11C-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 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Prelim...
Ausführliche Beschreibung
Gespeichert in:
| Autor*in: |
Andersen, Valdemar L. [verfasserIn] |
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| Format: |
E-Artikel |
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| Sprache: |
Englisch |
| Erschienen: |
2014transfer abstract |
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| Umfang: |
4 |
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| Übergeordnetes Werk: |
Enthalten in: Feeding European sea bass ( - Torrecillas, S. ELSEVIER, 2018, a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines, Amsterdam [u.a.] |
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| Übergeordnetes Werk: |
volume:24 ; year:2014 ; number:11 ; day:1 ; month:06 ; pages:2408-2411 ; extent:4 |
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| DOI / URN: |
10.1016/j.bmcl.2014.04.044 |
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| 520 | |a 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 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [11C]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. [11C]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. | ||
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10.1016/j.bmcl.2014.04.044 doi GBVA2014016000002.pica (DE-627)ELV012501581 (ELSEVIER)S0960-894X(14)00392-8 DE-627 ger DE-627 rakwb eng 540 610 540 DE-600 610 DE-600 630 VZ 22 ssgn 46.00 bkl Andersen, Valdemar L. verfasserin aut 11C-labeling and preliminary evaluation of vortioxetine as a PET radioligand 2014transfer abstract 4 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier 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 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [11C]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. [11C]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. 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 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [11C]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. [11C]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. Cross-coupling Elsevier Palladium Elsevier Carbon-11 Elsevier Vortioxetine Elsevier PET Elsevier Hansen, Hanne D. oth Herth, Matthias M. oth Knudsen, Gitte M. oth Kristensen, Jesper L. oth Enthalten in Elsevier Science Torrecillas, S. ELSEVIER Feeding European sea bass ( 2018 a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines Amsterdam [u.a.] (DE-627)ELV000272361 volume:24 year:2014 number:11 day:1 month:06 pages:2408-2411 extent:4 https://doi.org/10.1016/j.bmcl.2014.04.044 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 46.00 Tiermedizin: Allgemeines VZ AR 24 2014 11 1 0601 2408-2411 4 045F 540 |
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10.1016/j.bmcl.2014.04.044 doi GBVA2014016000002.pica (DE-627)ELV012501581 (ELSEVIER)S0960-894X(14)00392-8 DE-627 ger DE-627 rakwb eng 540 610 540 DE-600 610 DE-600 630 VZ 22 ssgn 46.00 bkl Andersen, Valdemar L. verfasserin aut 11C-labeling and preliminary evaluation of vortioxetine as a PET radioligand 2014transfer abstract 4 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier 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 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [11C]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. [11C]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. 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 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [11C]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. [11C]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. Cross-coupling Elsevier Palladium Elsevier Carbon-11 Elsevier Vortioxetine Elsevier PET Elsevier Hansen, Hanne D. oth Herth, Matthias M. oth Knudsen, Gitte M. oth Kristensen, Jesper L. oth Enthalten in Elsevier Science Torrecillas, S. ELSEVIER Feeding European sea bass ( 2018 a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines Amsterdam [u.a.] (DE-627)ELV000272361 volume:24 year:2014 number:11 day:1 month:06 pages:2408-2411 extent:4 https://doi.org/10.1016/j.bmcl.2014.04.044 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 46.00 Tiermedizin: Allgemeines VZ AR 24 2014 11 1 0601 2408-2411 4 045F 540 |
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10.1016/j.bmcl.2014.04.044 doi GBVA2014016000002.pica (DE-627)ELV012501581 (ELSEVIER)S0960-894X(14)00392-8 DE-627 ger DE-627 rakwb eng 540 610 540 DE-600 610 DE-600 630 VZ 22 ssgn 46.00 bkl Andersen, Valdemar L. verfasserin aut 11C-labeling and preliminary evaluation of vortioxetine as a PET radioligand 2014transfer abstract 4 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier 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 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [11C]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. [11C]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. 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 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [11C]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. [11C]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. Cross-coupling Elsevier Palladium Elsevier Carbon-11 Elsevier Vortioxetine Elsevier PET Elsevier Hansen, Hanne D. oth Herth, Matthias M. oth Knudsen, Gitte M. oth Kristensen, Jesper L. oth Enthalten in Elsevier Science Torrecillas, S. ELSEVIER Feeding European sea bass ( 2018 a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines Amsterdam [u.a.] (DE-627)ELV000272361 volume:24 year:2014 number:11 day:1 month:06 pages:2408-2411 extent:4 https://doi.org/10.1016/j.bmcl.2014.04.044 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 46.00 Tiermedizin: Allgemeines VZ AR 24 2014 11 1 0601 2408-2411 4 045F 540 |
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10.1016/j.bmcl.2014.04.044 doi GBVA2014016000002.pica (DE-627)ELV012501581 (ELSEVIER)S0960-894X(14)00392-8 DE-627 ger DE-627 rakwb eng 540 610 540 DE-600 610 DE-600 630 VZ 22 ssgn 46.00 bkl Andersen, Valdemar L. verfasserin aut 11C-labeling and preliminary evaluation of vortioxetine as a PET radioligand 2014transfer abstract 4 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier 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 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [11C]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. [11C]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. 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 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [11C]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. [11C]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. Cross-coupling Elsevier Palladium Elsevier Carbon-11 Elsevier Vortioxetine Elsevier PET Elsevier Hansen, Hanne D. oth Herth, Matthias M. oth Knudsen, Gitte M. oth Kristensen, Jesper L. oth Enthalten in Elsevier Science Torrecillas, S. ELSEVIER Feeding European sea bass ( 2018 a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines Amsterdam [u.a.] (DE-627)ELV000272361 volume:24 year:2014 number:11 day:1 month:06 pages:2408-2411 extent:4 https://doi.org/10.1016/j.bmcl.2014.04.044 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 46.00 Tiermedizin: Allgemeines VZ AR 24 2014 11 1 0601 2408-2411 4 045F 540 |
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10.1016/j.bmcl.2014.04.044 doi GBVA2014016000002.pica (DE-627)ELV012501581 (ELSEVIER)S0960-894X(14)00392-8 DE-627 ger DE-627 rakwb eng 540 610 540 DE-600 610 DE-600 630 VZ 22 ssgn 46.00 bkl Andersen, Valdemar L. verfasserin aut 11C-labeling and preliminary evaluation of vortioxetine as a PET radioligand 2014transfer abstract 4 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier 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 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [11C]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. [11C]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. 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 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [11C]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. [11C]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. Cross-coupling Elsevier Palladium Elsevier Carbon-11 Elsevier Vortioxetine Elsevier PET Elsevier Hansen, Hanne D. oth Herth, Matthias M. oth Knudsen, Gitte M. oth Kristensen, Jesper L. oth Enthalten in Elsevier Science Torrecillas, S. ELSEVIER Feeding European sea bass ( 2018 a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines Amsterdam [u.a.] (DE-627)ELV000272361 volume:24 year:2014 number:11 day:1 month:06 pages:2408-2411 extent:4 https://doi.org/10.1016/j.bmcl.2014.04.044 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 46.00 Tiermedizin: Allgemeines VZ AR 24 2014 11 1 0601 2408-2411 4 045F 540 |
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11C-labeling and preliminary evaluation of vortioxetine as a PET radioligand |
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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 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [11C]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. [11C]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. |
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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 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [11C]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. [11C]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. |
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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 11C-labeling of vortioxetine with [11C]MeI using a Suzuki-protocol that allows for the presence of an unprotected amine. Preliminary evaluation of [11C]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. [11C]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. |
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