对含羰基的生物大分子进行原位间接放射性标记的有效方法

Q4 Chemistry

Asian Journal of Chemistry Pub Date : 2024-02-28 DOI:10.14233/ajchem.2024.31197

Barakat M. Shabsoug, Ned D. Heindel

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引用次数: 0

摘要

合成了[125I] 2-(2,3-二碘-4-羟基苯基)-1,3,4-噁二唑（收率为 48%），并在原位进行酸水解，用对硝基苯甲醛直接衍生，得到了所需的 125I 酰腙（收率为 89%）。在一只 Sprague-Dawley 大鼠体内对 125I噁二唑进行了血液清除动力学研究，结果显示其具有双相行为。这项研究表明，125I噁二唑具有潜在的代谢稳定性，足以进行至少 2 小时的成像和跟踪，使其成为原位间接标记含羰基大分子和酮类固醇的可行选择。

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A Useful Method for in situ Indirect Radiolabeling of Carbonyl-Containing Biomolecules

[125I] 2-(2,3-diiodo-4-hydroxyphenyl)-1,3,4-oxadiazole was synthesized (48% yield) and acid-hydrolyzed in situ with direct derivatization with p-nitro benzaldehyde to obtain the required 125I hydrazone (89% yield). A blood clearance kinetic study was performed on the 125I oxadiazole in a Sprague-Dawley rat and a biphasic behaviour was obtained. This study shows that 125I oxadiazole has potential to be metabolically stable and enough to allow imaging and tracking for a minimum of 2 h, making it a viable option for in situ indirect labeling of carbonyl containing macromolecules and keto steroids.

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来源期刊

Asian Journal of Chemistry 化学-化学综合

CiteScore

0.80

自引率

0.00%

发文量

229

审稿时长

4 months

期刊介绍： Information not localized