[18F]氟司必啶是一种用于脑部σ(1)受体PET成像临床研究的新型放射性示踪剂，其放射性合成及纯化程序的自动化。
Automation of the radiosynthesis and purification procedures for [18F]Fluspidine preparation, a new radiotracer for clinical investigations in PET imaging of σ(1) receptors in brain.
作者信息
Maisonial-Besset Aurélie, Funke Uta, Wenzel Barbara, Fischer Steffen, Holl Katharina, Wünsch Bernhard, Steinbach Jörg, Brust Peter
机构信息
Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research(1), Research Site Leipzig, Department of Neuroradiopharmaceuticals, Germany.
Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research(1), Research Site Leipzig, Department of Neuroradiopharmaceuticals, Germany.
出版信息
Appl Radiat Isot. 2014 Feb;84:1-7. doi: 10.1016/j.apradiso.2013.10.015. Epub 2013 Nov 5.
The radiosynthesis of [(18)F]Fluspidine, a potent σ1 receptor imaging probe for pre-clinical/clinical studies, was implemented on a TRACERlab(TM) FX F-N synthesizer. [(18)F]2 was synthesized in 15 min at 85 °C starting from its tosylate precursor. Purification via semi-preparative RP-HPLC was investigated using different columns and eluent compositions and was most successful on a polar RP phase with acetonitrile/water buffered with NH4OAc. After solid phase extraction, [(18)F]Fluspidine was formulated and produced within 59±4 min with an overall radiochemical yield of 37±8%, a radiochemical purity of 99.3±0.5% and high specific activity (176.6±52.0 GBq/µmol).
[(18)F]氟司必林是一种用于临床前/临床研究的强效σ1受体成像探针，其放射性合成是在TRACERlab(TM) FX F-N合成仪上进行的。[(18)F]2从其甲苯磺酸盐前体开始，在85°C下15分钟内合成。使用不同的色谱柱和洗脱液组成研究了通过半制备RP-HPLC进行的纯化，在以NH4OAc缓冲的乙腈/水的极性RP相上最为成功。经过固相萃取后，[(18)F]氟司必林在59±4分钟内配制完成，总放射化学产率为37±8%，放射化学纯度为99.3±0.5%，比活度高(176.6±52.0 GBq/µmol)。
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