• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Life sciences >Differences between D- and L-aspartate binding to the Na+-dependent binding sites on glutamate transporters in frozen sections of rat brain.
【24h】

Differences between D- and L-aspartate binding to the Na+-dependent binding sites on glutamate transporters in frozen sections of rat brain.

机译：在大鼠脑冷冻切片中，D-天冬氨酸和L-天冬氨酸结合至谷氨酸转运蛋白上Na +-依赖性结合位点之间的差异。

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

The Na+-dependent, "high-affinity" transport of L-glutamate (GluT) in brain tissue has become a significant focus of interest, particularly since it has been revealed that abnormalities of GluT may be associated with serious neurological disorders. Using quantitative autoradiography on 3H-sensitive films, we have studied, in thaw-mounted sections of rat brain, the distribution and pharmacology of radioligand binding to sites with characteristics of the substrate-recognition/binding locus on GluT. The technique makes it possible to determine not only the intensity of binding in brain regions but, with a high level of precision, pharmacological constants such as IC50 or nH. [3H]L-aspartate and [3H]D-aspartate are two classical radioligands used in studies of GluT. We have determined IC50 values for the inhibition of [3H]L- and [3H]D-aspartate binding by their non-radioactive counterparts in the cerebral neocortex. hippocampus, striatum, septal nuclei and the cerebellar cortex. The two radioligands did not appreciably differ from each other in their interactions with the binding sites in the forebrain, consistent with all Na+-dependent GluT binding sites in that region having no stereoselectivity for aspartate enantiomers. In the cerebellar cortex, however, the data indicated the presence of a GluT binding site that preferred L- over D-aspartate. These findings contrast with many previous observations and suggest that the pharmacological characteristics of the ligand binding sites on GluT in the mammalian cerebellar cortex may have to be re-assessed and/or a possibility of an existence of (a) hitherto unknown molecule(s) with properties of a glutamate transporter be considered.
机译：依赖于Na +的L-谷氨酸（GluT）在脑组织中的“高亲和力”运输已成为人们关注的重要焦点，特别是因为已经发现GluT异常可能与严重的神经系统疾病有关。我们在3H敏感胶片上使用定量放射自显影技术，在大鼠脑的解冻部位研究了放射性配体结合到具有GluT底物识别/结合位点特征的位点的分布和药理作用。该技术不仅可以确定大脑区域的结合强度，而且还可以高精度地确定诸如IC50或nH的药理常数。 [3H] L-天冬氨酸和[3H] D-天冬氨酸是用于GluT研究的两种经典的放射性配体。我们已经确定了它们在大脑新皮层中的非放射性对应物对[3H] L-和[3H] D-天冬氨酸结合的抑制作用的IC50值。海马，纹状体，中隔核和小脑皮质。两种放射性配体在与前脑中结合位点的相互作用上没有明显不同，这与该区域中所有对Na +依赖的GluT结合位点均无天冬氨酸对映体立体选择性一致。但是，在小脑皮质中，数据表明存在GluT结合位点，该位点优先于L-而不是D-天冬氨酸。这些发现与许多先前的观察结果形成对比，并暗示可能必须重新评估哺乳动物小脑皮质中GluT上配体结合位点的药理特性和/或存在迄今未知的分子的可能性。具有谷氨酸转运蛋白的性质。

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