Centro de Química, Campus de Gualtar, Universidade do Minho, 4710-057 Braga, Portugal.
Nucl Med Biol. 2011 Apr;38(3):363-70. doi: 10.1016/j.nucmedbio.2010.10.003. Epub 2010 Dec 3.
In this work, we report on a synthetic strategy using amphiphilic DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid)-based chelators bearing a variable-sized α-alkyl chain at one of the pendant acetate arms (from 6 to 14 carbon atoms), compatible with their covalent coupling to amine-bearing biomolecules. The amphiphilic behavior of the micelles-forming Ga(III) chelates (critical micellar concentration), their stability in blood serum and their lipophilicity (logP) were investigated. Biodistribution studies with the (67)Ga-labeled chelates were performed in Wistar rats, which showed a predominant liver uptake with almost no traces of the radiochelates in the body after 24 h.
在这项工作中，我们报告了一种使用两亲性 DOTA（1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸）基螯合剂的合成策略，该螯合剂在一个侧臂上带有可变大小的α-烷基链（从 6 个到 14 个碳原子），与它们与含胺的生物分子的共价偶联相容。研究了形成胶束的 Ga(III)螯合物的两亲性（临界胶束浓度）、它们在血清中的稳定性和疏水性（logP）。用（67）Ga 标记的螯合物在 Wistar 大鼠中进行了分布研究，结果表明，在 24 小时后，放射性螯合物在体内的肝脏摄取量较高，几乎没有痕迹。
