Synthesis of 3-[1H-imidazol-4-yl] propyl 4-[18F] fluorobenzyl ether ([18F] fluoroproxyfan): A potential radioligand for imaging histamine H3 receptors

Ren Iwata, Géza Horváth, Claudio Pascali, A. Bogni, Kazuhiko Yanai, Zoltán Kovács, Tatsuo Ido

Research output: Contribution to journalArticle

Abstract

3-[1H-Imidazol-4-yl]propyl 4-fluorobenzyl ether (fluoroproxyfan), a potential histamine H3 receptor ligand, was labeled with 18F for clinical PET studies. The synthesis involved the O-alkylation of 3-(1 -triphenylmethyl-1H-imidazol-4-yl)propanol with 4-[18F]fluorobenzyl bromide in the presence of silver triflate and a non-nucleophilic amine base. 4-[18F]Fluoroproxyfan was obtained within 100 min from the end of bombardment (EOB) in 10% radiochemical yield (decay corrected to EOB) with a radiochemical purity > 99% and a specific activity >150 GBq/μmol.

Original languageEnglish
Pages (from-to)873-882
Number of pages10
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume43
Issue number9
DOIs
Publication statusPublished - 2000

Keywords

  • Fluorine-18
  • Fluoroproxyfan
  • Histamine H receptor
  • PET
  • Radioligand

ASJC Scopus subject areas

  • Clinical Biochemistry
  • Molecular Medicine
  • Analytical Chemistry
  • Organic Chemistry
  • Drug Discovery
  • Pharmacology

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