Synthesis and imaging study of [18F]FPTZFA

ZHOU Daming; ZHU Jianhua

doi:10.11889/j.0253-3219.2015.hjs.38.020301

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Synthesis and imaging study of [18F]FPTZFA

更新时间：2021-03-03

- Synthesis and imaging study of [18F]FPTZFA
- NUCLEAR TECHNIQUES Vol. 38, Issue 2, Article number: 020301(2015)
- 作者机构：
  
  复旦大学药学院放射药学教研室,上海,201203
- 作者简介：
- 基金信息：
- DOI：10.11889/j.0253-3219.2015.hjs.38.020301
  CLC：
- Published：02 February 2015
- 稿件说明：
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ZHOU Daming, ZHU Jianhua. Synthesis and imaging study of [18F]FPTZFA[J]. Nuclear techniques, 2015, 38(2): 020301
DOI：

ZHOU Daming, ZHU Jianhua. Synthesis and imaging study of [18F]FPTZFA[J]. Nuclear techniques, 2015, 38(2): 020301 DOI： 10.11889/j.0253-3219.2015.hjs.38.020301.

摘要

为研究正电子核素18F标记的叶酸衍生物([18F]FPTZFA)的合成及其在小鼠体内的生物学分布，以叶酸为起始原料，通过叶酸上羧基与2-叠氮基乙胺上氨基的成酯反应，将叠氮基团标记至叶酸，得到γ-叶酸-2-叠氮基乙酰胺(FA-N3)；同时以硝基羟基吡啶为原料，经过三步取代反应，将炔基、F连接至吡啶环上得到2-氟-3-(戊-4-炔基氧)吡啶(19F-PyKYNE)。19F-PyKYNE在K18F/K222作用下生成18F-PyKYNE。18F-PyKYNE的炔基与FA-N3的叠氮基团，在硫酸铜、抗坏血酸钠催化下发生点击化学反应，得到最终产物[18F]FPTZFA。整个放射性标记过程仅需40 min，[18F]FPTZFA放化纯度达51%，放化产率达37%。[18F]FPTZFA经放射性半制备高效液相色谱(High Performance Liquid Chromatography

HPLC)分离纯化后，观察其在不同时间段荷瘤小鼠体内的组织分布。荷瘤小鼠脏器及组织切片后的放射自显影显示[18F]FPTZFA的摄取集中在肝、肾和肿瘤组织。其中30 min肿瘤组织、肌肉的单位质量组织的放射性占注射剂量放射性的百分比(%ID/g)比值为3.6，肿瘤、血液的%ID/g比值为3.2。初步断定[18F]FPTZFA有较好的肿瘤靶向性。

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. Abstract

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