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

Xiaobo GU; Gangming CAI; Mengjun JIANG; Yaoyuan ZHOU; Rongjun ZHANG

doi:10.13538/j.1001-8042/nst.2013.06.016

Your Location：

Home >

Browse articles >

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

NUCLEAR CHEMISTRY, RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE | Updated：2021-01-20

- Synthesis and biological evaluation of ¹⁸F-FB-NGA as a hepatic asialoglycoprotein receptor PET imaging agent
- Nuclear Science and Techniques Vol. 24, Issue 6, Article number: 060301(2013)
- Affiliations：
  
  1.Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine,Wuxi 214063, China
  2.Department of Clinical Laboratory Science, the First Wuxi Affiliated Hospital of Nanjing Medical University, Wuxi Clinical Science Research Institute, Wuxi 214063, China
- Author bio：
  
  Corresponding author. E-mail address: zhangrongjun@jsinm.org
- Funds：
- DOI：10.13538/j.1001-8042/nst.2013.06.016
  CLC：
Scan for full text
Xiaobo GU, Gangming CAI, Mengjun JIANG, et al. Synthesis and biological evaluation of ¹⁸F-FB-NGA as a hepatic asialoglycoprotein receptor PET imaging agent. [J]. Nuclear Science and Techniques 24(6):060301(2013)
DOI：

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

摘要

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,18,F to get a PET molecular probe ,18,F-FB-NGA and evaluated its ability as a liver functional PET imaging agent. The ,18,F-FB-NGA was prepared with NGA by conjugation with ,N,- succinimidyl-4-,18,F-fluorobenzoate (,18,F-SFB) and purified with PD-10 desalting column. The radiolabeling yield and radiochemical purity of ,18,F-FB-NGA were determined by radio-HPLC. Starting with ,18,F-F,–, the total time for ,18,F-FB -NGA was about 120±10 min. The decay-corrected radiochemical yield is about 25–30%. The radiochemical purity of purified ,18,F-FB-NGA was more than 98%. Labeled with 185–1850 MBq ,18,F-SFB, the specific activity of ,18,F -FB- NGA was estimated to be 7.83–78.3 TBq/mmol. Biodistribution of ,18,F-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. ,18,F-FB-NGA is probably a potential PET liver imaging agent.

关键词

Keywords

Asialoglycoprotein receptor18F-FB-NGABiodistributionPET Imaging

references

Kokudo N, Vera D R, Makuuchi M. Nucl Med Biol, 2003, 30: 845-849.

Philippe C R, Ivan M D, Marty A L, et al. Bioconjug Chem, 2010, 21: 589-596.

Stadalnik R C, Vera D R. Nucl Med Biol, 2001, 28: 499-503.

Vera D R, Stadalnik R C, Krohn K A. J Nucl Med, 1985, 26: 1157-1167.

Vera D R, Hoh C K, Stadalnik R C, et al. Radiopharmaceuticals for the study of liver and renal function, San Diego, 2003, 795-822.

Zhang R J, Liang G L, Wan W X, et al. Nucl Tech, 2000, 23: 780-785.(in Chinese)

Zhang R J, Wan W X, Tao Y H, et al. Chin J Nucl Med, 2001, 21: 55-58.

Cai G M, Jiang M J, Zhou Y Y, et al. Pharmazie, 2011, 66: 761-765.

Zhou G L, Jiang M J, Zhang R J, et al. Nucl Tech, 2008, 31: 633-636.(in Chinese)

Becaud J, Karramkam M, Mu L, et al. J Label Compd Radiopharm, 2007, 50: S215.

Wuest F, Kohler L, Berndt M, et al. Amino Acids, 2009, 36: 283-295.

Vaidyanathan G, Zalusky M R. Nat Protoc, 2006, 1: 1655-1661.

Wester H J, Hamacher K, Stocklin G. Nucl Med Biol, 1996, 23: 365-372.

Wuest F, Hultsch C, Bergmann R, et al. Appl Radiat Isot, 2003, 59: 43-48.

Yang W J, Mou T T, Peng C, et al. Bioorg Med Chem, 2009, 17: 7510-7516.

Chen Z P, Liu C Y, Li X M, et al. Nucl Sci Tech, 2012, 23: 40-46.

Haka M S, Kilbourn M R, Watkins G L, et al. J Label Compnd Radiopharm, 1989, 27: 823-833.

Johnstrom P, Harris N G, Fryer T D, et al. Clin Sci, 2002, 103(Suppl 48): 4S.

Views

Downloads

CSCD

Alert me when the article has been cited

Submit

Tools

Publicity Resources

Preliminary evaluation of the radiotherapeutic efficacy of ¹³¹I-atorvastatin in rats with hepatocellular carcinoma

Preparation and biodistribution assessment of ⁶⁸Ga-DKFZ-PSMA-617 for PET prostate cancer imaging

Semi-automated synthesis, validation and microPET imaging of ¹⁸F-FP-DTBZ as a vesicular monoamine transporter ligand

Directly radiolabeled phage with spleen-targeting specificity

Nanographene oxide labeling with ¹⁸⁸Re

Related Author

No data

Related Institution

.O. BOX

Research Center for Nuclear Medicine, Shariati Hospital, Tehran University of Medical Sciences

Department of Chemistry, University of Zanjan

Nuclear Science and Technology Research Institute (NSTRI)

Beijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, College of Chemistry and Molecular Engineering, Peking University

Address：Editorial Office of NST, 2019 Jialuo Road, Jiading, Shanghai 201800, China Postal code：201800
Email：nst@sinap.ac.cn
Technical support is provided by Beijing Founder electronics co., LTD 沪ICP备05005479号-1 京公网安备11010802024621
It is recommended to read the content of this site in Chrome&IE9+. Please switch to extreme mode in browser 360.
Cookies We use cookies to help provide and enhance our service and tailor content. By continuing, you agree to the use of cookies.

⁰

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

DOI：10.13538/j.1001-8042/nst.2013.06.016

摘要

Abstract

关键词

Keywords

references

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