~(188)Re-TCTMP的合成及在小鼠体内的分布

~(188)Re-TCTMP的合成及在小鼠体内的分布

PREPARATION AND BIODISTRIBUTION OF ~(188)Re-TCTMP

摘要

摘要: 合成了氮杂环甲撑膦酸配体TCTMP(1,4,8,11 四氮杂环十四烷 1,4,8,11 四甲基膦酸),研究了亚锡还原下188Re TCTMP的制备条件,并探索了该配合物的体外稳定性及在正常小鼠体内分布。结果表明,pH=2,SnCl2量为0 8～1 6mg,配体量为50mg时,可以制得标记率大于95%的配合物188Re TCTMP;配合物具有很高的体外稳定性,室温下放置8d,标记率仍不低于95%。小鼠体内分布表明,配合物很快为小鼠骨骼摄取并保留较长时间;与188Re HEDP(1 羟基亚乙基二膦酸)相比,188Re TCTMP表现出更低的非靶组织摄取。因此,188Re TCTMP有望取代186,188Re HEDP,成为新型的缓解治疗骨肿瘤疼痛的放射性药物。

Abstract: TCTMP(1,4,8,11tertraaza cyclotetradecyl1,4,8,11tetramethylene phosphonate) is synthesized and coupled with 188Re. The coupling condition,stability and biodistribution of 188ReTCTMP in mice are investigated. The results show that satisfactory complexation yield of 188Re could be obtained under condition of medium pH=2.0,0.8～1.6 mg of SnCl2 and 50 mg of ligand. The complex exhibits high stability and maintains its high complexation yield (>95%) in 8 d without protection of N2. The results of biodistribution indicate considerably strong affinity of 188ReTCTMP to bone and very low nontarget tissue's uptake. The concentration of 188ReTCTMP in blood is (0.06±0.02)%/g at 6 h after injection,while the concentration of 188ReHEDP is (0.28±0.05) %/g at 6 h after injection,which might be due to the higher stability of 188ReTCTMP in vitro and in vivo. Comparing with 188ReHEDP,188ReTCTMP exhibits better potential for the treatment of metastases.

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