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Synthesis and characterisation of zirconium complexes for cell tracking with Zr-89 by positron emission tomography

机译:通过正电子发射断层扫描合成和表征用于Zr-89细胞追踪的锆复合物

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摘要

The increasing availability of the long half-life positron emitter Zr-89 (half life 78.4 h) suggests that it is a strong candidate for cell labelling and hence cell tracking using positron emission tomography. The aim was to produce a range of neutral ZrL_4 lipophilic complexes for cell labelling which could be prepared under radiopharmaceutical conditions. This was achieved when the ligand was oxine, tropolone or ethyl maltol. The complexes can be prepared in high yield from zirconium(IV) precursors in hydrochloric or oxalic acid solution. The oxinate and tropolonate complexes were the most amenable to chromatographic characterisation, and HPLC and ITLC protocols have been established to monitor their radiochemical purity. The radiochemical synthesis and quality control of ~(89)Zr(oxinate)_4 is reported as well as preliminary cell labelling data for the oxinate, tropolonate and ethyl maltolate complexes which indicates that ~(89)Zr(oxinate)_4 is the most promising candidate for further evaluation.
机译:长半衰期正电子发射器 Zr-89(半衰期 78.4 小时)的可用性不断提高,表明它是细胞标记的有力候选者,因此使用正电子发射断层扫描进行细胞跟踪。目的是生产一系列用于细胞标记的中性ZrL_4亲脂性复合物,这些复合物可以在放射性药物条件下制备。这是当配体是氧嘧啶、托波隆酮或乙基麦芽酚时实现的。该复合物可以从盐酸或草酸溶液中的锆(IV)前体中以高收率制备。氧酸盐和原氯酸盐复合物最适合色谱表征,并且已经建立了HPLC和ITLC方案来监测它们的放射化学纯度。报道了~(89)Zr(oxinate)_4的放射化学合成和质量控制,以及oxinate、tropolonate和ethyl-maltolate复合物的初步细胞标记数据,表明~(89)Zr(oxinate)_4是最有希望进一步评估的候选者。

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