Molecular and Physicochemical Aspects of Local Anesthetics Acting on Nicotinic Acetylcholine Receptor-containing Membranes

Local anesthetics inhibit the ion channel activity of nicotinic acetylcholine receptors in a noncompetitive fashion. This inhibitory action is ascribed to two possible inhibitory mechanisms: an openchannel- blocking mechanism and / or an allosteric process where the drug binds either to the closed channel or to other nonluminal sites, respectively.