Synthesis and in vitro evaluation of 18F-labelled S-fluoroalkyl diarylguanidines: Novel high-affinity NMDA receptor antagonists for imaging with PET

Edward G. Robins, Yongjun Zhao, Imtiaz Khan, Anthony Wilson, Sajinder K. Luthra, Erik Årstad

Research output: Contribution to journalArticlepeer-review

39 Citations (Scopus)


Two S-[18F]fluoroalkylated diarylguanidines were synthesized and evaluated in vitro as potential tracers for imaging of N-methyl-d-aspartate receptors (NMDARs) with positron emission tomography (PET). [18F]1 and [18F]10 were synthesized by [18F]fluoroethylation and [18F]fluoromethylation of the thiol precursor 6, respectively. [18F]1 is a promising candidate NMDAR PET tracer, with low nanomolar affinity for the NMDA PCP-site, high selectivity and moderate lipophilicity.

Original languageEnglish
Pages (from-to)1749-1751
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Issue number5
Publication statusPublished or Issued - 1 Mar 2010
Externally publishedYes


  • Fluorine-18
  • Glutamate
  • Imaging
  • NMDA
  • PET

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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