Labeling proteins with fluorine-18 using N-succinimidyl 4-[18F]fluorobenzoate.
Journal Article (Journal Article)
Two methods were investigated for the no-carrier-added synthesis of N-succinimidyl 4-[18F]fluorobenzoate (S[18F]FB). The first, an attempted nucleophilic aromatic substitution by [18F]fluoride on N-succinimidyl 4-nitrobenzoate was unsuccessful. The second method involved three steps; [18F]fluoride for trimethylammonium substitution on 4-formyl-N,N,N-trimethylanilinium triflate, oxidation to 4-[18F]fluorobenzoic acid, followed by reaction with N-hydroxysuccinimide and dicyclohexylcarbodiimide to form S[18F]FB. Total synthesis and purification time was 100 min and the overall radiochemical yield was 25% (decay corrected). A monoclonal antibody F(ab')2 fragment could be labeled in 40-60% yield by reaction with S[18F]FB for 15-20 min. The tissue distribution in normal mice and in vitro tumor binding of the antibody F(ab')2 labeled by reaction with S[18F]FB were comparable to those observed for the fragment after radioiodination using N-succinimidyl 4-[125I]iodobenzoate.
Full Text
Duke Authors
Cited Authors
- Vaidyanathan, G; Zalutsky, MR
Published Date
- April 1992
Published In
Volume / Issue
- 19 / 3
Start / End Page
- 275 - 281
PubMed ID
- 1629016
International Standard Serial Number (ISSN)
- 0883-2897
Digital Object Identifier (DOI)
- 10.1016/0883-2897(92)90111-b
Language
- eng
Conference Location
- England