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Wolfgang Wadsak, Leonhard-Key Mien, K. Shanab, K. M. Sindelar, Dagmar E. Ettlinger, Daniela Haeusler, H. Spreitzer, B. K. Keppler, H. Viernstein, Robert Dudczak, Kurt Kletter, Markus Mitterhauser
Radiosynthesis of the adenosine A3 receptor ligand 5-(2-[18F]fluoroethyl) 2,4-diethyl-3-(ethylsulfanylcarbonyl)- 6-phenylpyridine-5-carboxylate ([18F]FE@SUPPY)
Keywords: Adenosine, PET, Receptor, Fluorine-18, radioligand
Since to date very limited information on the distribution and function of the adenosine A3 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 [18F] 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) [18F]fluoride, 9.4–3.6 GBq of formulated [18F]FE@SUPPY (32.3±12.4%, based on [18F]fluoride, corrected for decay) were prepared in <105 min.
Radiochimica Acta, Oldenbourg Wissenschaftsverlag
Print ISSN: 0033-8230
Volume: 96, 02/2008
Pages: 119 - 124