全麻药物敏感的GLIC配体门控离子通道研究进展

Progressing in the Studying of General Anesthetics-sensitive GLIC Ligand-gated Ion Channel

五聚体配基门控离子通道（Pentameric ligand-gated ion channels．pLGICs）在动物体内广泛表达，是神经电位传导的主要参与者之一。介导pLGICs神经传导的递质主要有乙酰胆碱（Ach）．γ－氨基丁酸（GABA）．甘氨酸，5-羟色胺。五聚体配基门控离子通道家族不同成员在生理学及麻醉学中具有重要作用，它们受临床浓度的麻醉剂调节，在全麻机制的研究中发挥重要作用。但是．由于缺乏关于哺乳动物pLGIcs的完整的X线结构方面的信息。使得全麻药物与配体门控离子通道变构调节机制和作用位点的研究进展缓慢。现已明确pLGICs家族起源于原核生物，因为有20多种家族同系物在原核生物中克隆出来。特别是最近研究发现的原核无类囊体蓝藻（Gloebacter violaceus．GLlc），通过对其X线分子结构观察，使得人们首次高分辨率的了解了pLGICs家族．也为全麻药物与配体门控离子通道变构调节机制和作用位点的研究提供了新的信息。大量研究发现GLIC具有电生理特性，受质子和阳离子的激活而发挥门控效应，同时对临床浓度的麻醉药物敏感，甚至与一些麻醉药物显示出比pLGICs家族其他受体更强的亲和力。本文旨在对全麻药物敏感的GLIC配体门控离子通道的研究进展做一综述。

Pentameric ligand-gated ion channels （pLGICs） are widely expressed in the animal kingdom and are key participates of neurotransmission activated by acetylcholine（ACh）, γ-amminobutyric acid（GABA）,glycine and serotonin . The family members of pLGICs play an important rote in physiology and anesthesiology ,but the information as X-ray structure of an integral mammalian pLGIC is still lacking ,while the mechanism of general anaesthetics ,allosteric modulators of brain pLGICs, and their binding sites are all poorly understood ,It is now established that this family has a prokaryotic origin,since more than 20 homologues have been discovered in bacteria. In particular ,the bacterial homologue from GIoeobacter violaceus （GUC）,whose X-ray structure was recently solved, making the first high-resolution understanding of the pLGICs family .GLIC displays a ligand-gated ion channel function and is also sensitive to clinical concentrations of general anaesthetics, and even have more affinity than other family members.The progressing on the studying of general anestheticssensitive GLIC ligand-gated ion channel is reviewed in this paper.