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用于放射性核素治疗的铼(V)氮化物放射性药物。

Re(V) Nitrido Radiopharmaceuticals for Radionuclide Therapy.

作者信息

Boschi Alessandra, Martini Petra, Uccelli Licia

机构信息

Department of Morphology, Surgery and Experimental Medicine, University of Ferrara, Ferrara 44121, Italy.

Italy and Legnaro National Laboratories, Italian National Institute for Nuclear Physics (LNL-INFN), Legnaro (PD) 35020, Italy.

出版信息

Pharmaceuticals (Basel). 2017 Jan 19;10(1):12. doi: 10.3390/ph10010012.

Abstract

The favorable nuclear properties of rhenium-188 for therapeutic application are described, together with new methods for the preparation of high yield and stable Re radiopharmaceuticals characterized by the presence of the nitride rhenium core in their final chemical structure. Re is readily available from an W/Re generator system and a parallelism between the general synthetic procedures applied for the preparation of nitride technetium-99m and rhenium-188 theranostics radiopharmaceuticals is reported. Although some differences between the chemical characteristics of the two metallic nitrido fragments are highlighted, it is apparent that the same general procedures developed for the labelling of biologically active molecules with technetium-99m can be applied to rhenium-188 with minor modification. The availability of these chemical strategies, that allow the obtainment, in very high yield and in physiological condition, of Re radiopharmaceuticals, gives a new attractive prospective to employ this radionuclide for therapeutic applications.

摘要

本文描述了铼-188在治疗应用中良好的核性质,以及制备高产率和稳定的铼放射性药物的新方法,这些药物的最终化学结构中含有氮化铼核心。铼可从钨/铼发生器系统中轻松获得,并且报道了用于制备氮化锝-99m和铼-188治疗诊断放射性药物的一般合成程序之间的相似性。尽管强调了两种金属氮化物片段化学特性之间的一些差异,但显然,为用锝-99m标记生物活性分子而开发的相同一般程序稍作修改后即可应用于铼-188。这些化学策略能够在非常高的产率和生理条件下获得铼放射性药物,这为将这种放射性核素用于治疗应用提供了一个新的有吸引力的前景。

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