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J Med Chem. 2009 Sep 24;52(18):5586-9. doi: 10.1021/jm900892x.

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

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  • 1ABX Advanced Biochemical Compounds, Biomedizinische Forschungsreagenzien GmbH, Radeberg, Germany.

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.

PMID:
19694469
[PubMed - indexed for MEDLINE]
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