基于试剂盒的铝-[F]氟化物方法用于放射性标记微泡。

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

机构信息

Department of Chemistry, Molecular Sciences Research Hub, Imperial College London, UK.

Department of Surgery & Cancer, Imperial Centre for Translational and Experimental Medicine, Imperial College London, UK.

出版信息

Chem Commun (Camb). 2021 Nov 4;57(88):11677-11680. doi: 10.1039/d1cc04790f.

DOI:10.1039/d1cc04790f

PMID:34672307

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8567295/

Abstract

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

摘要

报道了 F 标记微泡（MBs）的生产方法，即铝-[F]氟化物（[F]AlF）放射性标记方法和简便的逆电子需求 Diels-Alder（IEDDA）“点击”化学。合成了一种[F]AlF-NODA 标记的四嗪，其放射化学产率优异（>95%RCY），并有效地与 -环辛烯（TCO）功能化磷脂（40-50%RCY）偶联，该磷脂被掺入 MBs（40-50%RCY）中。为了证明为临床研究生产 F 标记 MBs 的潜力，我们还描述了一种基于试剂盒的方法，该方法适用于医院放射药物配制环境。