2-^(18)F-A-85380的制备与MicroPET显像  

Synthesis and MicroPET Imaging of 2-^(18)F-A-85380

作　　者：张赟[1] 吴战宏[1] 李方[1] 朱立[1] Dollé F Kühnast B 

机构地区：[1]中国医学科学院中国协和医科大学北京协和医院核医学科,北京100730 [2]法国原子能委员会约里欧居里医院生物医学研究所

出　　处：《同位素》2008年第1期15-19,共5页Journal of Isotopes

摘　　要：通过对现有CTI公司计算机控制化学合成模块(CPCU)进行改造,合成了神经型烟碱乙酰胆碱受体(nAChRs)显像剂2-18F-A-85380,并用高效液相色谱(HPLC)检测了其放化纯度及比活度,所得的产品用于正常大鼠头部MicroPET显像。结果显示,采用改进方法合成2-18F-A-85380的总时间为45 min,放化收率为50%±5%(n=6),产品的放化纯度>99%,比活度为0.35±0.02 PBq/g。MicroPET显像结果表明,2-18F-A-85380在富含α4β2亚型nAChRs受体的丘脑中浓集程度明显高于周围其它组织。以上结果提示,利用CPCU半自动合成2-18F-A-85380,方法简便、稳定,产品的比活度较高;动物实验结果表明2-18F-A-85380已基本满足临床显像剂的要求。2-^18 F-A-85380 was synthesized by a modified chemistry process control unit （CPCU）. Radiochemical purity and specific radioactivity were measured by High Performance Liquid Chromatograph （HPLC）. After tail Vein injection of 2-^18F-A-85380, the rats were scanned with MicroPET. The decay-corrected radiochemical yield of 2-^18 F-A-85380 was 50%±5% （n=6） within 45 min total reaction time. The radiochemical purity was a- round 99% determined by the analytical HPLC. The specific radioactivity was 0. 35±0.02 PBq/g. 2-^18F-A-85380 was successful in visualizing thalamus, which is rich of Nicotinic acetylcholine receptor （nAChRs） compared with other tissues. 2-^18F-A-85380 can be conveniently synthesized with modified CPCU and the labeling yield was stable, the results of MicroPET imaging indicated that 2-^18F-A-85380 could be suitable for clinical translation.

关 键 词：2-^18F-A-85380 MICROPET 烟碱乙酰胆碱受体 

分 类 号：TQ463[化学工程—制药化工] R817[医药卫生—影像医学与核医学]