| Literature DB >> 19694469 |
János Marton1, Bent W Schoultz, Trine Hjørnevik, Alexander Drzezga, Behrooz H Yousefi, Hans-Jürgen Wester, Frode Willoch, Gjermund Henriksen.
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.Entities:
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Year: 2009 PMID： 19694469 DOI： 10.1021/jm900892x
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446