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(11)C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand.

Abstract
Pimavanserin is a selective serotonin 2A receptor (5-HT2AR) inverse agonist that has shown promise for treatment of psychotic symptoms in patients with Parkinson's disease. Here, we detail the (11)C-labeling and subsequently evaluate pimavanserin as a PET-radioligand in pigs. [(11)C]Pimavanserin was obtained by N-methylation of an appropriate precursor using [(11)C]MeOTf in acetone at 60°C giving radiochemical yields in the range of 1-1.7GBq (n=4). In Danish Landrace pigs the radio ligand readily entered the brain and displayed binding in the cortex in accordance with the distribution of 5-HT2ARs. However, this binding could not be blocked by either ketanserin or pimavanserin itself, indicating high nonspecific binding. The lack of displacement by the 5-HT2R antagonist and binding in the thalamus suggests that [(11)C]pimavanserin is not selective for the 5-HT2AR in pigs.
AuthorsValdemar L Andersen, Hanne D Hansen, Matthias M Herth, Agnete Dyssegaard, Gitte M Knudsen, Jesper L Kristensen
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 25 Issue 5 Pg. 1053-6 (Mar 01 2015) ISSN: 1464-3405 [Electronic] England
PMID25655720 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2015 Elsevier Ltd. All rights reserved.
Chemical References
  • Carbon Radioisotopes
  • Ligands
  • Piperidines
  • Radiopharmaceuticals
  • Receptor, Serotonin, 5-HT2A
  • Serotonin 5-HT2 Receptor Agonists
  • Urea
  • pimavanserin
Topics
  • Animals
  • Carbon Radioisotopes (analysis, metabolism)
  • Ligands
  • Methylation
  • Piperidines (analysis, metabolism)
  • Positron-Emission Tomography
  • Radiopharmaceuticals (analysis, metabolism)
  • Receptor, Serotonin, 5-HT2A (analysis, metabolism)
  • Serotonin 5-HT2 Receptor Agonists (analysis, metabolism)
  • Swine
  • Urea (analogs & derivatives, analysis, metabolism)

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