Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors

Hugo R. Arias, Pankaj Bhumireddy

Research output: Contribution to journalReview articlepeer-review

14 Scopus citations


The nicotinic acetylcholine receptor (AChR) is the archetype of the Cys-loop ligand-gated ion channel'receptor superfamily. Noncompetitive antagonists inhibit the AChR without interacting directly with agonist sites. Among non-competitive antagonists, general and local anesthetics have been used for decades to study the structure and function of muscle- as well as neurorial-type AChRs. In this review, we address and update all information regarding the characterization of binding sites and the mechanism of action for n-alkanols, barbiturates, inhalational and dissociative general anesthetics, as well as for tertiary and quaternary local anesthetics. The experimental evidence outlined in this review suggest that: (1) several neuronal-type AChRs might be targets for the pharmacological action of distinct anesthetics; (2) the molecular components of a specific anesthetic locus on a certain receptor type are different from the structural determinants of the site for the same anesthetic on a different receptor type; (3) there are unique binding sites for distinct anesthetics in the same receptor; (4) the affinity of a specific anesthetic depends on the AChR conformational state; (5) anesthetics may inhibit AChRs by different mechanisms including open-channel-blocking, augmenting the desensitization process, and/or inactivating the opening of resting receptors; and (6) some anesthetics may potentiate AChR activity.

Original languageEnglish
Pages (from-to)451-472
Number of pages22
JournalCurrent Protein and Peptide Science
Issue number5
StatePublished - 1 Oct 2005
Externally publishedYes


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