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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)

✍ Scribed by John L. Musachio; William B. Mathews; Hayden T. Ravert; F. Ivy Carroll; Robert F. Dannals

Publisher
John Wiley and Sons
Year
1994
Tongue
French
Weight
440 KB
Volume
34
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

(+)‐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.

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