Rötering Sven, Scheunemann Matthias, Günther Robert, Löser Reik, Hiller Achim, Brust Peter, Fischer Steffen, Steinbach Jörg
Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Departments of Neuroradiopharmaceuticals and Radiopharmaceutical and Chemical Biology, POB 51 01 19, D-01314 Dresden, Germany.
DanPET AB, Rosenstigen 7, SE-216 19 Malmö, Sweden.
Appl Radiat Isot. 2016 Aug;114:57-62. doi: 10.1016/j.apradiso.2016.04.028. Epub 2016 Apr 28.
Radiopharmacological investigations of [(18)F]NS14490 have proven that this radiotracer could be a potential PET radiotracer for imaging of alpha7 nicotinic acetylcholine receptor particularly with regard to vulnerable plaques of diseased vessels. For further optimisation of the previously automated one-pot radiosynthesis of [(18)F]NS14490 using a tosylate precursor, precursors with other leaving groups (nosylate and mosylate) were synthesized and compared with the tosylate with respect to their reactivities towards [(18)F]fluoride. The use of these different precursors resulted in comparable labelling yields of [(18)F]NS14490. A novel mosylate precursor was synthesized and evaluated, which has revealed a higher stability during a storage period of five months compared to the corresponding tosylate and nosylate.
[(18)F]NS14490的放射性药物研究已证明，这种放射性示踪剂可能是一种潜在的正电子发射断层显像（PET）放射性示踪剂，用于α7烟碱型乙酰胆碱受体成像，特别是关于病变血管的易损斑块。为了进一步优化先前使用甲苯磺酸酯前体对[(18)F]NS14490进行的自动化一锅法放射性合成，合成了具有其他离去基团（壬酸酯和甲磺酸酯）的前体，并将它们与甲苯磺酸酯在与[(18)F]氟化物的反应活性方面进行了比较。使用这些不同的前体导致[(18)F]NS14490具有相当的标记产率。合成并评估了一种新型甲磺酸酯前体，与相应的甲苯磺酸酯和壬酸酯相比，它在五个月的储存期内显示出更高的稳定性。
