Barrantes F J
Instituto de Investigaciones Bioquímicas, CONICET, Bahía Blanca, Argentina.
Braz J Med Biol Res. 1993 Jun;26(6):553-71.
The nicotinic acetylcholine receptor (AChR) is still the paradigm of rapid ligand-gated ion channels. Since the early finding of a motionally restricted shell of lipids ("annulus") in the immediate perimeter of the membrane-bound AChR, experimental evidence has supported the notion that the interface between the protein moiety and the adjacent lipid molecules is the site of action of a variety of pharmacologically relevant substances, including non-competitive inhibitors of the cholinergic system like some local anesthetics, short-chain alcohols, and steroids. Patch-clamp data on cells expressing the AChR protein add another dimension to this knowledge, enabling correlations to be established between the chemical composition of lipid-modified cells and the functional properties (ligand binding, channel gating) of the receptor protein in situ.
烟碱型乙酰胆碱受体（AChR）仍是快速配体门控离子通道的范例。自早期在膜结合型AChR紧邻周边发现脂质运动受限壳层（“环带”）以来，实验证据支持了这样一种观点，即蛋白质部分与相邻脂质分子之间的界面是多种药理相关物质的作用位点，这些物质包括胆碱能系统的非竞争性抑制剂，如一些局部麻醉剂、短链醇和类固醇。关于表达AChR蛋白的细胞的膜片钳数据为这一知识增添了新的维度，使得能够在脂质修饰细胞的化学成分与原位受体蛋白的功能特性（配体结合、通道门控）之间建立关联。
