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The adenosine A 2A  receptor (A 2A R) is regarded as a particularly appropriate target for non-dopaminergic treatment of Parkinson’s disease (PD). An increased A 2A R availability has been found in the human striatum at early stages of PD and in patients with PD and dyskinesias. The aim of this small animal positron emission tomography/magnetic resonance (PET/MR) imaging study was to investigate whether rotenone-treated mice reflect the aspect of striatal A 2A R upregulation in PD. For that purpose, we selected the known A 2A R-specific radiotracer [ 18 F] FESCH  and developed a simplified two-step one-pot radiosynthesis. PET images showed a high uptake of [ 18 F] FESCH  in the mouse striatum. Concomitantly, metabolism studies with [ 18 F] FESCH  revealed the presence of a brain-penetrant radiometabolite. In rotenone-treated mice, a slightly higher striatal A 2A R binding of [ 18 F] FESCH  was found. Nonetheless, the correlation between the increased A 2A R levels within the proposed PD animal model remains to be further investigated.

molecules

PET Imaging of the Adenosine A2A Receptor in the Rotenone-Based Mouse Model of Parkinson’s Disease with [18F]FESCH Synthesized by a Simplified Two-Step One-Pot Radiolabeling Strategy