• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Chinese science bulletin >~(99m)Tc complex conjugated to insulin: CMS radio-pharmaceuticals design based on principles of blood-brain barrier transport vector
【24h】

~(99m)Tc complex conjugated to insulin: CMS radio-pharmaceuticals design based on principles of blood-brain barrier transport vector

机译：〜（99m）Tc复合物与胰岛素结合：基于血脑屏障转运载体原理的CMS放射性药物设计

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Hydrophilic ~(99m)Tc-EC and nonlipophilic ~(99m)Tc-MAMA'-BA complexes, owing to the existing of intact blood-brain barrier (BBB) in vivo., cannot cross from to brain. Previous studies showed that insulin is selectively transported by receptor-mediated transcytosis through the brain capillary endothelial wall that makes up the BBB. In this paper, based on the characteristic of the insulin receptor enriched in brain capillary, the complexes of hydrophilic ~(99m)Tc-EC and nonlipophilic ~(99m)Tc-MAMA'-BA are conjugated to insulin respectively. After purification, the radiochemical purity of ~(99m)Tc-EC-insulin nd ~(99m)Tc-MAMA'-BA-insulin was > 90 percent and the stability HI vitro was good. Expectation for the special formulation can be internalized and endocytosed into the capillary membrane by the vector-mediated brain delivery system, and transported ~(99m)Tc-labeled conjugate through the BBB in vivo, thus enhancing brain uptake in mice. The biodistribution results of ~(99m)Tc-EC-insulin and ~(99m)Tc-MAMA'-BA-insulin in mice indicated that the brain uptake was higher than ~(99m)Tc-EC ~(99m)Tc-MAMA'-BA to some extent. The ratios of of ~(99m)Tc-EC-insulin to ~(99m)Tc-EC, ~(99m)Tc-MAMA'-BA-insulin to ~(99m)Tc-MAMA'-BA were 4-6 at 2 and 3 h post-injection respectively. In conclusion, the given results have illustrated a new way of brain uptake enhancing for nonlipophilic like complexes that have BBB delivery problems. It has a potential value for the ongoing development of ~(99m)Tc-labeled radiopharmaceuticals for CNS receptors imaging.
机译：由于体内存在完整的血脑屏障（BBB），亲水性〜（99m）Tc-EC和非亲和性〜（99m）Tc-MAMA'-BA复合物无法穿过大脑。先前的研究表明，胰岛素是通过受体介导的胞吞作用通过构成BBB的脑毛细血管内皮壁选择性转运的。本文根据脑毛细血管中丰富的胰岛素受体的特性，将亲水性〜（99m）Tc-EC和非亲脂性〜（99m）Tc-MAMA'-BA的复合物与胰岛素偶联。纯化后，〜（99m）Tc-EC-胰岛素和〜（99m）Tc-MAMA'-BA-胰岛素的放射化学纯度均大于90％，体外HI稳定性良好。可以通过载体介导的脑递送系统将对特殊制剂的期望内化并内吞到毛细血管膜中，并在体内通过BBB转运〜（99m）Tc标记的结合物，从而增强小鼠的脑摄取。 〜（99m）Tc-EC胰岛素和〜（99m）Tc-MAMA'-BA-胰岛素在小鼠中的生物分布结果表明，脑摄取高于〜（99m）Tc-EC〜（99m）Tc-MAMA '-BA在某种程度上。 〜（99m）Tc-EC-胰岛素与〜（99m）Tc-EC，〜（99m）Tc-MAMA'-BA-胰岛素与〜（99m）Tc-MAMA'-BA的比例为4-6注射后分别为2小时和3小时。总之，给定的结果说明了增加具有BBB传递问题的非亲脂性复合物的脑摄取新方法。它对正在进行的〜（99m）Tc标记的放射性药物用于CNS受体成像具有潜在的价值。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号