Synthesis of fluorine-18-labelled TSPO ligands for imaging neuroinflammation with Positron Emission Tomography

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• 作者：Dirk Roeda ; Bertrand Kuhnast ; Annelaure Damont ; Fré ; dé ; ric Dollé ; ; ^{frederic.dolle@cea.fr}
• 关键词：Fluorine-18 ; 18  ; kDa TSPO ; Radioligand ; Neuroinflammation
• 刊名：Journal of Fluorine Chemistry
• 出版年：2012
• 出版时间：February, 2012
• 年：2012
• 卷：134
• 期：Complete
• 页码：107-114
• 全文大小：414 K

文摘

Fluorine-18 radiochemistry is an essential tool in Positron Emission Tomography, providing the bridge between the cyclotron-produced raw radioisotope and the biomedical image of an in vivo radioactivity distribution. From the fluorine-18 labelled radioligands for the translocator protein 18 kDa that are produced in our laboratory, namely [¹⁸F]FEDAA1106, 6-[¹⁸F]F-PBR28, [¹⁸F]PBR111 and [¹⁸F]DPA-714, we address various aspects of fluorine-18 radiochemistry, such as rationales of radiotracer design, radioisotope production and [¹⁸F]fluoride activation, and procedures of radiofluorination, purification and formulation. Automation of the radiochemistry process has become indispensable in order to assure a constant radiopharmaceutical quality and reproducible radiochemical yields as well as to meet the required radiation protection aspects.