The Molecular Interaction Between Local Anesthetic/Antiarrhythmic Agents and Voltage-Gated Sodium Channels

1998 ◽  
Vol 8 (2) ◽  
pp. 83-88
Author(s):  
Jeffrey R Balser
Keyword(s):  
Sodium Channels ◽  
Local Anesthetic ◽  
Molecular Interaction ◽  
Antiarrhythmic Agents ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels

scholarly journals Electrostatic Contributions of Aromatic Residues in the Local Anesthetic Receptor of Voltage-Gated Sodium Channels

2008 ◽  
Vol 102 (1) ◽  
pp. 86-94 ◽  
Author(s):  
Christopher A. Ahern ◽  
Amy L. Eastwood ◽  
Dennis A. Dougherty ◽  
Richard Horn
Keyword(s):  
Sodium Channels ◽  
Local Anesthetic ◽  
Aromatic Residues ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels

Local Anesthetic Neurotoxicity Does Not Result from Blockade of Voltage-Gated Sodium Channels

1995 ◽  
Vol 81 (2) ◽  
pp. 338-346 ◽  
Author(s):  
Shinichi Sakura ◽  
Andrew W. Bollen ◽  
Ricardo Ciriales ◽  
Kenneth Drasner
Keyword(s):  
Sodium Channels ◽  
Local Anesthetic ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels

scholarly journals Use-Dependent Block of Voltage-Gated Sodium Channels by Orphenadrine through Binding at the Local Anesthetic Receptor

2009 ◽  
Vol 96 (3) ◽  
pp. 247a
Author(s):  
Jean-François Desaphy ◽  
Antonella Dipalma ◽  
Teresa Costanza ◽  
Michela De Bellis ◽  
Alfred L. George ◽  
...  
Keyword(s):  
Sodium Channels ◽  
Local Anesthetic ◽  
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.

Local Anesthetic Neurotoxicity Does Not Result from Blockade of Voltage-Gated Sodium Channels

1995 ◽  
Vol 81 (2) ◽  
pp. 338-346 ◽  
Author(s):  
Shinichi Sakura ◽  
Andrew W. Bollen ◽  
Ricardo Ciriales ◽  
Kenneth Drasner
Keyword(s):  
Sodium Channels ◽  
Local Anesthetic ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels
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