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Synthesis of 11 C‐labelled acamprosate for PET studies
Author(s) -
Courtyn Jan,
Goethals Patrick,
Eycken Johan Van der,
Dams Richard
Publication year - 2001
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.490
Subject(s) - chemistry , labelling , radiosynthesis , radiochemistry , acamprosate , high performance liquid chromatography , yield (engineering) , acylation , specific activity , aqueous solution , nuclear chemistry , in vivo , positron emission tomography , chromatography , nuclear medicine , organic chemistry , biochemistry , enzyme , catalysis , medicine , naltrexone , materials science , receptor , microbiology and biotechnology , biology , opioid , metallurgy
A method for labelling acamprosate (calcium N ‐acetyl homotaurinate), an anti‐craving compound for ethanol, with 11 C, has been developed for in vivo studies with positron emission tomography (PET). The synthesis was based on the acylation of homotaurinate using [ 11 C]acetyl chloride as the labelling agent. Reversed‐phase HPLC in highly aqueous mobile phase conditions was used for product purification. The radiochemical yield achieved was about 1.14 GBq (31 mCi) with a specific radioactivity of 8.14 GBq/µmol (220 mCi/µmol). For the identification of 11 C‐radioactivity and determination of specific radioactivities, HPLC and 1 H‐NMR were used. Copyright © 2001 John Wiley & Sons, Ltd.