Synthesis of a new cage ligand, SarAr, and its complexation with selected transition metal ions for potential use in radioimaging
Synthesis of a new cage ligand, SarAr, and its complexation with selected transition metal ions for potential use in radioimaging
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DOI：
10.1039/b103242a
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发表时间：
2001-01-01
期刊：
影响因子：
--
通讯作者：
Smith, SV
中科院分区：
文献类型：
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作者：
Di Bartolo, NM;Sargeson, AM;Smith, SV
设计了一种新的六氮杂环环笼形配体- 1-N-（4-氨基苄基）-3,6,10,13,16,19-六氮杂环[6.6.6]二十烷-1,8-二胺（SarAr），用于偶联蛋白质。合成了SarAr，并通过微量分析、H-1 NMR和电喷雾质谱对其进行了表征。选择的过渡金属离子(Cu（II), Ni（II）和Co(II)）在10(-6)M下由SarAr络合在30分钟内完成，pH值为6 ~ 8。研究了[Cu-64(SarAr)]（2+）配合物在放射成像中的应用。[Cu-64(sar)]（2+）配合物在人血浆中至少稳定174小时，在小鼠体内的生物分布研究表明，[Cu-64(SarAr)]（2+）配合物与游离的Cu-64（2+）不同，可通过肾脏系统迅速排出。综上所述，SarAr的合成简单、配位性好、[Cu(SarAr)]（2+）配合物对Cu-64解离的动力学和易于从小鼠体内清除的特性使其在核医学中具有诱人的应用前景。
A new hexaazamacrobicyclic cage ligand, 1-N-(4-aminobenzyl)-3,6,10,13,16,19-hexaazabicyclo[6.6.6]eicosane-1,8-diamine (SarAr) has been designed for conjugation to proteins. SarAr was synthesised and characterised by microanalyses, H-1 NMR and electrospray mass spectrometry. The complexation of selected transition metal ions (Cu(II), Ni(II) and Co(II) at 10(-6) M) by SarAr was complete within 30 min over pH 6 to 8. The [Cu-64(SarAr)](2+) complex was investigated with a view to applications in radioimaging. The [Cu-64(sar)](2+) complex was found to be stable in human plasma for at least 174 h and biodistribution studies in mice, showed that the [Cu-64(SarAr)](2+)complex was rapidly excreted through the renal system unlike the free Cu-64(2+). Overall, the simple synthesis, ready complexation behaviour of SarAr, the kineticinertness of the [Cu(SarAr)](2+) complex to dissociation of Cu-64 and its facile elimination from mice make it an attractive prospect for use in nuclear medicine.