CAJ | 학술논문

为了研究正电子核素~(18)F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~(18)F-进攻的离去基团,最后用~(18)F-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-~(19)FDG在HFLC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35 min(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1.0 min达到峰值,然后逐渐平衡.初步研究结果表明,6-~(18)FDG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.
위료연구정전자핵소~(18)F표기적포도당전운단백현상제6-~(18)불-6-탈양포도당적제비급재소서체내적생물학분포,이D-포도당위기시원료,경과병동화분갑철대1,2,3,5위간기적정위보호,연후용대갑분광선록화6위적간기반응득도능피~(18)F-진공적리거기단,최후용~(18)F-리자통과친핵취대반응실현대포도당6위적불대표기;반응중간체용NMR화MS표정,최종산물용표준품6-~(19)FDG재HFLC하대조학인,측정방화순도,관찰기재소서체내적생물학분포.6-~(18)불-6-탈양포도당적방사성표기과정수35 min(종가속기굉격결속산기),방화산솔70%±5%(교정후,n=5),방화순도>95%.소서체내적생물학분포표명,각개기관재1.0 min체도봉치,연후축점평형.초보연구결과표명,6-~(18)FDG시일충흔유개치적포도당전운단백현상제,위이후적체내외연구급활체현상전정료기출.
For the development glucose transport imaging, a radioactive glucose analogue was synthesized and evaluated. A glucose analogue, 6- [~(18) F] fluoro-6-deoxy-D-glucose (6-~(18) FDG), was prepared in two steps with one-pot synthesis from [~(18)SF]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-~(18)FDG was performed in mice: ~(18)F 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-~(18) FDG is promising as valid tracer of glucose transport.