Synthesis and fluoro-radiolabelling of serotonin(5-HT<sub>1A</sub>) receptor imaging agent <sup>18</sup>F-MPPF

WU Chunying1; 2   LIN Xiangtong1   LU Chunxiong2   ZHANG Zhengwei1    LIU Ping1    XUE Fangping1  1

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Synthesis and fluoro-radiolabelling of serotonin(5-HT_1A) receptor imaging agent ¹⁸F-MPPF

更新时间：2021-03-12

- Synthesis and fluoro-radiolabelling of serotonin(5-HT_1A) receptor imaging agent ¹⁸F-MPPF
- NUCLEAR TECHNIQUES Issue 5, (2003)
- 作者机构：
  
  1. 复旦大学华山医院核医学科PET中心
  2. 江苏省原子医学研究所核医学国家重点实验室
  3. 复旦大学华山医院核医学科PET中心,上海,200040
  4. 江苏省原子医学研究所核医学国家重点实验室无锡,214063
  5. ,上海,200040
- 作者简介：
- 基金信息：
  
  江苏省135医学重点人才基金(RC2002068);江苏省六大人才高峰基金(2003-07)资助
- DOI：
  CLC： R817.9
- Published：01 May 2003
- 稿件说明：
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[1]吴春英,林祥通,陆春雄,张政伟,刘平,薛方平.5-羟色胺受体显像剂~(18)F-MPPF的合成和标记[J].核技术,2003(05):371-374.

WU Chunying1, 2 LIN Xiangtong1 LU Chunxiong2 ZHANG Zhengwei1 LIU Ping1 XUE Fangping1 1. Synthesis and fluoro-radiolabelling of serotonin(5-HT_1A) receptor imaging agent ¹⁸F-MPPF[J]. Nuclear techniques, 2003, (5): 371-374.
[1]吴春英,林祥通,陆春雄,张政伟,刘平,薛方平.5-羟色胺受体显像剂~(18)F-MPPF的合成和标记[J].核技术,2003(05):371-374. DOI：

WU Chunying1, 2 LIN Xiangtong1 LU Chunxiong2 ZHANG Zhengwei1 LIU Ping1 XUE Fangping1 1. Synthesis and fluoro-radiolabelling of serotonin(5-HT_1A) receptor imaging agent ¹⁸F-MPPF[J]. Nuclear techniques, 2003, (5): 371-374. DOI：

摘要

报道了5-羟色胺（5-HT1A）受体显像剂4-[18F]氟-N-[2-[1-（2-甲氧基苯基）-1-哌嗪基乙基]-N-2吡啶基-苯甲酰胺（18F-fluoro-N-[2-[1-（2-methoxyphenyl）]-1-piperazinyl]ethyl-N-2-pridinyl-benzamide

18F-MPPF）的合成和标记。标记前体MPPNO2和各步合成中间体均由红外、元素分析、核磁共振和质谱确证;采用两种加热方法进行氟代亲核置换标记反应。结果显示

微波法标记的放化产额（34%—50%

n=10）明显比油浴加热标记法（8%—24%

n=10）高

反应时间（40—50min）也比油浴加热标记法（70—90min）短

用TLC和HPLC检测放射化学纯度（RCP）均大于95%

可用于临床前研究。

Abstract

The synthesis and fluoro-radiolabelling of serotonin(5-HT1A) receptor imaging agent 4-18F-fluoro-N-[2-[1-(2-methoxyphenyl)-1-piperazinyl]ethyl-N-2-pridinyl-benzamide

18F-MPPF) was reported . The chemical structure of the nitro- labellng precusor MPPNO2 and all its intermediates were verified by IR

elementary analysis

1HNMR and MS. Nucleophilic substitution of fluororeplacement reaction was proceeded by oil-bath heating or microwave heating methed. Radiochemical yield by microwave heating was higher than oil-bath heating

whereas synthetic time of the former was much more shorter than the latter. Final radiochemical purity was above 95% deter-mined by TLC . Thereby it can be used preclinically.

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Synthesis and fluoro-radiolabelling of serotonin(5-HT1A) receptor imaging agent 18F-MPPF

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摘要

Abstract

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references

Synthesis and fluoro-radiolabelling of serotonin(5-HT_1A) receptor imaging agent ¹⁸F-MPPF