Nuclear Science and Techniques

《核技术》(英文版) ISSN 1001-8042 CN 31-1559/TL     2019 Impact factor 1.556

Nuclear Science and Techniques ›› 2013, Vol. 24 ›› Issue (6): 060301 doi: 10.13538/j.1001-8042/nst.2013.06.016

• NUCLEAR CHEMISTRY,RADIOCHEMISTRY,RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE • Previous Articles     Next Articles

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

GU Xiaobo1 CAI Gangming1 JIANG Mengjun1,2#br# ZHOU Yaoyuan1 ZHANG Rongjun1,*   

  1. 1Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine,Wuxi 214063, China
    2Department of Clinical Laboratory Science, the First Wuxi Affiliated Hospital of Nanjing Medical University, Wuxi Clinical Science Research Institute, Wuxi 214063, China
  • Contact: ZHANG Rongjun E-mail:zhangrongjun@jsinm.org
  • Supported by:

    Supported by Jiangsu Province’s Key Medical Talents Program (No. RC2007097), Natural Science Foundation of Jiangsu Province, China (No. BK2010154) and Science Foundation of Health Department of Jiangsu Province (No.H201226).

GU Xiaobo, CAI Gangming, JIANG Mengjun. Synthesis and biological evaluation of 18F-FB-NGA as a hepatic asialoglycoprotein receptor PET imaging agent.Nuclear Science and Techniques, 2013, 24(6): 060301     doi: 10.13538/j.1001-8042/nst.2013.06.016

Abstract:

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.

Key words: Asialoglycoprotein receptor, 18F-FB-NGA, Biodistribution, PET Imaging