带有悬挂碳水化合物的阳离子锝和铼配合物。

Cationic technetium and rhenium complexes with pendant carbohydrates.

作者信息

Ferreira Cara L, Marques Fabio L N, Okamoto Miriam R Y, Otake Andréia H, Sugai Yuko, Mikata Yuji, Storr Tim, Bowen Meryn, Yano Shigenobu, Adam Michael J, Chammas Roger, Orvig Chris

机构信息

Medicinal Inorganic Chemistry Group, Department of Chemistry, University of British Columbia, 2036 Main Mall, Vancouver, BC, Canada.

出版信息

Appl Radiat Isot. 2010 Jun;68(6):1087-93. doi: 10.1016/j.apradiso.2010.01.033. Epub 2010 Jan 28.

DOI:10.1016/j.apradiso.2010.01.033

PMID:20153207

Abstract

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 (99m)Tc(CO)(3)(H(2)O)(3) (>98%) and (186)Re(CO)(3)(H(2)O)(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 (99m)Tc complexes demonstrated fast clearance from most background tissue, including >75% clearance of the activity in the kidneys and the liver within 2h post-injection.

摘要

三种碳水化合物共轭二吡啶甲胺螯合剂，即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-（2-氨基-2-脱氧-D-吡喃葡萄糖）（L(3)）与M(CO)(3)核（M = Tc、Re）形成络合物，并对所得络合物的性质进行了研究。报道了螯合剂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)）及相应铼络合物的合成与表征。所有螯合剂均能以高产率用(99m)Tc(CO)(3)(H(2)O)(3)（>98%）和(186)Re(CO)(3)(H(2)O)(3)（>80%）进行放射性标记。已确定螯合剂和铼络合物不是葡萄糖代谢酶己糖激酶的底物。然而，每种(99m)Tc络合物的生物分布显示，其能从大多数背景组织中快速清除，包括注射后2小时内肾脏和肝脏中>75%的放射性活性被清除。