与生物相容性树枝状聚合物的共轭增加了用于磁共振成像（MRI）的羟基吡啶酮（HOPO）配合物的镧系元素弛豫率。
Conjugation to Biocompatible Dendrimers Increases Lanthanide Relaxivity of Hydroxypyridinone (HOPO) Complexes for Magnetic Resonance Imaging (MRI).
作者信息
Klemm Piper J, Floyd William C, Andolina Christopher M, Fréchet Jean M J, Raymond Kenneth N
机构信息
Department of Chemistry, University of California, Berkeley, Berkeley, California 94720 United States.
出版信息
Eur J Inorg Chem. 2012 Apr;2012(12):2108-2114. doi: 10.1002/ejic.201101167.
Magnetic resonance imaging (MRI) contrast agents represent a worldwide billion-dollar market annually. While relaxivity enhancement contrast agents receive greater attention and a significantly larger market share, the commercial potential for relaxivity enhancing contrast agents remains a viable diagnostic option due to their increased relaxivity at high field strengths. Improving the contrast and biocompatibility of MRI probes may enable new diagnostic prospects for MRI. Paramagnetic lanthanides have the potential to decrease and proton relaxation times, but are not commercially used in MRI diagnostics as agents. In this article, oxygen donor chelates (hydroxypyridinone, HOPO, and terephthalamide, TAM) of various lanthanides are demonstrated as biocompatible macromolecular dendrimer conjugates for the development of MRI probes. These conjugates have relaxivities up to 374 mms per dendrimer, high bioavailability, and low toxicity.
磁共振成像（MRI）造影剂每年在全球的市场规模达数十亿美元。虽然弛豫率增强型造影剂受到了更多关注且占据了显著更大的市场份额，但由于其在高场强下弛豫率的增加，弛豫率增强型造影剂的商业潜力仍是一种可行的诊断选择。改善MRI探针的对比度和生物相容性可能为MRI带来新的诊断前景。顺磁性镧系元素有降低 和质子弛豫时间的潜力，但未作为造影剂在MRI诊断中商业化使用。在本文中，各种镧系元素的氧供体螯合物（羟基吡啶酮，HOPO，和对苯二甲酰胺，TAM）被证明是用于开发MRI探针的生物相容性大分子树枝状聚合物共轭物。这些共轭物每个树枝状聚合物的弛豫率高达374 mms，具有高生物利用度和低毒性。
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