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用于骨转移诊疗的方形酸双膦酸盐——简便的DOTA-唑来膦酸。

Squaric Acid Bisphposphonates for Theranostics of Bone Metastasis - the Easy DOTA-Zoledronate.

作者信息

Greifenstein Lukas, Engelbogen Nils, Máthé Domokos, Grus Tilmann, Rösch Frank, Bergmann Ralf

机构信息

Curanosticum Wiesbaden-Frankfurt, Wiesbaden, Germany.

Institute of Nuclear Chemistry, Johannes Gutenberg University, Mainz, Germany.

出版信息

Front Nucl Med. 2022 May 10;2:870910. doi: 10.3389/fnume.2022.870910. eCollection 2022.

Abstract

Bisphosponates are an interesting molecular class and in recent years their application has found its way into radiopharmaceutical research and thus into molecular imaging. In addition to great imaging of bone metastases, bisphospnate-based tracers for imaging also have some significant drawbacks. For example, their synthesis is often difficult. Additionally, this can lead to complex and almost impossible purification and quality control. This has limited the production and labeling of suitable molecular and their widespread use to a few facilities. Our squaric acid-based approach provides a way to overcome these problems and makes the synthesis as well as the purification of the compounds much easier. In addition, we were able to demonstrate that labeling with Ga is possible under the typical conditions.

摘要

双膦酸盐是一类有趣的分子,近年来它们已被应用于放射性药物研究,进而进入分子成像领域。除了对骨转移瘤有良好的成像效果外,基于双膦酸盐的成像示踪剂也存在一些显著缺点。例如,它们的合成往往很困难。此外,这可能导致复杂且几乎无法实现的纯化和质量控制。这限制了合适分子的生产、标记及其在少数机构中的广泛应用。我们基于方酸的方法提供了一种克服这些问题的途径,使化合物的合成和纯化变得更加容易。此外,我们能够证明在典型条件下用镓进行标记是可行的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d31d/11440830/d23c2c4d0385/fnume-02-870910-g0001.jpg

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