Preparation of dopamine D2 receptor imaging agent <sup>18</sup>F-Fallypride and biodistribution study in mice

YANG Min PAN Donghui XU Yuping WANG Songpei TANG Jie LIU Chunyi LUO Shineng

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Preparation of dopamine D2 receptor imaging agent ¹⁸F-Fallypride and biodistribution study in mice

更新时间：2021-03-12

- Preparation of dopamine D2 receptor imaging agent ¹⁸F-Fallypride and biodistribution study in mice
- NUCLEAR TECHNIQUES Issue 5, (2008)
- 作者机构：
  
  1. 江苏省原子医学研究所卫生部核医学重点实验室
  2. 江苏省原子医学研究所卫生部核医学重点实验室,无锡,214063
- 作者简介：
- 基金信息：
  
  江苏省医学重点人才项目(RC2007096);江苏省高技术研究计划(BG2006604);江苏省“六大人才高峰”资助;江苏省卫生厅(200334)资助
- DOI：
  CLC： R817
- Published：01 May 2008
- 稿件说明：
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[1]杨敏,潘栋辉,徐宇平,王颂佩,唐婕,刘春仪,罗世能.苯甲酰胺类多巴胺D2受体显像剂~(18)F-Fallypride的制备和生物分布[J].核技术,2008(05):360-363.

YANG Min PAN Donghui XU Yuping WANG Songpei TANG Jie LIU Chunyi LUO Shineng. Preparation of dopamine D2 receptor imaging agent ¹⁸F-Fallypride and biodistribution study in mice[J]. Nuclear techniques, 2008, (5): 360-363.
[1]杨敏,潘栋辉,徐宇平,王颂佩,唐婕,刘春仪,罗世能.苯甲酰胺类多巴胺D2受体显像剂~(18)F-Fallypride的制备和生物分布[J].核技术,2008(05):360-363. DOI：

YANG Min PAN Donghui XU Yuping WANG Songpei TANG Jie LIU Chunyi LUO Shineng. Preparation of dopamine D2 receptor imaging agent ¹⁸F-Fallypride and biodistribution study in mice[J]. Nuclear techniques, 2008, (5): 360-363. DOI：

摘要

以（s）-（-）-N-（1-烯丙基吡咯烷-2-氨基甲基）-5-（3-磺酰基）-2

3-二甲氧基苯甲酰胺为氟标记前体

用K222催化进行氟标记

合成了（s）-（-）-N-（1-烯丙基吡咯烷-2-氨基甲基）-5-（3-18F）-2

3-二甲氧基苯甲酰胺（18F-Fallypride）。考察标记物的放化纯度及稳定性

并进行ICR小鼠体内分布特性研究。结果显示

18F-Fallypride的放化产率为40.75%

合成时间40 min

放化纯度大于97%

标记物的生理盐水溶液室温放置4 h

放化纯大于95%。小鼠静脉注射18F-Fallypride后120 min

纹状体/小脑高达14.27。18F-Fallypride进入血液后很快被组织摄取

其中以肾的早期摄取最高（9.91±1.24）%ID.g-1

各脏器的清除均较快（T1/2<1 h）

骨的摄取率随时间的延长而增加。

Abstract

In this paper

we report preparation and biodistribution in mice of 18F-Fallypride

a dopamine D2 receptor PET imaging agent.18F-Fallypride was prepared by nucleophilic fluorination of(s)-N-[(1-allyl-2-pyrrolidinyl)methyl]-5-(3-tolunesulfonyloxypropyl)-2

3-dimethoxybenzamide with K18F/K222(Kryptofix) in a chemical process control unit.Purity and stability of the 18F-Fallypride were checked by HPLC and TLC

the dynamic distribution in brain and critical organs of ICR mice were studied.The radiolabelling yield of 18F-Fallypride was 40.75% and the radiochemistry purity was over 97%.The whole process(including synthesis

purification and analysis) took only 40 minutes.After 4 hours in room temperature

the radiochemical purity of 18F-Fallypride was still over 95%.The striatum uptake was good

the striatum/cerebellum ratio reached 14.27 at 120 min.Among the critical organs

kidney had the first and the highest uptake(9.91±1.24 %ID.g-1).All organs had quick clearance(T1/2<1 h).The radioactivity in bone increased with time.The results show that 18F-Fallypride has a high striatum uptake and a high striatum/ cerebellum ratio.18F-Fallypride is a good dopamine D2 receptor agent.The autosynthesis method of 18F-Fallypride is simple and fast with high labeling yield and high radiochemical purity.This method is fit for clinic use.

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Preparation of dopamine D2 receptor imaging agent 18F-Fallypride and biodistribution study in mice

DOI：

摘要

Abstract

关键词

Keywords

references

Preparation of dopamine D2 receptor imaging agent ¹⁸F-Fallypride and biodistribution study in mice