In Vivo Positron Emission Tomography (PET) Imaging with an αvβ6 Specific Peptide Radiolabeled using 18F-“Click” Chemistry: Evaluation and Comparison with the Corresponding 4-[18F]Fluorobenzoyl- and 2-[18F]Fluoropropionyl-Peptides
- 12 September 2008
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 51 (19) , 5901-5904
- https://doi.org/10.1021/jm800608s
Abstract
Numerous radiolabeled peptides have been utilized for in vivo imaging of a variety of cell surface receptors. For applications in PET using [18F]fluorine, peptides are radiolabeled via a prosthetic group approach. We previously developed solution-phase 18F-“click” radiolabeling and solid-phase radiolabeling using 4-[18F]fluorobenzoic and 2-[18F]fluoropropionic acids. Here we compare the three different radiolabeling approaches and report the effects on PET imaging and pharmacokinetics. The prosthetic groups did have an effect; metabolites with significantly different polarities were observed.Keywords
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