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海人酸受体激动剂、拮抗剂和变构调节剂。

Kainate receptor agonists, antagonists and allosteric modulators.

作者信息

Bleakman D, Gates M R, Ogden A M, Mackowiak M

机构信息

Eli Lilly and Company, Neuroscience Division, Corporate Center, Indianapolis, IN 46285, USA.

出版信息

Curr Pharm Des. 2002;8(10):873-85. doi: 10.2174/1381612024607108.

DOI:10.2174/1381612024607108
PMID:11945137
Abstract

Interest in kainate receptors has increased over the past few years. Our understanding of their physiology and pharmacology has improved markedly since their original cloning and expression in the early 1990s. For example, agonist profiles at recombinant kainate receptors have been used to identify and distinguish kainate receptors in neurons. Furthermore, the development of selective antagonists for kainate receptor subtypes has increased our understanding of the functional roles of kainate receptors in neurons and synaptic transmission. In this review we described the activity of agonists and antagonists at kainate receptors and their selectivity profiles at NMDA and non-NMDA receptors.

摘要

在过去几年里,对海人酸受体的关注有所增加。自20世纪90年代初首次克隆和表达以来,我们对其生理学和药理学的理解有了显著提高。例如,重组海人酸受体上的激动剂谱已被用于识别和区分神经元中的海人酸受体。此外,海人酸受体亚型选择性拮抗剂的开发增进了我们对海人酸受体在神经元和突触传递中功能作用的理解。在这篇综述中,我们描述了海人酸受体上激动剂和拮抗剂的活性以及它们在NMDA和非NMDA受体上的选择性谱。

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