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

作     者：GU Xiaobo CAI Gangming JIANG Mengjun ZHOU Yaoyuan ZHANG Rongjun 

作者机构：Key Laboratory of Nuclear MedicineMinistry of HealthJiangsu Key Laboratory of Molecular Nuclear MedicineJiangsu Institute of Nuclear Medicine Department of Clinical Laboratory Sciencethe First Wuxi Affiliated Hospital of Nanjing Medical UniversityWuxi Clinical Science Research Institute 

出 版 物：《Nuclear Science and Techniques》 (核技术（英文）)

年 卷 期：2013年第24卷第6期

页      面：50-55页

核心收录：

学科分类：0831[工学-生物医学工程（可授工学、理学、医学学位）] 100207[医学-影像医学与核医学] 1006[医学-中西医结合] 1002[医学-临床医学] 1001[医学-基础医学(可授医学、理学学位)] 08[工学] 1010[医学-医学技术（可授医学、理学学位）] 100106[医学-放射医学] 100602[医学-中西医结合临床] 10[医学] 

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) 

主　　题：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 

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 *** 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 *** 18F-FB-NGA was prepared with NGA by conjugation with Nsuccinimidyl-4-18F-fluorobenzoate(18F-SFB)and purified with PD-10 desalting *** radiolabeling yield and radiochemical purity of 18F-FB-NGA were determined by *** with 18F-F–,the total time for 18F-FB-NGA was about 120±10 *** 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/*** of 18F-FB-NGA in normal mice was investigated after injection through the tail *** results showed that the liver accumulated 39.47±3.42 and 12.12±6.11%ID/g at 10 and 30 min after injection,*** MicroPET images in mice were acquired with and without block after injection of the radiotracer,*** liver activity accumulation was observed at 5 min after injection in normal *** 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.