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A kit-based aluminium-[18F]fluoride approach to radiolabelled microbubbles.


ABSTRACT: The production of 18F-labelled microbubbles (MBs) via the aluminium-[18F]fluoride ([18F]AlF) radiolabelling method and facile inverse-electron-demand Diels-Alder (IEDDA) 'click' chemistry is reported. An [18F]AlF-NODA-labelled tetrazine was synthesised in excellent radiochemical yield (>95% RCY) and efficiently conjugated to a trans-cyclooctene (TCO) functionalised phospholipid (40-50% RCY), which was incorporated into MBs (40-50% RCY). To demonstrate the potential of producing 18F-labelled MBs for clinical studies, we also describe a kit-based approach which is amenable for use in a hospital radiopharmacy setting.

SUBMITTER: Teh JH 

PROVIDER: S-EPMC8567295 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature

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A kit-based aluminium-[<sup>18</sup>F]fluoride approach to radiolabelled microbubbles.

Teh Jin Hui JH   Braga Marta M   Allott Louis L   Barnes Chris C   Hernández-Gil Javier J   Tang Meng-Xing MX   Tang Meng-Xing MX   Aboagye Eric O EO   Long Nicholas J NJ  

Chemical communications (Cambridge, England) 20211104 88


The production of <sup>18</sup>F-labelled microbubbles (MBs) <i>via</i> the aluminium-[<sup>18</sup>F]fluoride ([<sup>18</sup>F]AlF) radiolabelling method and facile inverse-electron-demand Diels-Alder (IEDDA) 'click' chemistry is reported. An [<sup>18</sup>F]AlF-NODA-labelled tetrazine was synthesised in excellent radiochemical yield (>95% RCY) and efficiently conjugated to a <i>trans</i>-cyclooctene (TCO) functionalised phospholipid (40-50% RCY), which was incorporated into MBs (40-50% RCY). T  ...[more]

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