Neutrophil-Specific PET Cellular Imaging for ARDS

本研究的目的是开发一种PET成像检测方法，通过靶向特异性表达于中性粒细胞上的趋化因子受体CXCR2，特异性检测肺和其他器官的中性粒细胞。目前，还没有一种体内成像技术可以通过人体和动物的全身扫描特异性地显示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分子成像技术来实现这一目标，该技术可以以高灵敏度可视化生物标志物分子。考虑到未来的临床应用，为了开发易于临床操作的f18标记小分子示踪剂，我们在今年设计并合成了靶向CXCR2的PET候选示踪剂。为了评价这些放射性示踪剂的亲和力，首先合成了冷参考，即它们的非放射性参考。对不需特别制备甲酰戊酸前体的直接放射性氟化也进行了方法学研究，以方便原始结构的放射性标记方案。同时，还合成了尿素系列化合物的冷参考文献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.