1. Fully automated preparation and conjugation of N-succinimidyl 4-[18F]fluorobenzoate ([18F]SFB) with RGD peptide using a GE FASTlab™ synthesizer.
- Author
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Thonon D, Goblet D, Goukens E, Kaisin G, Paris J, Aerts J, Lignon S, Franci X, Hustinx R, and Luxen A
- Subjects
- Benzoates chemistry, Oligopeptides chemistry, Succinimides chemistry, Automation, Benzoates chemical synthesis, Fluorine Radioisotopes chemistry, Oligopeptides chemical synthesis, Radiochemistry instrumentation, Radiochemistry methods, Succinimides chemical synthesis
- Abstract
Purpose: The aim of this work was to automate the radiosynthesis of [(18)F]SFB, a widely used reagent for the labeling of biomolecules with (18)F on a new generation commercial synthesis module (FASTLab™, GE Healthcare)., Procedures: Two synthesis approaches were implemented on this module: the classical "two-pot radiosynthesis" and the more recently described "one-pot" method., Results: The "two-pot" approach affords [(18)F]SFB with a 42% decay-corrected yield in 57 min (n = 24) with a chemical purity sufficient to avoid an intermediate HPLC purification. The recently established "one-pot" method, afforded a product with a lower chemical purity, in the conditions used in this report. The lower d.c. yield obtained (32% (n = 15)) was related to the low (18)F labeling yields obtained in MeCN compared with DMSO. The subsequent conjugation step with a RGD (PRGD2) peptide was also successfully automated., Conclusions: The formulated [(18)F]FPRGD2 was obtained without any operator manipulation with a d.c. yield of 13% ± 3% (n = 13) in 130 min, a radiochemical purity >98% and a specific activity of 140 ± 40 TBq/mmol.
- Published
- 2011
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