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Improved 18 F Labeling of Peptides with a Fluoride-Aluminum-Chelate Complex

2010; American Chemical Society; Volume: 21; Issue: 7 Linguagem: Inglês

10.1021/bc100137x

1520-4812

William J. McBride, Christopher D'Souza, Robert M. Sharkey, Habibe Karacay, Edmund A. Rossi, Chien‐Hsing Chang, David M. Goldenberg,

Chemical Synthesis and Analysis

We reported previously the feasibility to radiolabel peptides with fluorine-18 (18F) using a rapid one-pot method that first mixes 18F− with Al3+ and then binds the (Al18F)2+ complex to a NOTA ligand on the peptide. In this report, we examined several new NOTA ligands and determined how temperature, reaction time, and reagent concentration affected the radiolabeling yield. Four structural variations of the NOTA ligand had isolated radiolabeling yields ranging from 5.8% to 87% under similar reaction conditions. All of the Al18F NOTA complexes were stable in vitro in human serum, and those that were tested in vivo also were stable. The radiolabeling reactions were performed at 100 °C, and the peptides could be labeled in as little as 5 min. The IMP467 peptide could be labeled up to 115 GBq/μmol (3100 Ci/mmol), with a total reaction and purification time of 30 min without chromatographic purification.