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Radiolabeling of ginkgolide B with 18 F
Author(s) -
Suehiro Makiko,
Simpson Norman R.,
van Heertum Ronald
Publication year - 2004
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.836
Subject(s) - chemistry , nucleophile , in vivo , trifluoromethanesulfonate , yield (engineering) , radiochemistry , stereochemistry , specific activity , positron , organic chemistry , materials science , physics , microbiology and biotechnology , quantum mechanics , electron , metallurgy , biology , enzyme , catalysis
Ginkgolide B, a terpene trilactone constituent of Gingko biloba extracts and an antagonist for the platelet activating factor (PAF) receptor, was radiolabeled with the positron emitter 18 F for visualizing its in vivo behavior using positron emission tomography (PET). The 7‐[ 18 F]fluoro analog of ginkgolide B (7‐ 18 FGB) was synthesized via nucleophilic displacement of the triflate group at C7 with [ 18 F]fluoride. The reaction was complete in 5–10 min, affording 7‐ 18 FGB in an average radiochemical yield of approximately 16% (decay corrected). The average specific activity at E.O.S. was approximately 40 GBq/µmol, and the radiochemical and chemical purity was greater than 95%. Copyright © 2004 John Wiley & Sons, Ltd.