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用于正电子发射断层显像(PET)成像中铜放射性核素稳定络合的交联大环螯合剂。

Cross-bridged macrocyclic chelators for stable complexation of copper radionuclides for PET imaging.

作者信息

Anderson C J, Wadas T J, Wong E H, Weisman G R

机构信息

Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA.

出版信息

Q J Nucl Med Mol Imaging. 2008 Jun;52(2):185-92. Epub 2007 Nov 28.

Abstract

Copper-64 (t(1/2)=12.7 h; beta+: 17.4%; E(beta+max)=656 keV; beta-: 39%; E(beta-max)=573 keV) has emerged as an important non-standard positron-emitting radionuclide for positron emission tomography imaging of diseased tissues. A significant challenge of working with copper radionuclides is that they must be delivered to the living system as a stable complex that is attached to a biological targeting molecule for effective imaging and therapy. Significant research has been devoted to the development of ligands that can stably chelate (64)Cu, in particular, the cross-bridged (CB) macrocyclic chelators. This review describes the coordination chemistry and biological behavior of (64)Cu-labeled CB complexes.

摘要

铜-64(半衰期t(1/2)=12.7小时;β+发射率:17.4%;最大β+能量E(beta+max)=656千电子伏特;β-发射率:39%;最大β-能量E(beta-max)=573千电子伏特)已成为用于患病组织正电子发射断层显像的一种重要的非标准正电子发射放射性核素。使用铜放射性核素的一个重大挑战是,它们必须作为一种稳定的配合物递送至生物系统,该配合物附着于生物靶向分子以实现有效的成像和治疗。大量研究致力于开发能够稳定螯合64Cu的配体,特别是交叉桥连(CB)大环螯合剂。本综述描述了64Cu标记的CB配合物的配位化学和生物学行为。

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