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
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
Affiliations
Susann Schröder
ROTOP Pharmaka Ltd., Department of Research and Development, Dresden 01328, Germany
Thu Hang Lai
Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, Germany
Magali Toussaint
Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, Germany
Mathias Kranz
PET Imaging Center, University Hospital of North Norway (UNN), Tromsø 9009, Norway
Alexandra Chovsepian
University Hospital Munich, Department of Psychiatry, Ludwig-Maximilians-Universität (LMU) Munich, Munich 80336, Germany
Qi Shang
University Hospital Munich, Department of Neurology, Ludwig-Maximilians-Universität (LMU) Munich, Munich 81377, Germany
Sladjana Dukić-Stefanović
Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, Germany
Winnie Deuther-Conrad
Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, Germany
Rodrigo Teodoro
Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, Germany
Barbara Wenzel
Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, Germany
Rareş-Petru Moldovan
Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, Germany
Francisco Pan-Montojo
University Hospital Munich, Department of Psychiatry, Ludwig-Maximilians-Universität (LMU) Munich, Munich 80336, Germany
Peter Brust
Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, Germany
The adenosine A2A receptor (A2AR) is regarded as a particularly appropriate target for non-dopaminergic treatment of Parkinson’s disease (PD). An increased A2AR 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 A2AR upregulation in PD. For that purpose, we selected the known A2AR-specific radiotracer [18F]FESCH and developed a simplified two-step one-pot radiosynthesis. PET images showed a high uptake of [18F]FESCH in the mouse striatum. Concomitantly, metabolism studies with [18F]FESCH revealed the presence of a brain-penetrant radiometabolite. In rotenone-treated mice, a slightly higher striatal A2AR binding of [18F]FESCH was found. Nonetheless, the correlation between the increased A2AR levels within the proposed PD animal model remains to be further investigated.
