Lu Shuiyu, Giamis Anthony M, Pike Victor W
Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, 10 Center Drive, Room B3 C346, Bethesda MD 20892-1003, USA.
Curr Radiopharm. 2009;2(1):nihpa81093. doi: 10.2174/1874471010902010049.
A commercial coiled-tube micro-reactor (NanoTek; Advion) was used as a convenient platform for the synthesis of [(18)F]fallypride in small doses (0.5-1.5 mCi) for micro-PET studies of brain dopamine subtype-2 receptors in rodents. Each radiosynthesis used low amounts (20-40 mug; 39-77 nmol) of tosylate precursor and [(18)F]fluoride ion (0.5-2.5 mCi). Optimization of the labeling reaction in the apparatus, with respect to the effects of precursor amount, reaction temperature, flow rate and [(18)F]fluoride ion to precursor ratio, was achieved rapidly and the decay-corrected radiochemical yield of [(18)F]fallypride (up to 88%) was reproducible. The low amounts of material used in each radiosynthesis allowed crude [(18)F]fallypride to be purified rapidly on an analytical-size reverse phase HPLC column, preceding formulation for intravenous injection. Scale-up of the reaction was easily achieved by continuously infusing reagent precursor solutions to obtain [(18)F]fallypride in much greater quantity.
一种商用盘管式微反应器（NanoTek；Advion）被用作一个便捷平台，用于小剂量（0.5 - 1.5毫居里）合成[(18)F]法利帕德，以用于对啮齿动物脑多巴胺2型受体进行微型正电子发射断层扫描（micro - PET）研究。每次放射性合成使用少量（20 - 40微克；39 - 77纳摩尔）的甲苯磺酸盐前体和[(18)F]氟离子（0.5 - 2.5毫居里）。关于前体用量、反应温度、流速以及[(18)F]氟离子与前体比例的影响，在该装置中对标记反应的优化迅速完成，并且[(18)F]法利帕德的衰变校正放射化学产率（高达88%）具有可重复性。每次放射性合成中使用的少量材料使得粗制的[(18)F]法利帕德在用于静脉注射的制剂制备之前，能够在分析尺寸的反相高效液相色谱柱上快速纯化。通过连续注入试剂前体溶液以获得数量更多的[(18)F]法利帕德，很容易实现反应的放大。
