THE MOLECULAR PHARMACOLOGY OF TOXINS THAT MODIFY VOLTAGE-GATED SODIUM CHANNELS

1989 ◽  
pp. 43-53
Author(s):  
G.R. Strichartz
Keyword(s):  
Sodium Channels ◽  
Molecular Pharmacology ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels

Ketamine Blockade of Voltage-gated Sodium Channels

2001 ◽  
Vol 95 (6) ◽  
pp. 1406-1413 ◽  
Author(s):  
Larry E. Wagner ◽  
Kevin J. Gingrich ◽  
John C. Kulli ◽  
Jay Yang
Keyword(s):  
Binding Site ◽  
Sodium Channels ◽  
Local Anesthetic ◽  
Molecular Pharmacology ◽  
Wild Type ◽  
General Anesthetic ◽  
Voltage Gated ◽  
Aspartate Receptor ◽  
Voltage Gated Sodium Channels ◽  
Steady State Inactivation

Background The general anesthetic ketamine is known to be an N-methyl-D-aspartate receptor blocker. Although ketamine also blocks voltage-gated sodium channels in a local anesthetic-like fashion, little information exists on the molecular pharmacology of this interaction. We measured the effects of ketamine on sodium channels. Methods Wild-type and mutant (F1579A) recombinant rat skeletal muscle sodium channels were expressed in Xenopus oocytes. The F1579A amino acid substitution site is part of the intrapore local anesthetic receptor. The effect of ketamine was measured in oocytes expressing wild-type or mutant sodium channels using two-electrode voltage clamp. Results Ketamine blocked sodium channels in a local anesthetic-like fashion, exhibiting tonic blockade (concentration for half-maximal inhibition [IC50] = 0.8 mm), phasic blockade (IC50 = 2.3 mm), and leftward shift of the steady-state inactivation; the parameters of these actions were strongly modified by alteration of the intrapore local anesthetic binding site (IC50 = 2.1 mm and IC50 = 10.3 mm for tonic and phasic blockade, respectively). Compared with lidocaine, ketamine showed greater tonic inhibition but less phasic blockade. Conclusions Ketamine interacts with sodium channels in a local anesthetic-like fashion, including sharing a binding site with commonly used clinical local anesthetics.

scholarly journals Erratum to: Voltage-gated Sodium Channels and Blockers: An Overview and Where Will They Go?

2020 ◽  
Author(s):  
Zhi-mei Li ◽  
Li-xia Chen ◽  
Hua Li
Keyword(s):  
Open Access ◽  
Sodium Channels ◽  
Voltage Gated ◽  
Internet Portal ◽  
Creative Commons ◽  
Link Type ◽  
Voltage Gated Sodium Channels

The article “Voltage-gated Sodium Channels and Blockers: An Overview and Where Will They Go?”, written by Zhi-mei LI, Li-xia CHEN, Hua LI, was originally published electronically on the publisher’s internet portal on December 2019 without open access. With the author(s)’ decision to opt for Open Choice, the copyright of the article is changed to © The Author(s) 2020 and the article is forthwith distributed under a Creative Commons Attribution 4.0 International License (https://creativecommons.org/licenses/by/4.0/), which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made.The original article has been corrected.Corresponding authors: Li-xia CHEN, Hua LI

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