Document Report Card

ID: ALA1155180

Journal: J Med Chem

Title: Synthesis and evaluation of a full-agonist orvinol for PET-imaging of opioid receptors: [11C]PEO.

Authors: Marton J, Schoultz BW, Hjørnevik T, Drzezga A, Yousefi BH, Wester HJ, Willoch F, Henriksen G.

Abstract: Antagonist radiotracers have shown only a low sensitivity for detecting competition from high-efficacy agonists at opioid receptors (ORs) in vivo. We report that [(11)C]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 [(11)C]PEO is saturable and selective to the mu-OR in rat brain.

CiteXplore: 19694469

DOI: 10.1021/jm900892x