Neutrophil-Specific PET Cellular Imaging for ARDS

本研究的目的是开发一种PET成像方法，通过靶向中性粒细胞特异性表达的趋化因子受体CXCR2，可以特异性地检测肺和其他器官的中性粒细胞，目前还没有体内成像技术可以特异性地显示通过全身扫描识别的人体以及动物的局部中性粒细胞浸润。因此，我们的目标是通过使用尖端的PET分子成像技术，可以实现高灵敏度的生物标志物分子的可视化。考虑到未来的临床应用，为了开发在临床环境中易于操作的F18标记的小分子示踪剂，我们设计并合成了今年针对CXCR 2的PET示踪剂候选物。为了评价这些放射性示踪剂的亲和力，首先合成冷参考，即它们的非放射性参考。直接放射性标记无需特殊制备的甲苯磺酸酯前体也是方法学研究，以促进放射性标记方案从原始结构。合成了尿素系列化合物的冷对照品和相应的放射性标记前体。

The goal of this study is to develop a PET imaging assay that can specifically detect neutrophils of the lung and other organs by targeting the CXCR2, achemokine receptor specifically expressed on neutrophils.At present, there is no in vivo imaging technique that can specifically visualize local neutrophil infiltration identified via systemic scanning of human body as well as animals. Therefore, we aim to achieve this by using cutting edge PET molecular imaging technology, which can visualize biomarker molecules with high sensitivity.Considering future clinical applications, to develop of small molecule tracers for F18-labeling that are easy to handle in clinical settings, we designed and synthesized PET tracer candidates targeting CXCR2 in this year. To evaluate the affinity of these radiotracers, cold references, i.e. their non-radioactive references, were synthesized first. The direct radiofluorination without the special preparation of tosylate precursor was also methodology investigation to facilitate the radiolabelling protocol from original structures. In contract, the cold references of urea series of compounds and the corresponding precursors for radiolabelling were also synthesized.