使用通过直接活化途径生产的 64Cu 制备[64Cu]Cu-NOTA 复合物,作为一种潜在的肾脏 PET 成像剂

IF 1.4 3区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR
Sourav Patra, Sachin Jadhav, Priyalata Shetty, Khajan Singh, Ardhi Rajeswari, K. V. Vimalnath, Avik Chakraborty, Rubel Chakravarty, Sudipta Chakraborty
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引用次数: 0

摘要

与传统的伽马成像相比,肾脏正电子发射断层扫描(PET)能更准确地测定肾小球滤过率(GFR)。铜-64 [T ½ = 12.7 h, E β+ (max) = 653 keV, β+ 支化率 = 17.8 %, 1346 keV γ-光子 (0.54 %), EC (43.8 %), β- 发射 (38.4 %)]以其与 1,4,7-三氮杂环壬烷-1,4,7-三乙酸(NOTA)的亲水复合物的形式被提出作为肾脏 PET 成像的有效制剂。利用在研究反应堆中通过热中子活化产生的 64Cu,开发了一种冻干试剂盒,用于配制 370 MBq 剂量的[64Cu]Cu-NOTA 复合物。该复合物的合成率高达 99%,即使在受到异铁蛋白的挑战时也能保持其完整性。在健康 Wistar 大鼠身上进行的 PET/CT 成像和体内外生物分布研究证明了 [64Cu]Cu-NOTA 在肾脏中的快速积累和通过尿路的清除,从而阐明了它作为肾脏 PET 成像剂的有效性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation of [64Cu]Cu–NOTA complex as a potential renal PET imaging agent using 64Cu produced via the direct activation route
Glomerular filtration rate (GFR) could be determined more accurately using renal positron emission tomography (PET) than conventional gamma imaging. Copper-64 [T ½ = 12.7 h, E β+ (max) = 653 keV, β+ branching ratio = 17.8 %, 1346 keV γ-photon (0.54 %), EC (43.8 %), β emission (38.4 %)] in the form of its hydrophilic complex with 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) is proposed as a potent formulation for renal PET imaging. A lyophilized kit was developed for formulation of ∼370 MBq dose of [64Cu]Cu–NOTA complex in a facile single step process using 64Cu produced by thermal neutron activation in a research reactor. The complex could be synthesized with >99 % yield and retained its integrity even when challenged by apoferritin. The rapid accumulation of [64Cu]Cu–NOTA in the kidney and clearance through urinary path was demonstrated using PET/CT imaging and ex vivo biodistribution study carried out in healthy Wistar rats to elucidate its effectiveness as a renal PET-imaging agent.
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来源期刊
Radiochimica Acta
Radiochimica Acta 化学-核科学技术
CiteScore
2.90
自引率
16.70%
发文量
78
审稿时长
6 months
期刊介绍: Radiochimica Acta publishes manuscripts encompassing chemical aspects of nuclear science and technology.
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