Lipid effects on nicotinic acetylcholine receptor gating and kinetics: A structural-functional correlation

BARRANTES FJ

BRAZILIAN JOURNAL OF MEDICAL AND BIOLOGICAL RESEARCH

ASSOC BRAS DIVULG CIENTIFICA

Lugar: San Pablo; Año: 1993 vol. 26 p. 553 - 571

0100-879X

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.