Synthesis and evaluation of a full-agonist orvinol for PET-imaging of opioid receptors: [11C]PEO.
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.
Marton
János
J
ABX Advanced Biochemical Compounds, Biomedizinische Forschungsreagenzien GmbH, Radeberg, Germany.
Schoultz
Bent W
BW
Hjørnevik
Trine
T
Drzezga
Alexander
A
Yousefi
Behrooz H
BH
Wester
Hans-Jürgen
HJ
Willoch
Frode
F
Henriksen
Gjermund
G
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism; D016466:CHO Cells; D002250:Carbon Radioisotopes / Q000737:chemistry; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D007700:Kinetics; D008297:Male; D009019:Morphinans / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D049268:Positron-Emission Tomography; D051381:Rats; D017208:Rats, Wistar; D011957:Receptors, Opioid / Q000819:agonists* / Q000378:metabolism; D013379:Substrate Specificity
D002250:Carbon Radioisotopes; D009019:Morphinans; D011957:Receptors, Opioid; C544195:phenylethyl orvinol