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

Hugo   R.   Arias; Michael   P.   Blanton

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

Keywords: local anesthetic, open-channel-blocking mechanism, nicotinic acetylcholine receptor, achrs membrane

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Mini-Reviews in Medicinal Chemistry

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

Volume: 2 Issue: 4

Author(s): Hugo R. Arias and Michael P. Blanton

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Keywords: local anesthetic, open-channel-blocking mechanism, nicotinic acetylcholine receptor, achrs membrane

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

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Arias R. Hugo and Blanton P. Michael, Molecular and Physicochemical Aspects of Local Anesthetics Acting on Nicotinic Acetylcholine Receptor-containing Membranes, Mini-Reviews in Medicinal Chemistry 2002; 2 (4) . https://dx.doi.org/10.2174/1389557023406025