Synthesis and biological evaluation of ^(18)F-FB-NGA as a hepatic asialoglycoprotein receptor PET imaging agent

查看全文 作　　者：GU [1]Xiaobo;CAI [1]Gangming;JIANG [1,2]Mengjun;ZHOU [1]Yaoyuan;ZHANG [1]Rongjun 机构地区：[1]Key Laboratory of Nuclear Medicine,Ministry of Health,Jiangsu Key Laboratory of Molecular Nuclear Medicine,Jiangsu Institute of Nuclear Medicine;[2]Department of Clinical Laboratory Science,the First Wuxi Affiliated Hospital of Nanjing Medical University,Wuxi Clinical Science Research Institute 出　　处：《Nuclear Science and Techniques》索引2013年第24卷第6期,共6页 基　　金：Supported by Jiangsu Province’s Key Medical Talents Program(No.RC2007097);Natural Science Foundation of Jiangsu Province,China(No.BK2010154);Science Foundation of Health Department of Jiangsu Province(No.H201226) 摘　　要：Asialoglycoprotein receptor(ASGP-R)is a hepatic membrane receptor that uniquely exists on the surface of mammalian hepatocytes,and has been used as target of liver functional imaging agents for many years.We labeled the Galactosyl-neoglycoalbumin(NGA)with 18F to get a PET molecular probe 18F-FB-NGA and evaluated its ability as a liver functional PET imaging agent.The 18F-FB-NGA was prepared with NGA by conjugation with Nsuccinimidyl-4-18F-fluorobenzoate(18F-SFB)and purified with PD-10 desalting column.The radiolabeling yield and radiochemical purity of 18F-FB-NGA were determined by radio-HPLC.Starting with 18F-F–,the total time for 18F-FB-NGA was about 120±10 min.The decay-corrected radiochemical yield is about 25–30%.The radiochemical purity of purified 18F-FB-NGA was more than 98%.Labeled with 185–1850 MBq 18F-SFB,the specific activity of 18F-FBNGA was estimated to be 7.83–78.3 TBq/mmol.Biodistribution of 18F-FB-NGA in normal mice was investigated after injection through the tail vein.The results showed that the liver accumulated 39.47±3.42 and 12.12±6.11%ID/g at 10 and 30 min after injection,respectively.Dynamic MicroPET images in mice were acquired with and without block after injection of the radiotracer,respectively.High liver activity accumulation was observed at 5 min after injection in normal group.On the contrary,the liver accumulation was significantly lower after block,indicating the specific binding to ASGP-R.18F-FB-NGA is probably a potential PET liver imaging agent. 关 键 词：去唾液酸糖蛋白受体 细胞膜受体 肝功能 PET 显像剂 生物学评价 放射化学纯度 放射性标记