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

Valdemar L Andersen; Hanne D Hansen; Matthias M Herth; Gitte M Knudsen; Jesper Langgaard Kristensen

doi:10.1016/j.bmcl.2014.04.044

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

Valdemar L Andersen, Hanne D Hansen, Matthias M Herth, Gitte M Knudsen, Jesper Langgaard Kristensen

Institut for Klinisk Medicin

12 Citationer (Scopus)

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 (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.

Originalsprog	Engelsk
Tidsskrift	Bioorganic & Medicinal Chemistry Letters
Vol/bind	24
Udgave nummer	11
Sider (fra-til)	2408-2411
Antal sider	4
ISSN	0960-894X
DOI	https://doi.org/10.1016/j.bmcl.2014.04.044
Status	Udgivet - 1 jun. 2014

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10.1016/j.bmcl.2014.04.044

Citationsformater

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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 (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.",

author = "Andersen, {Valdemar L} and Hansen, {Hanne D} and Herth, {Matthias M} and Knudsen, {Gitte M} and Kristensen, {Jesper Langgaard}",

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AU - Andersen, Valdemar L

AU - Hansen, Hanne D

AU - Herth, Matthias M

AU - Knudsen, Gitte M

AU - Kristensen, Jesper Langgaard

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

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SN - 0960-894X

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SP - 2408

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JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

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ER -

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

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