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[18F]Fluoroalkyl azides for rapid radiolabeling and (Re)investigation of their potential towards in vivo click chemistryElectronic supplementary information (ESI) available. See DOI: 10.1039/c7ob00880e
In recent years, radiofluorinated alkyl azides have been reported for click radiolabeling and pretargeted PET imaging, but only little is known about the biodistribution and metabolism of these compounds. In this work, we present a significantly improved procedure for the synthesis of [ 18 F]fluoroe...
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| Main Authors: | , , , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Online Access: | Get full text |
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| Summary: | In recent years, radiofluorinated alkyl azides have been reported for
click
radiolabeling and pretargeted PET imaging, but only little is known about the biodistribution and metabolism of these compounds. In this work, we present a significantly improved procedure for the synthesis of [
18
F]fluoroethyl azide and reinvestigated this radiolabeled probe in detail showing poor stability and very restricted suitability for
in vivo
application. Therefore, modified low-molecular-weight [
18
F]fluoroalkyl azides were developed. Propargyl-tagged endomorphin-1 (as model compound) was successfully radiolabeled in high yield and short reaction time making these probes useful and efficient bioorthogonal tools for rapid radiolabeling. Biodistribution, pharmacokinetics and
in vivo
stability were studied by preclinical PET/MR scanning and metabolite analysis. The results of this study revealed only limited applicability of [
18
F]fluoroalkyl azides for
in vivo
application.
[
18
F]Fluoroalkyl azides were developed as efficient click agents for rapid radiolabeling, and (re)investigated towards application in pretargeted PET imaging. |
|---|---|
| ISSN: | 1477-0520 1477-0539 |
| DOI: | 10.1039/c7ob00880e |