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基于简化两步一锅法放射性标记策略合成的[F]FESCH在鱼藤酮诱导的帕金森病小鼠模型中对腺苷A受体的PET成像

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

作者信息

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

机构信息

ROTOP Pharmaka Ltd., Department of Research and Development, Dresden 01328, Germany.

Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Leipzig 04318, Germany.

出版信息

Molecules. 2020 Apr 2;25(7):1633. doi: 10.3390/molecules25071633.

DOI:10.3390/molecules25071633
PMID:32252340
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7180622/
Abstract

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

摘要

腺苷A受体（AR）被认为是帕金森病（PD）非多巴胺能治疗的一个特别合适的靶点。在PD早期的人类纹状体以及患有PD和运动障碍的患者中，已发现AR的可用性增加。这项小动物正电子发射断层扫描/磁共振（PET/MR）成像研究的目的是调查用鱼藤酮处理的小鼠是否反映了PD中纹状体AR上调的情况。为此，我们选择了已知的AR特异性放射性示踪剂[F]，并开发了一种简化的两步一锅法放射性合成方法。PET图像显示[F]在小鼠纹状体中有高摄取。同时，用[F]进行的代谢研究揭示了一种可穿透脑的放射性代谢物的存在。在用鱼藤酮处理的小鼠中，发现[F]的纹状体AR结合略高。尽管如此，在拟议的PD动物模型中AR水平增加之间的相关性仍有待进一步研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/e4309d7c6dfc/molecules-25-01633-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/686a75916e8b/molecules-25-01633-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/60f20c945111/molecules-25-01633-sch001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/019e96a114c6/molecules-25-01633-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/fe2b6f29b544/molecules-25-01633-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/d4ed7ed8a4d1/molecules-25-01633-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/9123321f5936/molecules-25-01633-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/e4309d7c6dfc/molecules-25-01633-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/686a75916e8b/molecules-25-01633-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/60f20c945111/molecules-25-01633-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/fbd3829d4db8/molecules-25-01633-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/019e96a114c6/molecules-25-01633-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/fe2b6f29b544/molecules-25-01633-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/d4ed7ed8a4d1/molecules-25-01633-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/9123321f5936/molecules-25-01633-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d81/7180622/e4309d7c6dfc/molecules-25-01633-g007.jpg

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