These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Convergent 18F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT2A receptor PET ligands.
    Author: Petersen IN, Villadsen J, Hansen HD, Jensen AA, Lehel S, Gillings N, Herth MM, Knudsen GM, Kristensen JL.
    Journal: Bioorg Med Chem; 2016 Nov 01; 24(21):5353-5356. PubMed ID: 27624522.
    Abstract:
    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.
    [Abstract] [Full Text] [Related] [New Search]