Preparation and first evaluation of [18F]FE@SUPPY: a new PET tracer for the adenosine A3 receptor

The A3Adenosine Receptor: History and Perspectives

“…Interestingly, the 5-(2-fluoroethyl) 2,4-diethyl-3-(ethylsulfanylcarbonyl)-6-phenylpyridine-5-carboxylate compound was presented as a ligand with high affinity, able to serve as the first positron emission tomography tracer for the A 3 AR (Wadsak et al, 2008).…”

Automatisation and First Evaluation of [18F]FE@SUPPY:2, an Alternative PET-Tracer for the Adenosine A3 Receptor: A Comparison with [18F]FE@SUPPY

“…The semi-preparative HPLC system (as part of the GE TRACERlab Fx FN synthesizer) consisted of a Sykam S1021 pump (Sykam GmbH, Eresing, Germany) and a UV detector (254 nm) and a radioactivity detector in series. This precursor was prepared as described previously [1,2,7]. Briefly, OH@SUPPY, prepared according to [8] was reacted with toluene-4-sulfonyl chloride in THF and purified by recrystallization.…”

“…The residue was purified via column chromatography. The reference compound was obtained according to [1,2,7]. Briefly, OH@SUPPY [8] was treated with diethylaminosulfur trifluoride (DAST) at -78°C.…”

“…18 F]FE@SUPPY, the first PET-tracer [1,2]. Hence, having developed a series of fluoroethyl-esters over the last five years [24][25][26][27][28][29], it was obvious for us to develop [ 18 F]FE@SUPPY:2.…”

“…18 F]fluoroethyl) 2,4-diethyl-3-(ethylsulfanylcarbonyl)-6-phenylpyridine-5-carboxylate) as the first PET-tracer for the A3AR [1,2]. The radiosynthesis was performed in a simple one-pot one-step reaction with good and reliable radiolabeling yields and good specific radioactivities.…”