Nuclear Techniques ›› 2019, Vol. 42 ›› Issue (8): 80303-080303.doi: 10.11889/j.0253-3219.2019.hjs.42.080303

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

Automated radiosynthesis and preliminary Micro-PET/CT imaging of [18F]AlF-NOTA-P-L-Lys6-GnRH

Baoyuan LI1,Kongzhen HU2(),Xiong LI1()   

  1. 1. The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou 510120, China
    2. PET Center, Department of Nuclear Medicine, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China
  • Received:2019-04-15 Revised:2019-05-08 Online:2019-08-10 Published:2019-08-26
  • Contact: Kongzhen HU,Xiong LI E-mail:58997018@qq.com;43293854@qq.com
  • About author:LI Baoyuan, male, born in 1981, graduated from Anhui Normal University in 2005, master student, focusing on the PET pharmaceuticals
  • Supported by:
    National Natural Science Foundation of China(81701729);Southern Medical University(2017J010)

Abstract:

[Backgroud] Gonadotropin releasing hormone (GnRH) receptor is overexpressed in many human tumors and is currently used as a target for molecular imaging.

Purpose

This study aims to design and synthesize a new 18F-labeled GnRH peptide by automatic radiosynthesis for preliminary Micro-PET/CT imaging.

Methods

[18F]AlF-NOTA-P-L-Lys6-GnRH was automated radiolabeled with 18F by using Al18F complex on the modified PET-MF-2V-IT-I synthesis module. The stability of [18F]AlF-NOTA-P-L-Lys6-GnRH was incubated in phosphate buffer saline (PBS) at 37 oC and the octanol/water partition coefficient was studied. The dynamic Micro-positron emission tomography (PET) study of [18F]AlF-NOTA-P-L-Lys6-GnRH in nude mice bearing PC-3 cancer was carried out.

Results

The total radiochemical synthesis and purification of [18F]AlF-NOTA-P-L-Lys6-GnRH was completed in 35 min with a decay-corrected yield of (25±6)% and a specific activity of 8~30 GBq?μmol-1 (n=6). The logP value of [18F]AlF-NOTA-P-L-Lys6-GnRH was -2.70±0.06 and the tracer was stable in phosphate-buffered saline for 2 h. Dynamic PET imaging analysis revealed that [18F]AlF-NOTA-P-L-Lys6-GnRH was clearly delineated in PC-3 xenografted tumor with high tumor-to-muscle ratios and excreted mainly through the kidneys.

Conclusion

[18F]AlF-NOTA-P-L-Lys6-GnRH was an efficient automated production of commercially available synthetic modules that could be used as a potential PET tracer for the imaging PC-3 prostate tumors.

Key words: [18F]AlF-NOTA-P-L-Lys6-GnRH, GnRH, Automated radiosynthesis, Micro-PET/CT

CLC Number: 

  • TL92+3