Nashmi Raad, Lester Henry A
Division of Biology, California Institute of Technology, Pasadena, CA 91125, USA.
J Mol Neurosci. 2006;30(1-2):181-4. doi: 10.1385/JMN:30:1:181.
Nicotinic acetylcholine receptors (nAChRs) are members of the Cys-loop superfamily of pentameric ligand-gated ion channels, which include GABA (A and C), serotonin, and glycine receptors. Currently, 12 neuronal nAChR subunits have been identified (alpha2-10 and beta2-4) and are generally grouped into alpha subunits, which contain two adjacent cysteine residues essential for ACh binding, and beta subunits, which lack these residues. The majority of neuronal nAChRs fall into two categories: those that bind agonist with high affinity (nM concentrations); and those that bind with lower affinity (microM concentrations). The low-affinity receptors are presumably homomeric alpha7 receptors that are alpha-bungarotoxin sensitive, whereas alpha4beta2 nAChRs account for >90% of the high-affinity nicotinic receptors in the brain (Whiting and Lindstrom, 1986). Their physiological contributions to neurotransmission, signaling, and behavior are not completely understood. Precise mapping of subcellular and neuroanatomical localizations of neuronal nAChR subunits will help elucidate the physiological role of neuronal nAChRs and their role in nicotine addiction.
烟碱型乙酰胆碱受体(nAChRs)是五聚体配体门控离子通道的半胱氨酸环超家族成员,该超家族还包括GABA(A和C)、5-羟色胺和甘氨酸受体。目前,已鉴定出12种神经元nAChR亚基(α2 - 10和β2 - 4),通常分为α亚基和β亚基,α亚基含有两个对乙酰胆碱结合至关重要的相邻半胱氨酸残基,而β亚基则缺乏这些残基。大多数神经元nAChRs可分为两类:一类以高亲和力(纳摩尔浓度)结合激动剂;另一类以较低亲和力(微摩尔浓度)结合。低亲和力受体可能是对α - 银环蛇毒素敏感的同聚体α7受体,而α4β2 nAChRs占大脑中高亲和力烟碱型受体的90%以上(怀廷和林德斯特伦,1986年)。它们对神经传递、信号传导和行为的生理作用尚未完全了解。对神经元nAChR亚基的亚细胞和神经解剖定位进行精确映射,将有助于阐明神经元nAChRs的生理作用及其在尼古丁成瘾中的作用。