title: 18F-labeled sufentanil for PET-imaging of mu-opioid receptors.
abstract: The synthesis of an (18)F-labeled sufentanil analogue with apparent high mu-opioid receptor selectivity is reported. Intravenous injection of N-[4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl]-N-phenyl-2-(+/-)-[(18)F]fluoropropan-amide in mice resulted in high brain uptake and a regional brain activity distribution corresponding to the mu-opioid receptor expression pattern. The developed ligand is a promising tracer for extended protocols in mu-opioid receptor mapping and quantitation with positron emission tomography.
authors.affiliation: Department of Nuclear Medicine, Klinikum rechts der Isar, Technische Universität München, Ismaningerstrasse 22, 81675 München, Germany.
authors.forename: Gjermund
authors.initials: G
authors.lastname: Henriksen
authors.forename: Stefan
authors.initials: S
authors.lastname: Platzer
authors.forename: Andrea
authors.initials: A
authors.lastname: Hauser
authors.forename: Frode
authors.initials: F
authors.lastname: Willoch
authors.forename: Achim
authors.initials: A
authors.lastname: Berthele
authors.forename: Markus
authors.initials: M
authors.lastname: Schwaiger
authors.forename: Hans-Jürgen
authors.initials: HJ
authors.lastname: Wester
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism; D005462:Fluorine Radioisotopes; D051379:Mice; D049268:Positron-Emission Tomography / Q000379:methods; D019275:Radiopharmaceuticals / Q000378:metabolism*; D017450:Receptors, Opioid, mu / Q000378:metabolism*; D017409:Sufentanil / Q000031:analogs & derivatives / Q000378:metabolism*
chemical_list: D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D017450:Receptors, Opioid, mu; D017409:Sufentanil