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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

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

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

Volume 2, Issue 4, 2002

Page: [385 - 410] Pages: 26

DOI: 10.2174/1389557023406025

Price: $65

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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