Convergent ¹⁸F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT_2A receptor PET ligands

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• 作者：Ida Nymann Petersen^a ; Jonas Villadsen^b ; Hanne Demant Hansen^b ; Anders A. Jensen^a ; Szabolcs Lehel^c ; Nic Gillings^c ; Matthias M. Herth^a ; ^c ; Gitte M. Knudsen^b ; Jesper L. Kristensen^a ; ^{jesper.kristensen@sund.ku.dk" class="auth_mail" title="E-mail the corresponding author}
• 关键词：18F-labeling ; PET ; Serotonin ; 5-HT2A receptor agonist
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2016
• 出版时间：1 November 2016
• 年：2016
• 卷：24
• 期：21
• 页码：5353-5356
• 全文大小：744 K

文摘

Positron emission tomography (PET) investigations of the 5-HT_2A receptor (5-HT_2AR) 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-HT_2A receptor antagonist, did not result in significant blocking, the radioligands seem unsuitable for neuroimaging of the 5-HT_2AR in vivo.