三种碳-11标记的苯乙胺衍生物的合成与生物分布研究  

Synthesis and Bio-distribution of Three Carbon-11-Labeled Phenylethylamine Derivatives

作　　者：何玉林[1,2] 张晓军[1] 刘健[1] 付华平[1] 李云刚[1] 张锦明[1] 

机构地区：[1]解放军总医院核医学科,北京100853 [2]内蒙古医科大学附属医院核医学科,呼和浩特010050

出　　处：《同位素》2017年第1期9-15,共7页Journal of Isotopes

基　　金：国家自然科学基金(81660295);内蒙古自治区自然科学基金(2016MS(LH)0812)

摘　　要：通过氨基甲基化的方法用碳-11甲基标记了N-甲基苯乙胺、N-甲基间羟基苯乙胺和N-甲基酪胺三种化合物,评价了放射性核素标记的三种化合物在昆明小鼠体内的生物分布特征。合成结果显示,[11 C]-N-甲基苯乙胺合成包括HPLC分离总耗时约30min,放化产率为25%、放化纯度>98%,[11 C]-N-甲基间羟基苯乙胺合成包括HPLC分离总耗时约25min,放化产率为13%、放化纯度>97%,[11 C]-N-甲基酪胺合成包括HPLC分离总耗时约25min,放化产率为28%、放化纯度>98%;小鼠体内生物分布结果显示:三个标记物在各测定时间点小鼠靶器官心肌的摄取均比肺、肝、脾、肾等非靶器官的摄取低,心肌摄取与肌肉摄取相近。注射后10min时[11 C]-N-甲基苯乙胺的心与肺放射性摄取比为1/2.08、心与肝为1/2.94,[11 C]-N-甲基间羟基苯乙胺的心与肺放射性摄取比为1/2.56、心与肝为1/2.76,[11 C]-N-甲基酪胺的心与肺放射性摄取比为1/1.85、心与肝为1/5。以上结果提示,碳-11甲基标记N-甲基苯乙胺、N-甲基间羟基苯乙胺和N-甲基酪胺的合成方法虽然简单,但是心肌靶向性差,不适用于核素心肌显像。N-methylphenylethylamine,N-m-MeTyramine and N-P-MeTyramine were labeled with Carbon-11 by methylation of amino group.Biological distribution characteristics of the three radiolabeled compounds in Kunming mice were evaluated.Synthesis of [11C]-N-methylphenethylamine requires 30 minutes including HPLC separationtime.The yield was 25%and the radiochemical purity was more than 98%.Synthesis of[11C]m-MeTyramine required 25 minutes including HPLC separation time.The yield was 13% and the radiochemical purity was more than 97%.Synthesis of [11C]PMeTyramine required 25 minutes including HPLC separation time.The yield was 28%and the radiochemical purity was more than 98%.Distribution study showed that amount of the three marker uptaken by the target organism-myocardium,at each time point was smaller than that uptaken by non-target organs like lung,liver,spleen,kidney.Myocardial uptake was similar with that of muscle.After injection of the markers for 10 minutes,concentration of[11C]-N-methylphenethylamine in lung and liver was2.08 and 2.94 times higher than that in heart,respectively.Concentration of[11C]mMeTyramine in lung and liver was 2.56,2.76 higher than that in heart,respectively.Concentration of[11C]P-MeTyramine in lung and liver was 1.85 and 5higher than that in heart,respectively.Present results suggested that although synthetic methods of 11 C labeled N-methylphenylethylamine,N-m-MeTyramine and N-P-MeTyramine were simple,but the targeting in myocardium were poor and might not be suitable for myocardial perfusion imaging.

关 键 词：儿茶酚胺 苯乙胺 碳-11标记 心肌摄取 正电子显像剂 

分 类 号：TL923[核科学技术—核燃料循环与材料] R817.93[医药卫生—影像医学与核医学]