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The Capital Region of Denmark - a part of Copenhagen University Hospital
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Convergent (18)F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT2A receptor PET ligands

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  1. Synthesis and evaluation of [¹¹C]Cimbi-806 as a potential PET ligand for 5-HT₇ receptor imaging

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  1. Prevalence of cognitive impairment and its relation to mental health in Danish lymphoma survivors

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  2. A high-resolution in vivo atlas of the human brain's benzodiazepine binding site of GABAA receptors

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  3. Nondisplaceable Binding Is a Potential Confounding Factor in 11C-PBR28 Translocator Protein PET Studies

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  4. Reward processing in major depressive disorder and prediction of treatment response - Neuropharm study

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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 and Medicinal Chemistry
Volume24
Issue number21
Pages (from-to)5353-5356
Number of pages4
ISSN0968-0896
DOIs
Publication statusPublished - 1 Nov 2016

ID: 49675081