^(11)C-间羟基麻黄碱的自动化合成及心肌显像研究  

Automatic synthesis and myocardial imaging of 11C-meta-hydroxyephedrine

作　　者：何玉林[1] 张国建[1] 白侠[1] 周伟娜[1] 王文睿[1] 王相成[1] He Yulin;Zhang Guojian;Bai Xia;Zhou Weina;Wang Wenrui;Wang Xiangcheng(Department of Nuclear Medicine of the Affiliated Hospital of Inner Mongolia Medical University,Key Laboratory of Molecular Imaging of Inner Mongolia Autonomous Region,Hohhot 010050,China)

机构地区：[1]内蒙古医科大学附属医院核医学科、内蒙古自治区分子影像学重点实验室,呼和浩特010050

出　　处：《中华核医学与分子影像杂志》2022年第11期672-675,共4页Chinese Journal of Nuclear Medicine and Molecular Imaging

基　　金：国家自然科学基金(82060323,81960318,81960319)。

摘　　要：目的实现11C-间羟基麻黄碱(mHED)的全自动化合成,并对其进行显像研究。方法采用11C-三氟甲基磺酰基甲烷(11CH3-triflate)法制备11C-mHED,粗产品经半制备高效液相色谱(HPLC)纯化得到终产物,采用放射性HPLC测定其放化纯和比活度;取5只正常SD大鼠行microPET/CT显像确定其心肌摄取和排泄过程;行心肌梗死患者(男,42岁)PET/CT显像评价其临床显像价值。结果通过商用合成器实现了11C-mHED的自动化合成,总合成时间约30 min,放化产率为(15±2)%(非衰减校正,n=10),放化纯>98%,比活度约为65 GBq/mmol;正常SD大鼠的microPET/CT显像示注射显像剂后10 min心肌摄取最高,后逐渐从心肌排泄并经过肝胆排出;心肌梗死患者PET/CT显像可见左心室下壁近心尖部显像剂缺损,与超声和心电图检查结果相匹配。结论成功自动化制备11C-mHED,产物放化产率和比活度较高,可高度浓聚于心肌,心肌梗死患者显像效果良好。Objective To realize a fully automated synthesis of 11C-meta-hydroxyephedrine(mHED)and to perform imaging studies with it.Methods 11C-mHED was prepared by the 11CH3-triflate method.The crude product was purified by semi-preparative high performance liquid chromatograph(HPLC)to obtain the final product.The radiochemical purity and specific activity were determined by radio-HPLC.The myocardial uptake and excretion process of the agent were monitored by microPET/CT imaging on 5 normal SD rats.The clinical imaging value was evaluated using PET/CT imaging in a patient(male,42 years old)with myocardial infarction.Results The automated synthesis of 11C-mHED was realized by a commercial synthesizer.The total synthesis time was about 30 min.The radiochemical yield was(15±2)%(non-decay corrected,n=10)and the radiochemical purity was greater than 98%.The specific activity was about 65 GBq/mmol.MicroPET/CT imaging in normal SD rats showed the myocardial uptake was highest at 10 min after the injection of imaging agent,and then the imaging agent was gradually excreted from the myocardium through the liver and gallbladder.PET/CT imaging of a patient with myocardial infarction showed an imaging agent defect near the apex in the inferior wall of the left ventricle,which was matched with results of ultrasound and electrocardiogram examination.Conclusions 11C-mHED can be successfully prepared automatically,with high radiochemical yield and specific activity.It can also highly concentrate in the myocardium,and the imaging effect with this agent is good in a patient with myocardial infarction.

关 键 词：麻黄碱 同位素标记 碳放射性同位素 正电子发射断层显像术 体层摄影术 X线计算机 心肌 大鼠 

分 类 号：R817.4[医药卫生—影像医学与核医学]