Neuroinflammation in Low-Level PM2.5-Exposed Rats Illustrated by PET via an Improved Automated Produced [¹⁸F]FEPPA: A Feasibility Study.

IF 2.2 4区医学 Q3 BIOCHEMICAL RESEARCH METHODS

Molecular Imaging Pub Date : 2022-06-07 eCollection Date: 2022-01-01 DOI:10.1155/2022/1076444

Mei-Fang Cheng, Tsun-Jen Cheng, Yue Leon Guo, Ching-Hung Chiu, Hung-Ming Wu, Ruoh-Fang Yen, Ya-Yao Huang, Wen-Sheng Huang, Chyng-Yann Shiue

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引用次数: 1

Abstract

Background: [¹⁸F]FEPPA is a potent TSPO imaging agent that has been found to be a potential tracer for imaging neuroinflammation. In order to fulfill the demand of this tracer for preclinical and clinical studies, we have developed a one-pot automated synthesis with simplified HPLC purification of this tracer, which was then used for PET imaging of neuroinflammation in fine particulate matter- (PM2.5-) exposed rats.

Results: Using this automated synthesis method, the RCY of the [¹⁸F]FEPPA was 38 ± 4% (n = 17, EOB) in a synthesis time of 83 ± 8 min from EOB. The radiochemical purity and molar activities were greater than 99% and 209 ± 138 GBq/μmol (EOS, n = 15), respectively. The quality of the [¹⁸F]FEPPA synthesized by this method met the U.S. Pharmacopoeia (USP) criteria. The stability test showed that the [¹⁸F]FEPPA was stable at 21 ± 2°C for up to 4 hr after the end of synthesis (EOS). Moreover, microPET imaging showed that increased tracer activity of [¹⁸F]FEPPA in the brain of PM2.5-exposed rats (n = 6) were higher than that of normal controls (n = 6) and regional-specific.

Conclusions: Using the improved semipreparative HPLC purification, [¹⁸F]FEPPA has been produced in high quantity, high quality, and high reproducibility and, for the first time, used for PET imaging the effects of PM2.5 in the rat brain. It is ready to be used for imaging inflammation in various clinical or preclinical studies, especially for nearby PET centers without cyclotrons.

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PET显示低浓度pm2.5暴露大鼠神经炎症通过改进的自动化生产[18F]FEPPA:可行性研究。

背景:[18F]FEPPA是一种有效的TSPO显像剂，已被发现是神经炎症成像的潜在示踪剂。为了满足该示踪剂临床前和临床研究的需求，我们开发了一锅自动化合成方法，简化HPLC纯化该示踪剂，然后用于细颗粒物(PM2.5)暴露大鼠神经炎症的PET成像。结果:采用该自动合成方法，[18F]FEPPA的RCY为38±4% (n = 17, EOB)，合成时间为83±8 min。放化学纯度大于99%，摩尔活性大于209±138 GBq/μmol (EOS, n = 15)。该方法合成的[18F]FEPPA质量符合美国药典(USP)标准。稳定性测试表明，[18F]FEPPA在合成结束(EOS)后，在21±2°C下稳定达4小时。此外，微pet成像显示pm2.5暴露大鼠(n = 6)脑内[18F]FEPPA示踪剂活性升高，高于正常对照组(n = 6)，且具有区域特异性。结论:采用改进的半制备型高效液相色谱纯化方法[18F]，制备出了高数量、高质量、高重现性的FEPPA，并首次用于PET成像PM2.5在大鼠脑内的作用。它可以用于各种临床或临床前研究中的炎症成像，特别是对于附近没有回旋加速器的PET中心。

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来源期刊

Molecular Imaging Biochemistry, Genetics and Molecular Biology-Biotechnology

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3.60%

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期刊介绍： Molecular Imaging is a peer-reviewed, open access journal highlighting the breadth of molecular imaging research from basic science to preclinical studies to human applications. This serves both the scientific and clinical communities by disseminating novel results and concepts relevant to the biological study of normal and disease processes in both basic and translational studies ranging from mice to humans.

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