Olaru Alexandra M, Robertson Thomas B R, Lewis Jennifer S, Antony Alex, Iali Wissam, Mewis Ryan E, Duckett Simon B
Centre for Hyperpolarization in Magnetic Resonance, Department of Chemistry University of York Heslington YO10 5NY United Kingdom.
School of Science and the Environment, Division of Chemistry and Environmental Science Manchester Metropolitan University John Dalton Building, Chester St. Manchester M1 5GD United Kingdom.
ChemistryOpen. 2017 Dec 21;7(1):97-105. doi: 10.1002/open.201700166. eCollection 2018 Jan.
Fluorinated ligands have a variety of uses in chemistry and industry, but it is their medical applications as F-labelled positron emission tomography (PET) tracers where they are most visible. In this work, we illustrate the potential of using F-containing ligands as future magnetic resonance imaging (MRI) contrast agents and as probes in magnetic resonance spectroscopy studies by significantly increasing their magnetic resonance detectability through the signal amplification by reversible exchange (SABRE) hyperpolarization method. We achieve F SABRE polarization in a wide range of molecules, including those essential to medication, and analyze how their steric bulk, the substrate loading, polarization transfer field, pH, and rate of ligand exchange impact the efficiency of SABRE. We conclude by presenting F MRI results in phantoms, which demonstrate that many of these agents show great promise as future F MRI contrast agents for diagnostic investigations.
氟化配体在化学和工业中有多种用途,但它们作为F标记的正电子发射断层扫描(PET)示踪剂的医学应用最为显著。在这项工作中,我们通过可逆交换信号放大(SABRE)超极化方法显著提高含氟配体的磁共振可检测性,从而展示了将其用作未来磁共振成像(MRI)造影剂以及磁共振波谱研究中的探针的潜力。我们在包括药物关键分子在内的多种分子中实现了F SABRE极化,并分析了它们的空间位阻、底物负载、极化转移场、pH值和配体交换速率如何影响SABRE的效率。我们通过展示在模型中的F MRI结果得出结论,这些结果表明许多此类试剂作为未来用于诊断研究的F MRI造影剂具有很大的潜力。