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(11)C-labeling and preliminary evaluation of vortioxetine as a PET radioligand

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  1. Improved radiosynthesis and preliminary in vivo evaluation of the 11C-labeled tetrazine [11C]AE-1 for pretargeted PET imaging

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  2. Labeling and preliminary in vivo evaluation of the 5-HT(7) receptor selective agonist [(11)C]E-55888

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  3. (11)C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand

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  4. Synthesis, in vitro and in vivo evaluation of [11C]MMTP: a potential PET ligand for mGluR1 receptors

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  1. The Modulatory Role of Serotonin on Human Impulsive Aggression

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  2. Hot and cold cognitive disturbances in antidepressant-free patients with major depressive disorder: a NeuroPharm study

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  3. Structural brain abnormalities associated with cognitive impairments in bipolar disorder

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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 (11)C-labeling of vortioxetine with [(11)C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [(11)C]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. [(11)C]vortioxetine displayed slow tracer kinetics with peak uptake after 60 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.

Original languageEnglish
JournalBioorganic & Medicinal Chemistry Letters
Volume24
Issue number11
Pages (from-to)2408-11
Number of pages4
ISSN0960-894X
DOIs
Publication statusPublished - 1 Jun 2014

ID: 44558373