Synthesis and Evaluation of¹¹C-LY2795050 as a κ-Opioid Receptor Antagonist Radiotracer for PET Imaging

Abstract

(11)C-LY2795050 displayed favorable pharmacokinetic properties and binding profiles in vivo and therefore is a suitable ligand for imaging the KOR in primates. This newly developed KOR antagonist tracer has since been advanced to PET imaging of KOR in humans and constitutes the first successful KOR antagonist radiotracer.