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角关联技术在放射性药物前体研究中的应用

Perturbed Angular Correlation as a Tool to Study Precursors for Radiopharmaceuticals.

机构信息

Dzhelepov Laboratory of Nuclear Problems, Joint Institute for Nuclear Research, Dubna 141980, Russian Federation.

Department of High-Energy Chemistry and Radioecology, D. Mendeleev University of Chemical Technology of Russia, Moscow 125047, Russian Federation.

出版信息

Inorg Chem. 2020 Sep 8;59(17):12209-12217. doi: 10.1021/acs.inorgchem.0c01208. Epub 2020 Aug 24.

Abstract

One of the key components of radiopharmaceuticals for targeting imaging and therapy is a stable bifunctional chelating system to attach radionuclides to selective delivery systems. After-effects of radioactive decay can cause the release of a radioactive isotope from its chelation agent. Perturbed angular correlation (PAC) of γ-rays has become a unique technique to study the behavior of complexes formed between a chelating agent and radionuclide (in real time) over a relevant range of concentrations (10 M). In the present work, four radionuclides, In, Cd, and Eu, were investigated with diethylenetriaminepentaacetic acid (DTPA) at different pH values to determine the stability constants of the complexes as well as the effects of post-decay processes, which play a major role in determining the suitability of these complexes for application as radiopharmaceuticals (e.g., generators). The study provides a convenient parameter for the characterization of radionuclide-chelator systems using the PAC method. PAC is proven to be a suitable tool to study novel chelators and radiopharmaceutical precursors attached to radiometals.

摘要

放射性药物的关键组成部分之一是一种稳定的双功能螯合系统,用于将放射性核素连接到选择性输送系统上。放射性衰变的后效会导致放射性同位素从其螯合剂中释放出来。受激角关联(PAC)的γ射线已经成为一种独特的技术,可以在相关浓度范围内(10 M)实时研究螯合剂与放射性核素之间形成的配合物的行为。在本工作中,研究了四种放射性核素,即 In、Cd 和 Eu,与二乙三胺五乙酸(DTPA)在不同 pH 值下的相互作用,以确定配合物的稳定常数以及后衰变过程的影响,后衰变过程在确定这些配合物作为放射性药物(例如发生器)的适用性方面起着主要作用。该研究为使用 PAC 方法对放射性核素-螯合剂系统进行表征提供了一个方便的参数。PAC 被证明是一种研究附着在放射性金属上的新型螯合剂和放射性药物前体的合适工具。

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