Employees – University of Copenhagen

Evaluation of 3-Ethyl-3-(phenylpiperazinylbutyl)oxindoles as PET Ligands for the Serotonin 5-HT7 Receptor: Synthesis, Pharmacology, Radiolabeling, and in Vivo Brain Imaging in Pigs

Research output: Contribution to journalJournal articleResearchpeer-review

Standard

Evaluation of 3-Ethyl-3-(phenylpiperazinylbutyl)oxindoles as PET Ligands for the Serotonin 5-HT7 Receptor : Synthesis, Pharmacology, Radiolabeling, and in Vivo Brain Imaging in Pigs. / Herth, Matthias M; Andersen, Valdemar L; Hansen, Hanne D; Stroth, Nikolas; Volk, Balázs; Lehel, Szabolcs; Dyssegaard, Agnete; Ettrup, Anders; Svenningsson, Per; Knudsen, Gitte M; Kristensen, Jesper Langgaard.

In: Journal of Medicinal Chemistry, Vol. 58, No. 8, 13.04.2015, p. 3631–3636.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Herth, MM, Andersen, VL, Hansen, HD, Stroth, N, Volk, B, Lehel, S, Dyssegaard, A, Ettrup, A, Svenningsson, P, Knudsen, GM & Kristensen, JL 2015, 'Evaluation of 3-Ethyl-3-(phenylpiperazinylbutyl)oxindoles as PET Ligands for the Serotonin 5-HT7 Receptor: Synthesis, Pharmacology, Radiolabeling, and in Vivo Brain Imaging in Pigs' Journal of Medicinal Chemistry, vol. 58, no. 8, pp. 3631–3636. https://doi.org/10.1021/acs.jmedchem.5b00095

APA

Herth, M. M., Andersen, V. L., Hansen, H. D., Stroth, N., Volk, B., Lehel, S., ... Kristensen, J. L. (2015). Evaluation of 3-Ethyl-3-(phenylpiperazinylbutyl)oxindoles as PET Ligands for the Serotonin 5-HT7 Receptor: Synthesis, Pharmacology, Radiolabeling, and in Vivo Brain Imaging in Pigs. Journal of Medicinal Chemistry, 58(8), 3631–3636. https://doi.org/10.1021/acs.jmedchem.5b00095

Vancouver

Herth MM, Andersen VL, Hansen HD, Stroth N, Volk B, Lehel S et al. Evaluation of 3-Ethyl-3-(phenylpiperazinylbutyl)oxindoles as PET Ligands for the Serotonin 5-HT7 Receptor: Synthesis, Pharmacology, Radiolabeling, and in Vivo Brain Imaging in Pigs. Journal of Medicinal Chemistry. 2015 Apr 13;58(8):3631–3636. https://doi.org/10.1021/acs.jmedchem.5b00095

Author

Herth, Matthias M ; Andersen, Valdemar L ; Hansen, Hanne D ; Stroth, Nikolas ; Volk, Balázs ; Lehel, Szabolcs ; Dyssegaard, Agnete ; Ettrup, Anders ; Svenningsson, Per ; Knudsen, Gitte M ; Kristensen, Jesper Langgaard. / Evaluation of 3-Ethyl-3-(phenylpiperazinylbutyl)oxindoles as PET Ligands for the Serotonin 5-HT7 Receptor : Synthesis, Pharmacology, Radiolabeling, and in Vivo Brain Imaging in Pigs. In: Journal of Medicinal Chemistry. 2015 ; Vol. 58, No. 8. pp. 3631–3636.

Bibtex

@article{8cfa51bd938f494788a1f8214aa97df3,
title = "Evaluation of 3-Ethyl-3-(phenylpiperazinylbutyl)oxindoles as PET Ligands for the Serotonin 5-HT7 Receptor: Synthesis, Pharmacology, Radiolabeling, and in Vivo Brain Imaging in Pigs",
abstract = "We have investigated several oxindole derivatives in the pursuit of a 5-HT7 receptor PET ligand. Herein the synthesis, chiral separation, and pharmacological profiling of two possible PET candidates toward a wide selection of CNS-targets are detailed. Subsequent (11)C-labeling and in vivo evaluation in Danish landrace pigs showed that both ligands displayed high brain uptake. However, neither of the radioligands could be displaced by the 5-HT7 receptor selective inverse agonist SB-269970.",
author = "Herth, {Matthias M} and Andersen, {Valdemar L} and Hansen, {Hanne D} and Nikolas Stroth and Bal{\'a}zs Volk and Szabolcs Lehel and Agnete Dyssegaard and Anders Ettrup and Per Svenningsson and Knudsen, {Gitte M} and Kristensen, {Jesper Langgaard}",
year = "2015",
month = "4",
day = "13",
doi = "10.1021/acs.jmedchem.5b00095",
language = "English",
volume = "58",
pages = "3631–3636",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "8",

}

RIS

TY - JOUR

T1 - Evaluation of 3-Ethyl-3-(phenylpiperazinylbutyl)oxindoles as PET Ligands for the Serotonin 5-HT7 Receptor

T2 - Synthesis, Pharmacology, Radiolabeling, and in Vivo Brain Imaging in Pigs

AU - Herth, Matthias M

AU - Andersen, Valdemar L

AU - Hansen, Hanne D

AU - Stroth, Nikolas

AU - Volk, Balázs

AU - Lehel, Szabolcs

AU - Dyssegaard, Agnete

AU - Ettrup, Anders

AU - Svenningsson, Per

AU - Knudsen, Gitte M

AU - Kristensen, Jesper Langgaard

PY - 2015/4/13

Y1 - 2015/4/13

N2 - We have investigated several oxindole derivatives in the pursuit of a 5-HT7 receptor PET ligand. Herein the synthesis, chiral separation, and pharmacological profiling of two possible PET candidates toward a wide selection of CNS-targets are detailed. Subsequent (11)C-labeling and in vivo evaluation in Danish landrace pigs showed that both ligands displayed high brain uptake. However, neither of the radioligands could be displaced by the 5-HT7 receptor selective inverse agonist SB-269970.

AB - We have investigated several oxindole derivatives in the pursuit of a 5-HT7 receptor PET ligand. Herein the synthesis, chiral separation, and pharmacological profiling of two possible PET candidates toward a wide selection of CNS-targets are detailed. Subsequent (11)C-labeling and in vivo evaluation in Danish landrace pigs showed that both ligands displayed high brain uptake. However, neither of the radioligands could be displaced by the 5-HT7 receptor selective inverse agonist SB-269970.

U2 - 10.1021/acs.jmedchem.5b00095

DO - 10.1021/acs.jmedchem.5b00095

M3 - Journal article

VL - 58

SP - 3631

EP - 3636

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 8

ER -

ID: 135400850