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Synthesis of a radiotracer for studying σ receptors in vivo using PET: (+)‐ N ‐[ 11 C]‐benzyl‐ N ‐normetazocine (1 S , 5 S ,9 S ‐(+)‐ cis ‐2‐[ 11 C]‐2′‐hydroxy‐5,9‐dimethyl‐6,7‐benzomorphan)
Author(s) -
Musachio John L.,
Mathews William B.,
Ravert Hayden T.,
Carroll F. Ivy,
Dannals Robert F.
Publication year - 1994
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580340107
Subject(s) - chemistry , sodium iodide , iodide , in vivo , ligand (biochemistry) , specific activity , high performance liquid chromatography , ethanol , stereochemistry , medicinal chemistry , radiochemistry , receptor , nuclear chemistry , chromatography , organic chemistry , biochemistry , microbiology and biotechnology , biology , enzyme
(+)‐ N ‐[ 11 C]‐Benzyl‐ N ‐normetazocine (1 S ,5 S ,9 S ‐(+)‐ cis ‐2‐[ 11 C]‐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‐ 11 C]‐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.