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

Research output: Contribution to journalJournal articleResearchpeer-review

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

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.

Original languageEnglish
JournalBioorganic & Medicinal Chemistry
Volume24
Pages (from-to)5353-5356
Number of pages4
ISSN0968-0896
DOIs
Publication statusPublished - 2016

ID: 165693100