Synthesis and Evaluation of a Full-Agonist Orvinol for PET-Imaging of Opioid Receptors: [C-11]PEO

摘要

Antagonist radiotracers have shown only a low sensitivity for detecting competition from high-efficacy agonists at opioid receptors (ORs) in vivo. We report that [C-11]PEO binds with high affinity to mu and kappa-opioid receptors, is a full agonist, and concentrates in brain regions of rats with a high density of the mu-OR after intravenous injection. Blocking studies with mu and kappa-OR selective compounds demonstrated that the binding of [C-11]PEO is saturable and selective to the mu-OR in rat brain.