Nuclear Techniques ›› 2015, Vol. 38 ›› Issue (2): 20301-020301.doi: 10.11889/j.0253-3219.2015.hjs.38.020301

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

Synthesis and imaging study of [18F]FPTZFA

ZHOU Daming ZHU Jianhua   

  1. (Department of Radiopharmacy, School of Pharmacy, Fudan University, Shanghai 201203, China)
  • Received:2014-10-11 Revised:2014-10-31 Online:2015-02-10 Published:2015-02-02

Abstract: Background: Folate receptor is highly expressed in tumor cells. Labeling folic acid offers a way of tumor targeting. Purpose: This study aims to explore the synthesis and in vivo imaging of 18F labeled folic derivative [18F]FPTZFA. Method: Starting from folic acid, through the amino and carboxyl ester forming reaction, we get FA-N3, and then FA-N3 is labeled with 18F-Pykyne in the presence of CuSO4, VcNa to get the compound of [18F]FPTZFA. [18F]FPTZFA then characterized by Radio-HPLC (High Performance Liquid Chromatography) and separated by Semi-HPLC. In vivo imaging was carried out in KB tumor-bearing nude mice after intravenous injection of [18F]FPTZFA via tail vein and biodistribution of [18F]FPTZFA was performed in these mice. Results: The overall reaction time lasts for 40 min, with radiochemical purity of 51%, and radiochemical yield of 37%. The autoradiography of mice tissues showed [18F]FPTZFA concentrated in liver, kidney and tumor. The %ID/g ratio in tumor tissue and muscle is 3.6, %ID/g ratio in tumor tissue and blood is 3.2. Conclusion: The high efficiency and high yield make the synthesis of [18F]FPTZFA more convenient and the %ID/g ratio indicates [18F]FPTZFA as a promising tumor targeting tracer.

Key words: 18F, Folic acid, Click chemistry