Pijarowska-Kruszyna Justyna, Jaron Antoni, Kachniarz Artur, Malkowski Bogdan, Garnuszek Piotr, Mikolajczak Renata
National Centre for Nuclear Research, Radioisotope Centre POLATOM, Andrzeja Soltana 7, Otwock, 05-400, Poland.
Department of Nuclear Medicine, Oncology Centre Prof. Lukaszczyk Memorial Hospital, Bydgoszcz, Poland.
J Labelled Comp Radiopharm. 2016 Mar;59(3):82-6. doi: 10.1002/jlcr.3375. Epub 2016 Feb 8.
The use of [(18)F]labelled nortropane derivative 2β-carbomethoxy-3β-(4-chlorophenyl)-8-(2-fluoroethyl)-nortropane (FECNT) as a dopamine transporter ligand for PET imaging is dependent on efficient radiosynthesis method. Herein, the automated synthesis of [(18)F]FECNT from its chlorinated precursor in commercially available SynChrom [(18)F] R&D module has been developed. The synthesis unit was readily configured for the one-step synthesis from corresponding chlorinated precursor. The radiolabeling process involved a classical [(18)F]fluoride nucleophilic substitution performed at 110 °C for 12 min and finally HPLC and SPE purification. Crude [(18)F]FECNT was obtained with a radiolabeling yield of 59 ± 12% (n = 5). The average uncorrected amount of [(18)F]FECNT in the final formulated dose was 2.0 ± 0.5 GBq (32 ± 7% overall decay-corrected yields) obtained with radiochemical purity over 99% and specific activity of 55 GBq/µmol. The total duration of the procedure was 80-90 min. An automated radiosynthesis of [(18)F]FECNT with high radiochemical purity may provide a simple and robust method of radiopharmaceutical preparation for routine clinical applications.
将[(18)F]标记的降托烷衍生物2β-甲氧基羰基-3β-(4-氯苯基)-8-(2-氟乙基)-降托烷(FECNT)用作正电子发射断层显像(PET)成像的多巴胺转运体配体，取决于高效的放射性合成方法。本文报道了在市售的SynChrom [(18)F]研发模块中，由其氯化前体自动合成[(18)F]FECNT的方法。合成单元易于配置为从相应的氯化前体进行一步合成。放射性标记过程包括在110℃下进行12分钟的经典[(18)F]氟化物亲核取代反应，最后通过高效液相色谱(HPLC)和固相萃取(SPE)进行纯化。粗品[(18)F]FECNT的放射性标记产率为59±12%(n = 5)。最终制剂剂量中[(18)F]FECNT的平均未校正量为2.0±0.5 GBq(总体衰变校正产率为32±7%)，放射化学纯度超过99%，比活度为55 GBq/µmol。该过程的总时长为80 - 90分钟。具有高放射化学纯度的[(18)F]FECNT的自动放射性合成可为常规临床应用提供一种简单且可靠的放射性药物制备方法。
