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Convergent 18F-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.
Bioorg Med Chem; 24(21): 5353-5356, 2016 11 01.
Artigo em Inglês | MEDLINE | ID: mdl-27624522
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 11C-labeled agonist PET ligand ([11C]Cimbi-36), and the aim of this study was to identify a 18F-labeled analogue of this PET-ligand. Thus, we developed a convergent radiochemical approach giving easy access to 5 different 18F-labeled ligands structurally related to Cimbi-36 from a common 18F-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.
Selo DaSilva