Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10592095 | Bioorganic & Medicinal Chemistry Letters | 2014 | 4 Pages |
Abstract
Vortioxetine is a new multi-modal drug against major depressive disorder with high affinity for a range of different serotonergic targets in the CNS. We report the 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [11C]vortioxetine in a Danish Landrace pig showed rapid brain uptake and brain distribution in accordance with the pharmacological profile, all though an unexpected high binding in cerebellum was also observed. [11C]vortioxetine displayed slow tracer kinetics with peak uptake after 60Â min and with limited wash-out from the brain. Further studies are needed but this radioligand may prove to be a valuable tool in unraveling the clinical effects of vortioxetine.
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Authors
Valdemar L. Andersen, Hanne D. Hansen, Matthias M. Herth, Gitte M. Knudsen, Jesper L. Kristensen,