Gielen Marc
Laboratoire de neurobiologie, Ecole normale supérieure, CNRS, 46, rue d'Ulm, 75005 Paris, France.
Med Sci (Paris). 2010 Jan;26(1):65-72. doi: 10.1051/medsci/201026165.
In the brain of vertebrates, glutamate receptor ion channels (iGluR) mediate fast neurotransmission at excitatory synapses. They exist as distinct subfamilies (AMPA, Kainate and NMDA) differing in their functional properties. Yet, all iGluR are tetramers sharing a common molecular architecture, and a common scheme applies for the general mechanisms of their activation, which are discussed in this review. The dissection of the molecular mechanisms responsible for the operation of iGluR explain how they match their physiological requirements and paves the way to new strategies for pharmacological regulations of these receptors. This could prove useful for the discovery of drugs of therapeutic interest, such as cognitive enhancers, pain killers or anti-psychotics.
在脊椎动物的大脑中,谷氨酸受体离子通道(iGluR)在兴奋性突触处介导快速神经传递。它们以不同的亚家族形式存在(AMPA、海人藻酸和NMDA),功能特性各异。然而,所有的iGluR都是具有共同分子结构的四聚体,并且一种通用模式适用于其激活的一般机制,本综述将对此进行讨论。对负责iGluR运作的分子机制的剖析解释了它们如何满足其生理需求,并为这些受体的药理学调控新策略铺平了道路。这可能对发现具有治疗价值的药物有用,如认知增强剂、止痛药或抗精神病药物。