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Synthesis of N1′-([11C]methyl)naltrindole ([11C]MeNTI): A radioligand for positron emission tomographic studies of delta opioid receptors

✍ Scribed by John R. Lever; Chris M. Kinter; Hayden T. Ravert; John L. Musachio; William B. Mathews; Robert F. Dannals

Publisher
John Wiley and Sons
Year
1995
Tongue
French
Weight
508 KB
Volume
36
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

A delta opioid receptor antagonist, N1′‐methylnaltrindole (MeNTI), has been labeled with carbon‐11. The precursor for radiolabeling was prepared in 71% yield by benzylation of the phenolic moiety of naltrindole. Alkylation of the indole nitrogen using [^11^C]iodomethane and aqueous tetra(n‐butyl)ammonium hydroxide at 80 °C in dimethylformamide followed by hydrogenolysis (H~2~, 10% Pd‐C) of the benzyl protecting group gave [^11^C]MeNTI. The average (n = 10) time for radiosynthesis, HPLC purification and formulation was 24 min from end‐of‐bombardment. [^11^C]MeNTI of high radiochemical purity was obtained at end‐of‐synthesis with an average specific activity of 2050 mCi/μmol and radiochemical yield, based on [^11^C]iodomethane, of 6%.

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