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Convergent F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT receptor PET ligands. | LitMetric

Convergent F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT receptor PET ligands.

Bioorg Med Chem

Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 København Ø, Denmark. Electronic address:

Published: November 2016

AI Article Synopsis

  • PET scans can be important for studying diseases like depression, Alzheimer's, and schizophrenia through the 5-HT receptor system.
  • The researchers created a F-labeled version of an earlier C-labeled PET ligand called Cimbi-36, resulting in 5 new ligands.
  • However, tests showed that these new ligands didn't effectively block the 5-HT receptors in the brain, making them less useful for imaging in living subjects.

Article Abstract

Positron emission tomography (PET) investigations of the 5-HT receptor (5-HTR) system can be used as a research tool in diseases such as depression, Alzheimer's disease and schizophrenia. We have previously developed a C-labeled agonist PET ligand ([C]Cimbi-36), and the aim of this study was to identify a F-labeled analogue of this PET-ligand. Thus, we developed a convergent radiochemical approach giving easy access to 5 different F-labeled ligands structurally related to Cimbi-36 from a common F-labeled intermediate. After intravenous injection, all ligands entered the pig brain. However, since within-scan intervention with ketanserin, a known orthosteric 5-HT receptor antagonist, did not result in significant blocking, the radioligands seem unsuitable for neuroimaging of the 5-HTR in vivo.

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Source
http://dx.doi.org/10.1016/j.bmc.2016.08.056DOI Listing

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