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5-羟色胺受体显像剂^(18)F-MPPF的合成和标记 被引量：3

Synthesis and fluoro-radiolabelling of serotonin(5-HT_(1A)) receptor imaging agent ^(18)F-MPPF
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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。 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.
作者 吴春英 林祥通 陆春雄 张政伟 刘平 薛方平
机构地区 复旦大学华山医院核医学科PET中心 江苏省原子医学研究所核医学国家重点实验室
出处 《核技术》 CAS CSCD 北大核心 2003年第5期371-374,共4页 Nuclear Techniques
基金 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
关键词 5-羟色胺受体 ^18F标记 ^18F-MPPF 合成 Serotonin (5-HT1A) receptor, 18F labeling , 18F-MPPF, Synthesis.
分类号 O628.5 [理学—有机化学] R817.9 [医药卫生—影像医学与核医学]
  • 相关文献

参考文献7

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共引文献11

同被引文献11

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核技术
2003年 第5期

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