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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。
Through the modification of CUT’s computer controlled chemical synthesis module (CPCU), neuronal nicotinic acetylcholine receptor (nAChRs) imaging agent 2-18F-A-85380 was synthesized and detected by high performance liquid chromatography (HPLC) Its radiochemical purity and specific activity, the resulting product for the normal rat head MicroPET imaging. The results showed that the total time for the synthesis of 2-18F-A-85380 by the improved method was 45 min, the radiochemical yield was 50% ± 5% (n = 6), the radiochemical purity of the product was> 99% 0.35 ± 0.02 PBq / g. The results of MicroPET imaging showed that the concentration of 2-18F-A-85380 in the thalamus rich in α4β2 subtype nAChRs receptors was significantly higher than that in other tissues. The above results suggest that the method of semi-automatic synthesis of 2-18F-A-85380 by CPCU is simple and stable, and the specific activity of the product is high. Animal experiments show that 2-18F-A-85380 has basically met the requirements of clinical imaging agents.