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化学进展  2012 

64Cu放射性药物化学

, PP. 1720-1728

Keywords: 放射性药物,64Cu,配体

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Abstract:

64Cu半衰期为12.7h,其衰变过程既发射β+粒子(β+,0.655MeV,17.8%),又发射β-粒子(β-,0.573MeV,38.4%)。近20年来,随着铜配位化学的发展,新型配体不断出现(如DOTA、TETA、NOTA、CB-TE2A、C3B-DO2A等)。Cu(Ⅱ)的络合物在生物体内/外的稳定性不断提高,64Cu已经成功标记在氨基酸、多肽、蛋白、核酸等分子以及纳米颗粒上。64Cu可制成正电子显像药物用作诊断,同时也有发展为放射性治疗药物的潜力。新型铜配体和标记方法以及新的药物靶标的研究已经成为64Cu放射性药物研究的热点,至今已研制出了多种64Cu标记的放射性药物,如64Cu-ATSM是有效的肿瘤乏氧显像剂,64Cu-PTSM是优良的血流示踪剂等。本文旨在介绍64Cu(Ⅱ)几种主要类型的含氮配体以及64Cu标记的放射性药物在显像和治疗方面的最新研究进展,并展望其发展趋势。

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