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引用次数: 0
摘要
本研究对[64Cu]Cu-BPAMD（一种用于 PET 成像的新型骨探寻剂）进行了临床前评估和剂量估算。所制备的[64Cu]Cu-BPAMD 的比活度为 8.7 GBq/µmol，放射化学纯度（R.P.）为 98%。HA 结合结果显示，几乎所有的 [64Cu]Cu-BPAMD 复合物都与 HA 结合，结合量约为 15 毫克。在雄性叙利亚大鼠体内进行的生物分布研究表明，[64Cu]Cu-BPAMD 复合物在骨骼中大量蓄积，而在其他器官中的吸收则微乎其微。骨表面和骨髓分别吸收了 0.199 和 0.092 mGy/MBq，是吸收剂量最大的器官。这项研究证实了[64Cu]Cu-BPAMD 的生产具有较高的 R.P.，在骨转移的 PET 成像方面具有很大的潜力。与 68Ga-BPAMD 相比，主要人体器官的吸收剂量更低，这可以说是这种新型放射性标记化合物的优势之一。
Development of [64Cu]Cu-BPAMD for PET imaging of bone metastases
In this study, preclinical evaluation and dosimetric estimation of [64Cu]Cu-BPAMD, as a new bone-seeking agent for PET imaging, was studied. [64Cu]Cu-BPAMD was produced with a specific activity of 8.7 GBq/µmol and radiochemical purity (R.P.) of >98 %. The HA binding results showed the binding of nearly all [64Cu]Cu-BPAMD complex to HA at about 15 mg. Biodistribution studies in the male Syrian rats indicated considerable accumulation in the bone with negligible uptake in the other organs. The bone surface and the bone marrow receiving 0.199 and 0.092 mGy/MBq, respectively, are the organs with the most absorbed dose. This study confirms the production of [64Cu]Cu-BPAMD with high R.P. showing high potential for PET-imaging of bone metastases. The lower absorbed dose of mainly human organs compared to 68Ga-BPAMD can be considered one of the advantages of this new radiolabeled compound.
期刊介绍：
Accounts of Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry and biochemistry. These short reviews focus on research from the author’s own laboratory and are designed to teach the reader about a research project. In addition, Accounts of Chemical Research publishes commentaries that give an informed opinion on a current research problem. Special Issues online are devoted to a single topic of unusual activity and significance.
Accounts of Chemical Research replaces the traditional article abstract with an article "Conspectus." These entries synopsize the research affording the reader a closer look at the content and significance of an article. Through this provision of a more detailed description of the article contents, the Conspectus enhances the article's discoverability by search engines and the exposure for the research.
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