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.

中文翻译：

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基于鱼藤酮的帕金森病小鼠模型中腺苷 A2A 受体的 PET 成像与 [18F] FESCH 通过简化的两步一锅放射性标记策略合成

腺苷 A2A 受体 (A2AR) 被认为是非多巴胺能治疗帕金森病 (PD) 的特别合适的靶点。在 PD 早期阶段的人类纹状体以及患有 PD 和运动障碍的患者中发现 A2AR 可用性增加。这项小动物正电子发射断层扫描/磁共振 (PET/MR) 成像研究的目的是研究鱼藤酮治疗的小鼠是否反映了 PD 纹状体 A2AR 上调的方面。为此，我们选择了已知的 A2AR 特异性放射性示踪剂 [18F]FESCH，并开发了一种简化的两步一锅法放射性合成。PET 图像显示小鼠纹状体中 [18F]FESCH 的高摄取。同时，[18F]FESCH 的代谢研究揭示了脑渗透性放射性代谢物的存在。在鱼藤酮处理的小鼠中，发现 [18F]FESCH 的纹状体 A2AR 结合略高。尽管如此，所提出的 PD 动物模型中 A2AR 水平增加之间的相关性仍有待进一步研究。