Marton János, Schoultz Bent W, Hjørnevik Trine, Drzezga Alexander, Yousefi Behrooz H, Wester Hans-Jürgen, Willoch Frode, Henriksen Gjermund
ABX Advanced Biochemical Compounds, Biomedizinische Forschungsreagenzien GmbH, Radeberg, Germany.
J Med Chem. 2009 Sep 24;52(18):5586-9. doi: 10.1021/jm900892x.
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.
拮抗剂放射性示踪剂在体内检测阿片受体（ORs）上高效激动剂的竞争时仅表现出低灵敏度。我们报告[(11)C]PEO与μ和κ阿片受体具有高亲和力，是一种完全激动剂，静脉注射后在μ-OR高密度的大鼠脑区中聚集。用μ和κ-OR选择性化合物进行的阻断研究表明，[(11)C]PEO在大鼠脑中的结合对μ-OR是可饱和且选择性的。
