PET Imaging of the Adenosine A<sub>2A</sub> Receptor in the Rotenone-Based Mouse Model of Parkinson’s Disease with [<sup>18</sup>F]FESCH Synthesized by a Simplified Two-Step One-Pot Radiolabeling Strategy

oleh: Susann Schröder, Thu Hang Lai, Magali Toussaint, Mathias Kranz, Alexandra Chovsepian, Qi Shang, Sladjana Dukić-Stefanović, Winnie Deuther-Conrad, Rodrigo Teodoro, Barbara Wenzel, Rareş-Petru Moldovan, Francisco Pan-Montojo, Peter Brust

Format: Article
Diterbitkan: MDPI AG 2020-04-01

Deskripsi

The adenosine A<sub>2A</sub> receptor (A<sub>2A</sub>R) is regarded as a particularly appropriate target for non-dopaminergic treatment of Parkinson’s disease (PD). An increased A<sub>2A</sub>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<sub>2A</sub>R upregulation in PD. For that purpose, we selected the known A<sub>2A</sub>R-specific radiotracer [<sup>18</sup>F]<b>FESCH</b> and developed a simplified two-step one-pot radiosynthesis. PET images showed a high uptake of [<sup>18</sup>F]<b>FESCH</b> in the mouse striatum. Concomitantly, metabolism studies with [<sup>18</sup>F]<b>FESCH</b> revealed the presence of a brain-penetrant radiometabolite. In rotenone-treated mice, a slightly higher striatal A<sub>2A</sub>R binding of [<sup>18</sup>F]<b>FESCH</b> was found. Nonetheless, the correlation between the increased A<sub>2A</sub>R levels within the proposed PD animal model remains to be further investigated.