【摘要】 为了研究正电子核素18F标记的葡萄糖转运蛋白显像剂6-18氟-6-脱氧葡萄糖的制备及在小鼠体内的生物学分布,以D-葡萄糖为起始原料,经过丙酮和苯甲醛对1,2,3,5位羟基的定位保护,然后用对甲苯磺酰氯和6位的羟基反应得到能被18F-进攻的离去基团,最后用18F-离子通过亲核取代反应实现对葡萄糖6位的氟代标记;反应中间体用NMR和MS表征,最终产物用标准品6-19FDG在HPLC下对照确认,测定放化纯度,观察其在小鼠体内的生物学分布.6-18氟-6-脱氧葡萄糖的放射性标记过程需35min(从加速器轰击结束算起),放化产率70%±5%(校正后,n=5),放化纯度>95%.小鼠体内的生物学分布表明,各个器官在1.0min达到峰值,然后逐渐平衡.初步研究结果表明,6-18FDG是一种很有价值的葡萄糖转运蛋白显像剂,为以后的体内外研究及活体显像奠定了基础.更多还原

【Abstract】 For the development glucose transport imaging,a radioactive glucose analogue was synthesized and evaluated.A glucose analogue,6-[18F]fluoro-6-deoxy-D-glucose(6-18FDG),was prepared in two steps with one-pot synthesis from [18F]fluoride and tosyl-precursor.Starting with D-glucose,the D-glucose was reacted with acetone and benzaldehyde to protect hydoxy,then reacted with p-toluenesulfonyl choride(TsCl)to get the tosyl-precursor.All the intermediates were identified with NMR and MS.The total radiosysthesis spent 35 min and with 70%±5%(EOB,decay corrected,n =5),with the radiochemical purity>95%.Biodistribution of 6-18FDG was performed in mice:18F activities in brain,liver,and heart reach the peak in 1.0 min after the injection,so reached a constant level.These results support that 6-18FDG is promising as valid tracer of glucose transport.更多还原