Fully Automated Preparation and Conjugation of N-Succinimidyl 4-[18F]Fluorobenzoate ([18F]SFB) with RGD Peptide Using a GE FASTlab™ Synthesizer

Autor: Joël Aerts, Roland Hustinx, David Goblet, Jérôme Paris, Steve Lignon, Eve Goukens, David Thonon, Geoffroy Kaisin, André Luxen, Xavier Franci
Rok vydání: 2011
Předmět:
Zdroj: Molecular Imaging and Biology. 13:1088-1095
ISSN: 1860-2002
1536-1632
Popis: 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).Two synthesis approaches were implemented on this module: the classical "two-pot radiosynthesis" and the more recently described "one-pot" method.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.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 purity98% and a specific activity of 140 ± 40 TBq/mmol.
Databáze: OpenAIRE
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