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

TY - JOUR

T1 - (11)C-labeling and preliminary evaluation of vortioxetine as a PET radioligand

AU - Andersen, Valdemar L

AU - Hansen, Hanne D

AU - Herth, Matthias M

AU - Knudsen, Gitte M

AU - Kristensen, Jesper Langgaard

N1 - Copyright © 2014 Elsevier Ltd. All rights reserved.

PY - 2014/6/1

Y1 - 2014/6/1

N2 - 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 60min 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.

AB - 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 60min 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.

U2 - 10.1016/j.bmcl.2014.04.044

DO - 10.1016/j.bmcl.2014.04.044

M3 - Journal article

C2 - 24786133

SN - 0960-894X

VL - 24

SP - 2408

EP - 2411

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 11

ER -