Molecular and physicochemical aspects of local anesthetics acting on nicotinic acetylcholine receptor-containing membranes

Mini Rev Med Chem. 2002 Aug;2(4):385-410. doi: 10.2174/1389557023406025.

Abstract

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 open-channel-blocking mechanism and/or an allosteric process where the drug binds either to the closed channel or to other nonluminal sites, respectively.

Publication types

  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Allosteric Regulation / drug effects
  • Anesthetics, Local / chemistry*
  • Anesthetics, Local / pharmacology
  • Animals
  • Humans
  • Ion Channels / antagonists & inhibitors*
  • Membrane Potentials / drug effects
  • Nicotinic Antagonists / chemistry
  • Nicotinic Antagonists / pharmacology
  • Receptors, Nicotinic / chemistry
  • Receptors, Nicotinic / drug effects*
  • Receptors, Nicotinic / physiology
  • Structure-Activity Relationship

Substances

  • Anesthetics, Local
  • Ion Channels
  • Nicotinic Antagonists
  • Receptors, Nicotinic