18F-labeled sufentanil for PET-imaging of mu-opioid receptors.
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.
Henriksen
Gjermund
G
Department of Nuclear Medicine, Klinikum rechts der Isar, Technische Universität München, Ismaningerstrasse 22, 81675 München, Germany.
Platzer
Stefan
S
Hauser
Andrea
A
Willoch
Frode
F
Berthele
Achim
A
Schwaiger
Markus
M
Wester
Hans-Jürgen
HJ
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*
D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D017450:Receptors, Opioid, mu; D017409:Sufentanil