Radiosynthesis of [5-[ 11C]methanesulfonyl-2-((S)-2,2,2- trifluoro-1-methyl-ethoxy)-phenyl]-[5-(tetrahydro-pyran-4-yl)-1, 3-dihydro-isoindol-2-yl]-methanone ([ 11C]RO5013853), a novel PET tracer for the glycine transporter type i (GlyT1)

Emmanuel Pinard, Serge Burner, Philipp Cueni, Thomas Hartung, Roger D. Norcross, Philipp Schmid, Pius Waldmeier, Guy Zielinski, Hayden T. Ravert, Daniel P. Holt, Robert F. Dannals

Research output: Contribution to journalArticlepeer-review

Abstract

The glycine transporter type 1 (GlyT1) has emerged as a key novel target for the treatment of schizophrenia. We have recently discovered and developed [ 11C]RO5013853 as a novel positron emission tomography tracer for GlyT1 for which a reliable five-step synthetic route was established. The incorporation of the radioisotope was achieved in the final step through methylation of a sodium sulfinate precursor, itself easily accessible upon reduction of the corresponding sulfonyl-chloride analog. [ 11C] RO5013853 was prepared with high specific activity (>49 GBq/μmol) and high radiochemical purity (100%). A validation study of [ 11C]RO5013853 in animal imaging studies is in progress.

Original languageEnglish (US)
Pages (from-to)702-707
Number of pages6
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume54
Issue number11
DOIs
StatePublished - Sep 1 2011

Keywords

  • GlyT1
  • PET
  • [ C]RO5013853
  • carbon-11
  • glycine
  • radiolabeling
  • transporter

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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