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; K. Shanab; K. Weber; B. Schmidt; K. M. Sindelar; Dagmar E. Ettlinger; Daniela Haeusler; H. Spreitzer; B. K. Keppler; H. Viernstein; Robert Dudczak; Kurt Kletter; Markus Mitterhauser

doi:10.1524/ract.2008.1467

Published by De Gruyter (O) September 25, 2009

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 , K. Shanab , K. Weber , B. Schmidt , K. M. Sindelar , Dagmar E. Ettlinger , Daniela Haeusler , H. Spreitzer , B. K. Keppler , H. Viernstein , Robert Dudczak , Kurt Kletter and Markus Mitterhauser

From the journal rca - Radiochimica Acta

https://doi.org/10.1524/ract.2008.1467

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Summary

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.

Keywords: Adenosine; PET; Receptor; Fluorine-18; Radioligand

Received: 2007-June-21

Accepted: 2007-September-11

Published Online: 2009-09-25

Published in Print: 2008-02

Radiosynthesis of the adenosine A₃ receptor ligand 5-(2-[¹⁸F]fluoroethyl) 2,4-diethyl-3-(ethylsulfanylcarbonyl)- 6-phenylpyridine-5-carboxylate ([¹⁸F]FE@SUPPY)

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