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

Ida Nymann Petersen; Jonas Villadsen; Hanne Demant Hansen; Anders A Jensen; Szabolcs Lehel; Nic Gillings; Matthias M Herth; Gitte M Knudsen; Jesper L Kristensen

doi:10.1016/j.bmc.2016.08.056

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

Ida Nymann Petersen, Jonas Villadsen, Hanne Demant Hansen, Anders A Jensen, Szabolcs Lehel, Nic Gillings, Matthias M Herth, Gitte M Knudsen, Jesper L Kristensen

15 Citationer (Scopus)

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.

Originalsprog	Engelsk
Tidsskrift	Bioorganic and Medicinal Chemistry
Vol/bind	24
Udgave nummer	21
Sider (fra-til)	5353-5356
Antal sider	4
ISSN	0968-0896
DOI	https://doi.org/10.1016/j.bmc.2016.08.056
Status	Udgivet - 1 nov. 2016

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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\}",

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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

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.

UR - https://www.scopus.com/pages/publications/84991507033

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DO - 10.1016/j.bmc.2016.08.056

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SN - 0968-0896

VL - 24

SP - 5353

EP - 5356

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 21

ER -

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

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