O-(2-[^(18)F]氟代乙基)-5-羟基-L-色氨酸的合成、生物分布及MicroPET显像

Synthesis,Biodistribution and MicroPET Imaging of O-(2-[^(18)F]fluoroethyl)-5-hydroxy-L-try-ptophan

通过对现有CTI公司计算机控制的化学合成模块(CPCU)进行改造,合成了L-5-羟基色氨酸类似物(5-18FEHTP),并用高效液相(HPLC)检测其放化纯度,所得产品用于昆明小鼠的S180肉瘤模型显像。结果显示,采用改进方法合成5-18FEHTP的总时间是45 min,放化收率为12%～16%(n=15),产品的放化纯度>98%。正常昆明小鼠体内生物分布显示,其脑组织摄取较低,最大摄取率为(2.354±0.405)%ID/g。血液清除较快,30 min时摄取率已降为(2.974±0.278)%ID/g。肾脏给药60 min摄取率值最大为(11.706±0.374)%ID/g,5-18FEHTP经过肾脏排出体外。MicroPET小鼠显像结果表明,5-18FEHTP在S180肉瘤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5-18FEHTP,方法简便、稳定,产品纯度较高。小鼠生物分布和显像结果表明,5-18FEHTP可能成为一种新的PET显像剂。

O-（2-[^18F] fluoroethyl）-5-hydroxy-L-try-ptophanl （5-^18 FEHTP） was synthesized by using a modified chemistry process control unit（CPCU）. Radiochemical purity was over 98% measured by High Performance Liquid Chromatograph（HPLC）. After injecting of 5-^18 FEHTP through tail vein, the mice was scanned with MicroPET. The no decay corrected radiochemical yield of 5-^18 FEHTP was 12 %-16 % （n = 15） within 45 min total reaction time, and the manually purified time was about 20 min. 5-18FEHTP can be conveniently synthesized with modified CPCU and the labeling yield was stable, the number value of biodistribution in the Kunming mice showed that the uptake of 5-^18FEHTP in the brains was low, and the cleanup from blood was very fast, and 5-^18FEHTP was eliminated through kidneys.The results of Micro PET imaging indicated that 5-^18 FEHTP may be a new promising PET tracer.