2008•Radiochimica ActaRequires access
Radiosynthesis of the adenosine A3 receptor ligand 5-(2-[18F]fluoroethyl) 2,4-diethyl-3-(ethylsulfanylcarbonyl)- 6-phenylpyridine-5-carboxylate ([18F]FE@SUPPY)
Wolfgang Wadsak, Leonhard‐Key Mien, Karem Shanab, Karl Weber, Bernd M. Schmidt, Karoline M. Sindelar, Dagmar E. Ettlinger, Daniela Haeusler, Helmut Spreitzer, Bernhard K. Keppler, Helmut Viernstein, Robert Dudczak, Kurt Kletter, Markus Mitterhauser
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Abstract
Since to date very limited information on the distribution and function of the adenosine A 3 receptor is available, the development of a suitable radioligand is needed. Such a selective radioligand can then be used for quantitative autoradiography, preclinical studies in animals and subsequent human PET applications. Recently, a promising candidate compound, 5-(2-fluoroethyl) 2,4-diethyl-3-(ethylsulfanylcarbonyl)-6-phenylpyridine-5-carboxylate (FE@SUPPY), has been presented. The successful preparation of a suitable labelling precursor and the evaluation and optimization of the radiosynthesis of [ 18 F] FE@SUPPY is presented herewith. For satisfactory yields, a reaction temperature of 75 °C has to be applied for at least 20 min using 8–10 mg of precursor. Until now, 15 complete high-scale radiosyntheses were performed. Starting from an average of 51±12 GBq (average ±SD; range: 30–67 GBq) [ 18 F]fluoride, 9.4–3.6 GBq of formulated [ 18 F]FE@SUPPY (32.3±12.4%, based on [ 18 F]fluoride, corrected for decay) were prepared in <105 min.