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

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

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 2 , Issue 4 , 2002

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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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Article Details

VOLUME: 2
ISSUE: 4
Year: 2002
Page: [385 - 410]
Pages: 26
DOI: 10.2174/1389557023406025
Price: $58

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