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

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@article{3c50eea638144757b565b119e896e95c,
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 {\textcopyright} 2016 Elsevier Ltd. All rights reserved.",
year = "2016",
month = nov,
day = "1",
doi = "10.1016/j.bmc.2016.08.056",
language = "English",
volume = "24",
pages = "5353--5356",
journal = "Bioorganic and Medicinal Chemistry",
issn = "0968-0896",
publisher = "Pergamon",
number = "21",

}

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 - 2016/11/1

Y1 - 2016/11/1

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

C2 - 27624522

VL - 24

SP - 5353

EP - 5356

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

SN - 0968-0896

IS - 21

ER -

ID: 49675081