Automation of the radiosynthesis and purification procedures for [F-18]Fluspidine preparation, a new radiotracer for clinical investigations in PET imaging of sigma(1) receptors in brain

作者：Maisonial Besset Aurelie^*; Funke Uta; Wenzel Barbara; Fischer Steffen; Holl Katharina; Wuensch Bernhard; Steinbach Joerg; Brust Peter

来源：Applied Radiation and Isotopes, 2014, 84: 1-7.

DOI：10.1016/j.apradiso.2013.10.015

• [F-18]Fluspidine
• One-step automated radiosynthesis
• Positron emission tomography
• sigma(1) receptors

The radiosynthesis of [F-18]Fluspidine, a potent sigma(1) receptor imaging probe for pre-clinical/clinical studies, was implemented on a TRACERlab (TM) FX F-N synthesizer. [F-18]2 was synthesized in 15 min at 85 degrees 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, [F-18]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/mu mol).

• 出版日期2014-2