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, David, Goblet, David, Goukens, Eve, Kaisin, Geoffroy, Paris, Jérôme, Aerts, Joël, Lignon, Steve, Franci, Xavier, Hustinx, Roland, Luxen, André, Paris, Jérôme, Aerts, Joël, and Luxen, André
- Subjects
MOLECULAR biology ,BIOMOLECULES ,FLUOROBENZOIC acid ,POSITRON emission tomography ,RADIOCHEMISTRY ,ANTI-infective agents ,AUTOMATION ,COMPARATIVE studies ,PHYSICAL & theoretical chemistry ,FLUORINE isotopes ,HETEROCYCLIC compounds ,RESEARCH methodology ,MEDICAL cooperation ,MOLECULAR structure ,OLIGOPEPTIDES ,RADIOISOTOPES ,RESEARCH ,EVALUATION research ,EQUIPMENT & supplies - 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. [ABSTRACT FROM AUTHOR]- Published
- 2011
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