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Appl Radiat Isot. 2015 Jan;95:76-84. doi: 10.1016/j.apradiso.2014.09.016. Epub 2014 Oct 8.

A high-yield automated radiosynthesis of the alpha-7 nicotinic receptor radioligand [18F]NS10743.

Author information

1
Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Germany. Electronic address: r.teodoro@hzdr.de.
2
Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, Germany.
3
Molecular Neuroimaging Program, Molecular Imaging Center, National Institute of Radiological Sciences, Inage-ku, Chiba, Japan.
4
DanPET AB, Malmö, Sweden.

Abstract

[18F]NS10743, a promising and highly competitive α7 nAChR radioligand has been synthesized so far by microwave irradiation using a manual single-mode device followed by a palladium-catalyzed reduction of remaining nitro-precursor for HPLC separation purposes. For further preclinical and clinical use, regulated production of [18F]NS10743 by fully automated radiosynthesis is a crucial requirement. Therefore, we chose a commercial synthesis module and developed the automated radiosynthesis of [18F]NS10743. Besides evaluation of several radiosynthesis procedures, we performed an extensive HPLC study for quantitative separation of [18F]NS10743 from the corresponding nitro precursor. After implementation of the optimized procedure on a TRACERlabTM FX F-N synthesis module, [18F]NS10743 was obtained in high radiochemical purity (≥99%) with an overall radiochemical yield of 32.2±7% (n=3). The specific activities at the end of the synthesis were 571±17GBq/µmol (n=3).

KEYWORDS:

Alpha-7 nicotinic acetylcholine receptor radioligand; Automated radiosynthesis; Pet WAVE microwave CEM(®); Radiofluorination; TRACERlab(TM) FX F-N

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