Synthesis of a radiotracer for studying σ receptors in vivo using PET: (+)‐N‐[11C]‐benzyl‐N‐normetazocine (1S, 5S,9S‐(+)‐cis‐2‐[11C]‐2′‐hydroxy‐5,9‐dimethyl‐6,7‐benzomorphan)

John L. Musachio, William B. Mathews, Hayden T. Ravert, F. Ivy Carroll, Robert F. Dannals

Research output: Contribution to journalArticlepeer-review

Abstract

(+)‐N‐[11C]‐Benzyl‐N‐normetazocine (1S,5S,9S‐(+)‐cis‐2‐[11C]‐benzyl‐2′‐hydroxy‐5,9‐dimethyl‐6,7‐benzomorphan), a potent and selective ligand for the σ receptor, was prepared by N‐benzylation of (+)‐cis‐N‐normetazocine with [α‐11C]‐benzyl iodide in ethanol using sodium hydrogen carbonate as the proton acceptor. The radiotracer was purified by semi‐preparative reverse‐phase HPLC. The average specific activity was 746 mCi/μmol calculated at end‐of‐synthesis (EOS). The average time of synthesis including formulation was 35 minutes.

Original languageEnglish (US)
Pages (from-to)49-57
Number of pages9
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume34
Issue number1
DOIs
StatePublished - Jan 1994

ASJC Scopus subject areas

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

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