(11)C-labeling and preliminary evaluation of vortioxetine as a PET radioligand
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(11)C-labeling and preliminary evaluation of vortioxetine as a PET radioligand. / Andersen, Valdemar L; Hansen, Hanne D; Herth, Matthias M; Knudsen, Gitte M; Kristensen, Jesper Langgaard.
In: Bioorganic & Medicinal Chemistry Letters, Vol. 24, No. 11, 19.04.2014, p. 2408-2411.Research output: Contribution to journal › Journal article › Research › peer-review
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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 - 2014/4/19
Y1 - 2014/4/19
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
VL - 24
SP - 2408
EP - 2411
JO - Bioorganic & Medicinal Chemistry Letters
JF - Bioorganic & Medicinal Chemistry Letters
SN - 0960-894X
IS - 11
ER -
ID: 109521780