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

14 Citationer (Scopus)


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.

TidsskriftBioorganic and Medicinal Chemistry
Udgave nummer21
Sider (fra-til)5353-5356
Antal sider4
StatusUdgivet - 1 nov. 2016


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