Cationic technetium and rhenium complexes with pendant carbohydrates
Cationic technetium and rhenium complexes with pendant carbohydrates
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DOI：
10.1016/j.apradiso.2010.01.033
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发表时间：
2010-06-01
影响因子：
1.6
通讯作者：
Orvig, Chris
中科院分区：
文献类型：
--
作者：
Ferreira, Cara L.;Marques, Fabio L. N.;Orvig, Chris
三种碳水化合物共轭二吡啶甲基胺螯合剂，2-双（2-吡啶甲基）氨基）乙基1-脱氧-1-硫代-β-D-吡喃葡萄糖苷（L-1），2-双（2-吡啶基甲基）氨基）乙基-β-D-吡喃葡萄糖苷（L-2）和2-双（2-吡啶甲基）氨基）甲酰胺-N-将2-氨基-2-脱氧-D-吡喃葡萄糖（L-3）与[M（Co）（3）]（+）核（M=Tc，Re）形成配合物，研究了配合物的性质。报道了螯合剂2-二（2-吡啶甲基）氨基）乙基1-脱氧-1-硫代-β-D-吡喃葡萄糖苷（L-1）及其铼配合物的合成与表征。所有螯合剂均以高产率用[（99）mTc（CO）（3）（H2O）（3）]（+）（> 98%）和[Re-186（CO）（3）（H2O）（3）]（+）（> 80%）进行放射性标记。螯合剂和Re-络合物被确定为不是葡萄糖代谢酶己糖激酶的底物。然而，每种Tc-99 m络合物的生物分布表明从大多数背景组织的快速清除，包括在注射后2小时内在肾脏和肝脏中>75%的活性清除。(C)2010爱思唯尔有限公司版权所有。
Three carbohydrate conjugated dipicolylamine chelators, 2-bis(2-pyridinylmethyl)amino)ethyl 1-deoxy-1-thio-beta-D-glucopyranoside (L-1), 2-bis(2-pyridinylmethyl)amino)ethyl-beta-D-glucopyranoside (L-2), and 2-bis(2-pyridinylmethyl)amino)carboxamide-N-(2-amino-2-deoxy-D-glucopyranose) (L-3) were complexed to the [M(Co)(3)](+) core (M=Tc, Re) and the properties of the resulting complexes were investigated. Synthesis and characterization of the chelator 2-bis(2-pyridinylmethyl)amino)ethyl 1-deoxy-1-thio-beta-D-glucopyranoside (L-1) and the corresponding Re complex are reported. All chelators were radiolabeled in high yield with [(99)mTc(CO)(3)(H2O)(3)](+) ( > 98%) and [Re-186(CO)(3)(H2O)(3)](+) ( > 80%). The chelators and Re-complexes were determined to not be substrates for the glucose metabolism enzyme hexokinase. However, the biodistribution of each of the Tc-99m complexes demonstrated fast clearance from most background tissue, including >75% clearance of the activity in the kidneys and the liver within 2 h post-injection. (C) 2010 Elsevier Ltd. All rights reserved.