Neuronal Nicotinic Acetylcholine Receptor Structure and Function and Response to Nicotine.
Neuronal Nicotinic Acetylcholine Receptor Structure and Function and Response to Nicotine.
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DOI：
10.1016/bs.irn.2015.07.001
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发表时间：
2015
影响因子：
--
通讯作者：
Dani JA
中科院分区：
文献类型：
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作者：
Dani JA
烟碱乙酰胆碱受体（nAChR）属于配体门控离子通道的“Cys环”超家族，其包括GABAA、甘氨酸和5-羟色胺（5-HT 3）受体。哺乳动物nAChR有16个同源亚基，由一个多基因家族编码。这些亚基联合收割机形成许多不同的nAChR亚型，具有不同的表达模式、不同的功能特性和不同的药理学特征。由于胆碱能神经支配普遍存在，并且nAChR表达极其广泛，因此几乎大脑的每个区域都受到尼古丁机制的影响。本文简要介绍了受体/通道复合物本身的结构和功能特性。综述还总结了从烟草中获得的低尼古丁浓度的激活和脱敏nAChRs。对通道浇口的三维结构和结构特征的认识已达到高级阶段。同样，通道的基本功能特性也得到了合理的理解。正是这些受体/通道特性构成了nAChR参与哺乳动物大脑几乎每个解剖区域的基础。
Nicotinic acetylcholine receptors (nAChRs) belong to the “Cys-loop” superfamily of ligand-gated ion channels that includes GABAA, glycine, and serotonin (5-HT3) receptors. There are 16 homologous mammalian nAChR subunits encoded by a multigene family. These subunits combine to form many different nAChR subtypes with various expression patterns, diverse functional properties, and differing pharmacological characteristics. Because cholinergic innervation is pervasive and nAChR expression is extremely broad, practically every area of the brain is impinged upon by nicotinic mechanisms. This review briefly examines the structural and functional properties of the receptor/channel complex itself. The review also summarizes activation and desensitization of nAChRs by the low nicotine concentrations obtained from tobacco. Knowledge of the three-dimensional structure and the structural characteristics of channel gating has reached an advanced stage. Likewise, the basic functional properties of the channel also are reasonably well understood. It is these receptor/channel properties that underlie the participation of nAChRs in nearly every anatomical region of the mammalian brain.