(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 journalJournal articleResearchpeer-review

Harvard

Andersen, VL, Hansen, HD, Herth, MM, Knudsen, GM & Kristensen, JL 2014, '(11)C-labeling and preliminary evaluation of vortioxetine as a PET radioligand', Bioorganic & Medicinal Chemistry Letters, vol. 24, no. 11, pp. 2408-2411. https://doi.org/10.1016/j.bmcl.2014.04.044

APA

Andersen, V. L., Hansen, H. D., Herth, M. M., Knudsen, G. M., & Kristensen, J. L. (2014). (11)C-labeling and preliminary evaluation of vortioxetine as a PET radioligand. Bioorganic & Medicinal Chemistry Letters, 24(11), 2408-2411. https://doi.org/10.1016/j.bmcl.2014.04.044

Vancouver

Andersen VL, Hansen HD, Herth MM, Knudsen GM, Kristensen JL. (11)C-labeling and preliminary evaluation of vortioxetine as a PET radioligand. Bioorganic & Medicinal Chemistry Letters. 2014 Apr 19;24(11):2408-2411. https://doi.org/10.1016/j.bmcl.2014.04.044

Author

Andersen, Valdemar L ; Hansen, Hanne D ; Herth, Matthias M ; Knudsen, Gitte M ; Kristensen, Jesper Langgaard. / (11)C-labeling and preliminary evaluation of vortioxetine as a PET radioligand. In: Bioorganic & Medicinal Chemistry Letters. 2014 ; Vol. 24, No. 11. pp. 2408-2411.

Bibtex

@article{960e129a197b4acc963152a5c8fac482,
title = "(11)C-labeling and preliminary evaluation of vortioxetine as a PET radioligand",
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}",
note = "Copyright {\circledC} 2014 Elsevier Ltd. All rights reserved.",
year = "2014",
month = "4",
day = "19",
doi = "10.1016/j.bmcl.2014.04.044",
language = "English",
volume = "24",
pages = "2408--2411",
journal = "Bioorganic & Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Pergamon Press",
number = "11",

}

RIS

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

VL - 24

SP - 2408

EP - 2411

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

SN - 0960-894X

IS - 11

ER -

ID: 109521780