice
Nabulsi NB, Smith DE, Kilbourn MR. [11C]Glycylsarcosine: synthesis and in vivo evaluation as a PET tracer of PepT2 transporter function in kidney of PepT2 null and wild-type mice. Bioorganic & Medicinal Chemistry 2005, 13: 2993-3001. PMID: 15781409, DOI: 10.1016/j.bmc.2005.02.002.Peer-Reviewed Original ResearchConceptsRapid renal eliminationWild-type micePept2 knockout micePeptide transporter PEPT2Renal eliminationSlow clearanceKnockout miceActive reabsorptionRapid clearancePET tracersPotential radiotracerMouse kidneyPeptide reabsorptionKidneyTransporter PEPT2ClearanceVivo evaluationGly-SarPelvis regionReabsorptionMedullaTransporter functionMicePEPT2Initial uptake