中文摘要：

G-蛋白偶联受体（TGR5）是一类位于细胞膜上的胆汁酸受体,与体内的糖代谢、能量代谢和胰高血糖素样多肽1的分泌密切相关.相对于正常组织,TGR5在多种肿瘤组织中过量表达,并与患者的预后相关,是肿瘤诊断、治疗和预后评估的一个潜在靶点.因此,利用点击化学的方法简单高效的制备了一种靶向TGR5的18-F-PET探针[18FF] FEA-LCA.该探针具有较高的放射化学产率（66％～74％）、比活度（大于300 PBq/mol）和放射化学纯度（大于99％）.[18F]FEA-LCA具有其母体化合物LCA相似的亲脂性,并具有良好的体外稳定性.本工作为进一步研究[18F] FEA-LCA作为TGR5过量表达的肿瘤的PET探针奠定了良好的基础.

英文摘要：

G protein-coupled receptor （TGR5） is a cell-surface bile acid receptor which is closely related to glucose metabolism, energy expenditure and the secretion of glucagon-like peptide-1. TGR5 is a potential target for diagnosis, treatment and prognosis evaluation of the tumors, whose expression is strongly upregulated in many tumors compared to expres- sion levels in normal tissues and is associated with the prognosis of the patients. Therefore, the 18F-PET probe [18F]FEA-LCA was prepared with the simply and efficiency click chemis- try method with a high radiochemical yield （66%-74%）, high radiochemical purity （〉99%）, and high specific activity （〉300 PBq/mol）. [18F]FEA-LCA has a similar lipophilicity to the parental bile acid lithocholic acid and a high metabolic stability in vitro.This work make a solid foundation for further study the [18F]FEA-LCA as the PET probe tO the tumors of TGRS-overexpression.