Labeling and preliminary in vivo evaluation of the 5-HT7 receptor selective agonist [(11)C]E-55888

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Labeling and preliminary in vivo evaluation of the 5-HT7 receptor selective agonist [(11)C]E-55888. / Hansen, Hanne D; Andersen, Valdemar L; Lehel, Szabolcs; Magnussen, Janus H; Dyssegaard, Agnete; Stroth, Nikolas; Kristensen, Jesper Langgaard; Knudsen, Gitte M; Herth, Matthias M.

In: Bioorganic & Medicinal Chemistry Letters, Vol. 25, No. 9, 01.05.2015, p. 1901-4.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Hansen, HD, Andersen, VL, Lehel, S, Magnussen, JH, Dyssegaard, A, Stroth, N, Kristensen, JL, Knudsen, GM & Herth, MM 2015, 'Labeling and preliminary in vivo evaluation of the 5-HT7 receptor selective agonist [(11)C]E-55888', Bioorganic & Medicinal Chemistry Letters, vol. 25, no. 9, pp. 1901-4. https://doi.org/10.1016/j.bmcl.2015.03.039

APA

Hansen, H. D., Andersen, V. L., Lehel, S., Magnussen, J. H., Dyssegaard, A., Stroth, N., ... Herth, M. M. (2015). Labeling and preliminary in vivo evaluation of the 5-HT7 receptor selective agonist [(11)C]E-55888. Bioorganic & Medicinal Chemistry Letters, 25(9), 1901-4. https://doi.org/10.1016/j.bmcl.2015.03.039

Vancouver

Hansen HD, Andersen VL, Lehel S, Magnussen JH, Dyssegaard A, Stroth N et al. Labeling and preliminary in vivo evaluation of the 5-HT7 receptor selective agonist [(11)C]E-55888. Bioorganic & Medicinal Chemistry Letters. 2015 May 1;25(9):1901-4. https://doi.org/10.1016/j.bmcl.2015.03.039

Author

Hansen, Hanne D ; Andersen, Valdemar L ; Lehel, Szabolcs ; Magnussen, Janus H ; Dyssegaard, Agnete ; Stroth, Nikolas ; Kristensen, Jesper Langgaard ; Knudsen, Gitte M ; Herth, Matthias M. / Labeling and preliminary in vivo evaluation of the 5-HT7 receptor selective agonist [(11)C]E-55888. In: Bioorganic & Medicinal Chemistry Letters. 2015 ; Vol. 25, No. 9. pp. 1901-4.

Bibtex

@article{55a9283309624acf8e55481785669231,
title = "Labeling and preliminary in vivo evaluation of the 5-HT7 receptor selective agonist [(11)C]E-55888",
abstract = "E-55888 has been identified as a selective serotonin 7 (5-HT7) receptor agonist. In this study, we describe the synthesis, radiolabeling and in vivo evaluation of [(11)C]E-55888 as a radioligand for positron emission tomography (PET) imaging. [(11)C]E-55888 was obtained by N-methylation of an appropriate precursor using [(11)C]MeOTf in acetone at 60°C giving isolated quantities in the range of 1.7-2.4GBq. Studies in Danish Landrace pigs demonstrated that [(11)C]E-55888 has good brain uptake, however, the distribution in the brain tissue was dominated by non-specific binding, as binding could neither be displaced by the structurally different 5-HT7 receptor ligand SB-269970 nor by self-block with unlabeled E-55888. Based on these data, [(11)C]E-55888 does not show promise as a PET radioligand for imaging the 5-HT7 receptor in vivo.",
author = "Hansen, {Hanne D} and Andersen, {Valdemar L} and Szabolcs Lehel and Magnussen, {Janus H} and Agnete Dyssegaard and Nikolas Stroth and Kristensen, {Jesper Langgaard} and Knudsen, {Gitte M} and Herth, {Matthias M}",
note = "Copyright {\circledC} 2015 Elsevier Ltd. All rights reserved.",
year = "2015",
month = "5",
day = "1",
doi = "10.1016/j.bmcl.2015.03.039",
language = "English",
volume = "25",
pages = "1901--4",
journal = "Bioorganic & Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Pergamon Press",
number = "9",

}

RIS

TY - JOUR

T1 - Labeling and preliminary in vivo evaluation of the 5-HT7 receptor selective agonist [(11)C]E-55888

AU - Hansen, Hanne D

AU - Andersen, Valdemar L

AU - Lehel, Szabolcs

AU - Magnussen, Janus H

AU - Dyssegaard, Agnete

AU - Stroth, Nikolas

AU - Kristensen, Jesper Langgaard

AU - Knudsen, Gitte M

AU - Herth, Matthias M

N1 - Copyright © 2015 Elsevier Ltd. All rights reserved.

PY - 2015/5/1

Y1 - 2015/5/1

N2 - E-55888 has been identified as a selective serotonin 7 (5-HT7) receptor agonist. In this study, we describe the synthesis, radiolabeling and in vivo evaluation of [(11)C]E-55888 as a radioligand for positron emission tomography (PET) imaging. [(11)C]E-55888 was obtained by N-methylation of an appropriate precursor using [(11)C]MeOTf in acetone at 60°C giving isolated quantities in the range of 1.7-2.4GBq. Studies in Danish Landrace pigs demonstrated that [(11)C]E-55888 has good brain uptake, however, the distribution in the brain tissue was dominated by non-specific binding, as binding could neither be displaced by the structurally different 5-HT7 receptor ligand SB-269970 nor by self-block with unlabeled E-55888. Based on these data, [(11)C]E-55888 does not show promise as a PET radioligand for imaging the 5-HT7 receptor in vivo.

AB - E-55888 has been identified as a selective serotonin 7 (5-HT7) receptor agonist. In this study, we describe the synthesis, radiolabeling and in vivo evaluation of [(11)C]E-55888 as a radioligand for positron emission tomography (PET) imaging. [(11)C]E-55888 was obtained by N-methylation of an appropriate precursor using [(11)C]MeOTf in acetone at 60°C giving isolated quantities in the range of 1.7-2.4GBq. Studies in Danish Landrace pigs demonstrated that [(11)C]E-55888 has good brain uptake, however, the distribution in the brain tissue was dominated by non-specific binding, as binding could neither be displaced by the structurally different 5-HT7 receptor ligand SB-269970 nor by self-block with unlabeled E-55888. Based on these data, [(11)C]E-55888 does not show promise as a PET radioligand for imaging the 5-HT7 receptor in vivo.

U2 - 10.1016/j.bmcl.2015.03.039

DO - 10.1016/j.bmcl.2015.03.039

M3 - Journal article

C2 - 25857944

VL - 25

SP - 1901

EP - 1904

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

SN - 0960-894X

IS - 9

ER -

ID: 136803379