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合成聚合物放射性核素标记的新偶联策略。

New coupling strategy for radionuclide labeling of synthetic polymers.

作者信息

Hruby Martin, Kucka Jan, Novakova Michaela, Mackova Hana, Vetrik Miroslav

机构信息

Institute of Macromolecular Chemistry AS CR, v.v.i., Heyrovsky Sq. 2, 162 06 Prague 6, Czech Republic.

出版信息

Appl Radiat Isot. 2010 Feb;68(2):334-9. doi: 10.1016/j.apradiso.2009.11.039. Epub 2009 Nov 24.

Abstract

We have developed a radiolabeling strategy for synthetic polymers based on the formation of azo dye usable for both covalent and chelating labeling modalities under mild conditions. Poly[N-(2-hydroxypropyl)methacrylamide] and poly(N-isopropyl acrylamide) were used as model polymers. N-methacryloyl tyrosinamide was introduced into the polymers and the phenolic moiety was then reacted with diazotized chelator precursors. The conjugates were radiolabeled with both the covalently bound (iodine-125) and chelated (indium-111) radionuclides in high yields and sufficient in vitro stability of the labels was proven.

摘要

我们基于偶氮染料的形成开发了一种用于合成聚合物的放射性标记策略,该偶氮染料在温和条件下可用于共价和螯合标记方式。聚[N-(2-羟丙基)甲基丙烯酰胺]和聚(N-异丙基丙烯酰胺)用作模型聚合物。将N-甲基丙烯酰基酪氨酸酰胺引入聚合物中,然后使酚部分与重氮化的螯合剂前体反应。缀合物用共价结合的(碘-125)和螯合的(铟-111)放射性核素进行放射性标记,产率高,并且证明标记物在体外具有足够的稳定性。

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