Automation of the radiosynthesis and purification procedures for [18F]Fluspidine preparation, a new radiotracer for clinical investigations in PET imaging of σ1 receptors in brain.


Automation of the radiosynthesis and purification procedures for [18F]Fluspidine preparation, a new radiotracer for clinical investigations in PET imaging of σ1 receptors in brain.

Maisonial-Besset, A.; Funke, U.; Wenzel, B.; Fischer, S.; Holl, K.; Wünsch, B.; Steinbach, J.; Brust, P.

Abstract

The radiosynthesis of [18F]Fluspidine, a potent σ1 receptor imaging probe for preclinical/clinical studies, was implemented on a TRACERlabTM FX F-N synthesizer. [18F]2 was synthesized in 15 min at 85 °C starting from its tosylate precursor. Purification via semipreparative 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, [18F]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).1 receptor imaging probe for preclinical/clinical studies, was implemented on a TRACERlabTM FX F-N synthesizer. [18F]2 was synthesized in 15 min at 85 °C starting from its tosylate precursor. Purification via semipreparative 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, [18F]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).

Keywords: [18F]Fluspidine; one-step automated radiosynthesis; positron emission tomography; σ1 receptors

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