同位素 ›› 2017, Vol. 30 ›› Issue (3): 204-208.DOI: 10.7538/tws.2017.youxian.003

• 放射性药物与标记化合物 • 上一篇    下一篇

腺苷A2A受体显像剂11C-KW6002的合成与初步生物学评价

闫赋琴;周卫华;孙小萌;刘晓军   

  1. 中国武警总医院,北京100039
  • 出版日期:2017-08-20 发布日期:2017-08-10

The Synthesis and Evaluation of 11C-KW6002 as the PET Adenosine 2A Receptor Imaging Agent

YAN Fu-qin;ZHOU Wei-hua;SUN Xiao-meng;LIU Xiao-jun   

  1. General Hospital of Chinese People’s Armed Police Forces, Beijing 100039, China
  • Online:2017-08-20 Published:2017-08-10

摘要:

腺苷A2A受体与中枢神经退行性疾病密切相关,正电子核素标记的腺苷A2A受体显像剂可用于帕金森病(PD)的诊断与疗效评价。本研究采用碳-11标记[(E)-1,3-二乙基-8-(3,4-二甲氧基苯乙烯)-7-甲基-3,7-双氢-1H-嘌呤-2,6-二酮](KW6002)制备11C-KW6002,并进行正常鼠与PD模型鼠microPET显像。结果显示,以去甲基KW6002为标记前体,在NaOH条件下与三氟甲基磺酰基碳-11甲烷(11CH3-Trifcate)反应,标记率达56%(衰变校正,n=3)。经制备HPLC分离和固相萃取,产品放化纯度>99.5%,比活度为1.5×1014 Bq/g。11C-KW6002的microPET显像结果显示,正常大鼠双侧纹状体呈对称显像,PD模型鼠中毁损侧纹状体放射性较对侧明显增加,而同一模型的11C-CFT显像为毁损侧纹状体放射性缺失。表明11C-KW6002为具有临床应用的潜在腺苷A2A受体显像剂。

关键词: 腺苷A2A受体, 11C-KW6002, 合成, microPET, 显像剂

Abstract:

PET with selective adenosine 2A receptor (A2A) radiotracers can be used to study a neurodegenerative disorders in vivo and to diagnose of PD. The PET radiotracer 11C-KW6002 for imaging A2A was synthesized and evaluated, in normal and PD module rats. The results showed that the labeling yield was 56% (decay corrected yield, n=3) when 11CH3-Triflate reacted with nor-KW6002 under NaOH. The radiochemical purity of product was 99.5% with specific activity of 1.5×1014 Bq/g. The balance of radioactivity in striatum was observed in normal rats with microPET. A significant raised radioactivity on the striatum of lesion compared with the normal side. The radioactivity was found absence on the striatum of lesion with 11C-CFT. 11C-KW6002 is a potential PET radiotracer for imaging A2A.

Key words: A2A receptors, 11C-KW6002, synthesis, microPET, imaging agent