Convergent [18]F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT2A receptor PET ligands

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Convergent [18]F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT2A receptor PET ligands. / Petersen, Ida Nymann; Villadsen, Jonas; Hansen, Hanne Demant; Jensen, Anders A; Lehel, Szabolcs; Gillings, Nic; Herth, Matthias M; Knudsen, Gitte M; Kristensen, Jesper L.

In: Bioorganic & Medicinal Chemistry, Vol. 24, 2016, p. 5353-5356.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Petersen, IN, Villadsen, J, Hansen, HD, Jensen, AA, Lehel, S, Gillings, N, Herth, MM, Knudsen, GM & Kristensen, JL 2016, 'Convergent [18]F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT2A receptor PET ligands' Bioorganic & Medicinal Chemistry, vol. 24, pp. 5353-5356. https://doi.org/10.1016/j.bmc.2016.08.056

APA

Petersen, I. N., Villadsen, J., Hansen, H. D., Jensen, A. A., Lehel, S., Gillings, N., ... Kristensen, J. L. (2016). Convergent [18]F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT2A receptor PET ligands. Bioorganic & Medicinal Chemistry, 24, 5353-5356. https://doi.org/10.1016/j.bmc.2016.08.056

Vancouver

Petersen IN, Villadsen J, Hansen HD, Jensen AA, Lehel S, Gillings N et al. Convergent [18]F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT2A receptor PET ligands. Bioorganic & Medicinal Chemistry. 2016;24:5353-5356. https://doi.org/10.1016/j.bmc.2016.08.056

Author

Petersen, Ida Nymann ; Villadsen, Jonas ; Hansen, Hanne Demant ; Jensen, Anders A ; Lehel, Szabolcs ; Gillings, Nic ; Herth, Matthias M ; Knudsen, Gitte M ; Kristensen, Jesper L. / Convergent [18]F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT2A receptor PET ligands. In: Bioorganic & Medicinal Chemistry. 2016 ; Vol. 24. pp. 5353-5356.

Bibtex

@article{d5c458e0d7d54781b5074980aa8637cc,
title = "Convergent [18]F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT2A receptor PET ligands",
abstract = "Positron emission tomography (PET) investigations of the 5-HT2A receptor (5-HT2AR) system can be used as a research tool in diseases such as depression, Alzheimer's disease and schizophrenia. We have previously developed a (11)C-labeled agonist PET ligand ([(11)C]Cimbi-36), and the aim of this study was to identify a (18)F-labeled analogue of this PET-ligand. Thus, we developed a convergent radiochemical approach giving easy access to 5 different (18)F-labeled ligands structurally related to Cimbi-36 from a common (18)F-labeled intermediate. After intravenous injection, all ligands entered the pig brain. However, since within-scan intervention with ketanserin, a known orthosteric 5-HT2A receptor antagonist, did not result in significant blocking, the radioligands seem unsuitable for neuroimaging of the 5-HT2AR in vivo.",
author = "Petersen, {Ida Nymann} and Jonas Villadsen and Hansen, {Hanne Demant} and Jensen, {Anders A} and Szabolcs Lehel and Nic Gillings and Herth, {Matthias M} and Knudsen, {Gitte M} and Kristensen, {Jesper L}",
note = "Copyright {\circledC} 2016 Elsevier Ltd. All rights reserved.",
year = "2016",
doi = "10.1016/j.bmc.2016.08.056",
language = "English",
volume = "24",
pages = "5353--5356",
journal = "Bioorganic & Medicinal Chemistry",
issn = "0968-0896",
publisher = "Pergamon Press",

}

RIS

TY - JOUR

T1 - Convergent [18]F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT2A receptor PET ligands

AU - Petersen, Ida Nymann

AU - Villadsen, Jonas

AU - Hansen, Hanne Demant

AU - Jensen, Anders A

AU - Lehel, Szabolcs

AU - Gillings, Nic

AU - Herth, Matthias M

AU - Knudsen, Gitte M

AU - Kristensen, Jesper L

N1 - Copyright © 2016 Elsevier Ltd. All rights reserved.

PY - 2016

Y1 - 2016

N2 - Positron emission tomography (PET) investigations of the 5-HT2A receptor (5-HT2AR) system can be used as a research tool in diseases such as depression, Alzheimer's disease and schizophrenia. We have previously developed a (11)C-labeled agonist PET ligand ([(11)C]Cimbi-36), and the aim of this study was to identify a (18)F-labeled analogue of this PET-ligand. Thus, we developed a convergent radiochemical approach giving easy access to 5 different (18)F-labeled ligands structurally related to Cimbi-36 from a common (18)F-labeled intermediate. After intravenous injection, all ligands entered the pig brain. However, since within-scan intervention with ketanserin, a known orthosteric 5-HT2A receptor antagonist, did not result in significant blocking, the radioligands seem unsuitable for neuroimaging of the 5-HT2AR in vivo.

AB - Positron emission tomography (PET) investigations of the 5-HT2A receptor (5-HT2AR) system can be used as a research tool in diseases such as depression, Alzheimer's disease and schizophrenia. We have previously developed a (11)C-labeled agonist PET ligand ([(11)C]Cimbi-36), and the aim of this study was to identify a (18)F-labeled analogue of this PET-ligand. Thus, we developed a convergent radiochemical approach giving easy access to 5 different (18)F-labeled ligands structurally related to Cimbi-36 from a common (18)F-labeled intermediate. After intravenous injection, all ligands entered the pig brain. However, since within-scan intervention with ketanserin, a known orthosteric 5-HT2A receptor antagonist, did not result in significant blocking, the radioligands seem unsuitable for neuroimaging of the 5-HT2AR in vivo.

U2 - 10.1016/j.bmc.2016.08.056

DO - 10.1016/j.bmc.2016.08.056

M3 - Journal article

VL - 24

SP - 5353

EP - 5356

JO - Bioorganic & Medicinal Chemistry

JF - Bioorganic & Medicinal Chemistry

SN - 0968-0896

ER -

ID: 165693100