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
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 P...
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| Format: | Article |
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MDPI AG
2020-04-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/25/7/1633 |
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| author | 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 |
| author_facet | 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 |
| author_sort | Susann Schröder |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-10T20:43:10Z |
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| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T20:43:10Z |
| publishDate | 2020-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-a6ba38be238e498699ccd57b2c5d72c92023-11-19T20:30:06ZengMDPI AGMolecules1420-30492020-04-01257163310.3390/molecules25071633PET 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 StrategySusann Schröder0Thu Hang Lai1Magali Toussaint2Mathias Kranz3Alexandra Chovsepian4Qi Shang5Sladjana Dukić-Stefanović6Winnie Deuther-Conrad7Rodrigo Teodoro8Barbara Wenzel9Rareş-Petru Moldovan10Francisco Pan-Montojo11Peter Brust12ROTOP Pharmaka Ltd., Department of Research and Development, Dresden 01328, GermanyHelmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, GermanyHelmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, GermanyPET Imaging Center, University Hospital of North Norway (UNN), Tromsø 9009, NorwayUniversity Hospital Munich, Department of Psychiatry, Ludwig-Maximilians-Universität (LMU) Munich, Munich 80336, GermanyUniversity Hospital Munich, Department of Neurology, Ludwig-Maximilians-Universität (LMU) Munich, Munich 81377, GermanyHelmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, GermanyHelmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, GermanyHelmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, GermanyHelmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, GermanyHelmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, GermanyUniversity Hospital Munich, Department of Psychiatry, Ludwig-Maximilians-Universität (LMU) Munich, Munich 80336, GermanyHelmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, GermanyThe 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.https://www.mdpi.com/1420-3049/25/7/1633adenosine A<sub>2A</sub> receptorParkinson’s diseaserotenone-based mouse modelPET imaging[<sup>18</sup>F]<b>FESCH</b>two-step one-pot radiosynthesis |
| spellingShingle | 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 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 Molecules adenosine A<sub>2A</sub> receptor Parkinson’s disease rotenone-based mouse model PET imaging [<sup>18</sup>F]<b>FESCH</b> two-step one-pot radiosynthesis |
| title | 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 |
| title_full | 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 |
| title_fullStr | 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 |
| title_full_unstemmed | 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 |
| title_short | 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 |
| title_sort | 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 |
| topic | adenosine A<sub>2A</sub> receptor Parkinson’s disease rotenone-based mouse model PET imaging [<sup>18</sup>F]<b>FESCH</b> two-step one-pot radiosynthesis |
| url | https://www.mdpi.com/1420-3049/25/7/1633 |
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