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6-O-(2-[18F]Fluoroethyl)-6-O-Desmethyl-Diprenorphine ([18F]FE-DPN) Preferentially Binds to Mu Opioid Receptors In Vivo.
Levinstein, Marjorie R; Ventriglia, Emilya N; Gomez, Juan L; Budinich, Reece C; Marton, János; Henriksen, Gjermund; Holt, Daniel P; Dannals, Robert F; Pomper, Martin G; Zarate, Carlos A; Bonaventura, Jordi; Michaelides, Michael.
Affiliation
  • Levinstein MR; Biobehavioral Imaging and Molecular Neuropsychopharmacology Unit, National Institute On Drug Abuse Intramural Research Program, Baltimore, MD, 21224, USA.
  • Ventriglia EN; Biobehavioral Imaging and Molecular Neuropsychopharmacology Unit, National Institute On Drug Abuse Intramural Research Program, Baltimore, MD, 21224, USA.
  • Gomez JL; Biobehavioral Imaging and Molecular Neuropsychopharmacology Unit, National Institute On Drug Abuse Intramural Research Program, Baltimore, MD, 21224, USA.
  • Budinich RC; Biobehavioral Imaging and Molecular Neuropsychopharmacology Unit, National Institute On Drug Abuse Intramural Research Program, Baltimore, MD, 21224, USA.
  • Marton J; ABX Advanced Biochemical Compounds Biomedizinische Forschungsreagenzien GmbH, Heinrich-Glaeser-Strasse 10-14, 01454, Radeberg, Germany.
  • Henriksen G; Institute of Basic Medical Sciences, University of Oslo, Blindern, P. O. Box 1105, N-0317, Oslo, Norway.
  • Holt DP; Norwegian Medical Cyclotron Centre Ltd, Sognsvannsveien 20, N-0372, Oslo, Norway.
  • Dannals RF; Institute of Physics, University of Oslo, Sem Sælands vei 24, N-0371, Oslo, Norway.
  • Pomper MG; Department of Radiology, Johns Hopkins School of Medicine, Baltimore, MD, 21205, USA.
  • Zarate CA; Department of Radiology, Johns Hopkins School of Medicine, Baltimore, MD, 21205, USA.
  • Bonaventura J; Department of Radiology, Johns Hopkins School of Medicine, Baltimore, MD, 21205, USA.
  • Michaelides M; Experimental Therapeutics and Pathophysiology Branch, National Institute of Mental Health, Bethesda, MD, 20892, USA.
Mol Imaging Biol ; 25(2): 384-390, 2023 04.
Article in En | MEDLINE | ID: mdl-35999424
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.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Receptors, Opioid, mu / Positron-Emission Tomography Limits: Animals Language: En Journal: Mol Imaging Biol Journal subject: BIOLOGIA MOLECULAR / DIAGNOSTICO POR IMAGEM Year: 2023 Document type: Article Affiliation country: United States
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Receptors, Opioid, mu / Positron-Emission Tomography Limits: Animals Language: En Journal: Mol Imaging Biol Journal subject: BIOLOGIA MOLECULAR / DIAGNOSTICO POR IMAGEM Year: 2023 Document type: Article Affiliation country: United States