Marjorie R Levinstein1, Emilya N Ventriglia1, Juan L Gomez1, Reece C Budinich1, János Marton2, Gjermund Henriksen3,4,5, Daniel P Holt6, Robert F Dannals6, Martin G Pomper6, Carlos A Zarate7, Jordi Bonaventura8,9, Michael Michaelides10,11. 1. Biobehavioral Imaging and Molecular Neuropsychopharmacology Unit, National Institute On Drug Abuse Intramural Research Program, Baltimore, MD, 21224, USA. 2. ABX Advanced Biochemical Compounds Biomedizinische Forschungsreagenzien GmbH, Heinrich-Glaeser-Strasse 10-14, 01454, Radeberg, Germany. 3. Institute of Basic Medical Sciences, University of Oslo, Blindern, P. O. Box 1105, N-0317, Oslo, Norway. 4. Norwegian Medical Cyclotron Centre Ltd, Sognsvannsveien 20, N-0372, Oslo, Norway. 5. Institute of Physics, University of Oslo, Sem Sælands vei 24, N-0371, Oslo, Norway. 6. Department of Radiology, Johns Hopkins School of Medicine, Baltimore, MD, 21205, USA. 7. Experimental Therapeutics and Pathophysiology Branch, National Institute of Mental Health, Bethesda, MD, 20892, USA. 8. Departament de Patologia I Terapèutica Experimental, Institut de Neurociències, Universitat de Barcelona, L'Hospitalet de Llobregat, Catalonia, Spain. 9. Neuropharmacology and Pain Group, Neuroscience Program, Institut d'Investigació Biomèdica de Bellvitge, IDIBELL, 08907, L'Hospitalet de Llobregat, Catalonia, Spain. 10. Biobehavioral Imaging and Molecular Neuropsychopharmacology Unit, National Institute On Drug Abuse Intramural Research Program, Baltimore, MD, 21224, USA. mike.michaelides@nih.gov. 11. Department of Psychiatry and Behavioral Sciences, Johns Hopkins University School of Medicine, Baltimore, MD, 21205, USA. mike.michaelides@nih.gov.
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.
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.
Authors: H J Wester; F Willoch; T R Tölle; F Munz; M Herz; I Oye; J Schadrack; M Schwaiger; P Bartenstein Journal: J Nucl Med Date: 2000-07 Impact factor: 10.057