@article{b5c559538d9c4c87b1846852b4c2dc0f,
title = "6-O-(2-[18F]Fluoroethyl)-6-O-Desmethyl-Diprenorphine ([18F]FE-DPN) Preferentially Binds to Mu Opioid Receptors In Vivo",
abstract = "Purpose: 6-O-(2-[18F]Fluoroethyl)-6-O-desmethyl-diprenorphine ([18F]FE-DPN) is regarded as a non-selective opioid receptor radiotracer. Procedure: Here, we report the first characterization of [18F]FE-DPN synthesized from the novel precursor, 6-O-(2-tosyloxyethoxy)-6-O-desmethyl-3-O-trityl-diprenorphine (TE-TDDPN), using a one-pot, two-step nucleophilic radiosynthesis to image opioid receptors in rats and mice using positron emission tomography. Results: We also show that [18F]FE-DPN and [3H]DPN exhibit negligible brain uptake in mu opioid receptor (MOR) knockout mice. Conclusions: Taken together with prior findings, our results suggest that [18F]FE-DPN and [3H]DPN preferentially bind to MOR in rodents in vivo.",
keywords = "Diprenorphine, In vivo, Opioid, PET",
author = "Levinstein, {Marjorie R.} and Ventriglia, {Emilya N.} and Gomez, {Juan L.} and Budinich, {Reece C.} and J{\'a}nos Marton and Gjermund Henriksen and Holt, {Daniel P.} and Dannals, {Robert F.} and Pomper, {Martin G.} and Zarate, {Carlos A.} and Jordi Bonaventura and Michael Michaelides",
note = "Funding Information: This work was supported by the NIDA Intramural Research Program (ZIA000069, MM) and by Grants RYC-2019-027371-I (JB) funded by MCIN/AEI/1013039/501100011033 and by “ESF Investing in your future,” Plan Nacional Sobre Drogas 2021I070 (JB) funded by the Spanish Ministerio de Sanidad, and (EB024495, MGP) funded by NIBIB. Funding Information: MM has received research funding from AstraZeneca, Redpin Therapeutics, and Attune Neurosciences. CAZ is listed as a coinventor on a patent for the use of ketamine in major depression and suicidal ideation. CAZ is listed as a coinventor on a patent for the use of (2R,6R)-hydroxynorketamine, (S)-dehydronorketamine, and other stereoisomeric dehydro and hydroxylated metabolites of (R,S)-ketamine metabolites in the treatment of depression and neuropathic pain. CAZ is listed as coinventor on a patent application for the use of (2R,6R)-hydroxynorketamine and (2S,6S)-hydroxynorketamine in the treatment of depression, anxiety, anhedonia, suicidal ideation, and post-traumatic stress disorders. CAZ has assigned his patent rights to the US government but will share a percentage of any royalties that may be received by the government. All other authors declare no conflicts of interest. Publisher Copyright: {\textcopyright} 2022, This is a U.S. Government work and not under copyright protection in the US; foreign copyright protection may apply.",
year = "2023",
month = apr,
doi = "10.1007/s11307-022-01767-5",
language = "English (US)",
volume = "25",
pages = "384--390",
journal = "Molecular Imaging and Biology",
issn = "1536-1632",
publisher = "Springer Science and Business Media Deutschland GmbH",
number = "2",
}