Synthesis and Evaluation of
Three Structurally Related 18F‑Labeled Orvinols
of Different Intrinsic Activities:
6‑O‑[18F]Fluoroethyl-diprenorphine
([18F]FDPN), 6‑O‑[18F]Fluoroethyl-buprenorphine ([18F]FBPN), and 6‑O‑[18F]Fluoroethyl-phenethyl-orvinol ([18F]FPEO)
Posted on 2014-06-26 - 00:00
We report the synthesis and biological
evaluation of a triplet
of 6-O-18F-fluoroethylated derivatives
of structurally related orvinols that span across the full range of
intrinsic activities, the antagonist diprenorphine, the partial agonist
buprenorphine, and the full agonist phenethyl-orvinol. [18F]fluoroethyl-diprenorphine, [18F]fluoroethyl-buprenorphine,
and [18F]fluoroethyl-phenethyl-orvinol were prepared in
high yields and quality from their 6-O-desmethyl-precursors.
The results indicate suitable properties of the three 6-O-18F-fluoroethylated derivatives as functional analogues
to the native carbon-11 labeled versions with similar pharmacological
properties.
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Schoultz, Bent W.; Hjørnevik, Trine; Reed, Brian
J.; Marton, János; Coello, Christopher
S.; Willoch, Frode; et al. (2016). Synthesis and Evaluation of
Three Structurally Related 18F‑Labeled Orvinols
of Different Intrinsic Activities:
6‑O‑[18F]Fluoroethyl-diprenorphine
([18F]FDPN), 6‑O‑[18F]Fluoroethyl-buprenorphine ([18F]FBPN), and 6‑O‑[18F]Fluoroethyl-phenethyl-orvinol ([18F]FPEO). ACS Publications. Collection. https://doi.org/10.1021/jm500503k
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AUTHORS (7)
- BSBent W. SchoultzTHTrine HjørnevikBRBrian J. ReedJMJános MartonCCChristopher S. CoelloFWFrode WillochGHGjermund Henriksen
