NDLI: Molecular determinants of drug access to the receptor site for antiarrhythmic drugs in the cardiac Na+ channel.

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Molecular determinants of drug access to the receptor site for antiarrhythmic drugs in the cardiac Na+ channel.

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Molecular determinants of drug access to the receptor site for antiarrhythmic drugs in the cardiac Na+ channel.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Qu, Y. Scheuer, T. Rogers, J. Catterall, W. A. Tanada, T.
Description	Author Affiliation: Qu Y ( Department of Pharmacology, University of Washington, Seattle 98195-7280, USA.);
Abstract	The clinical efficacy of local anesthetic and antiarrhythmic drugs is due to their voltage- and frequency-dependent block of Na+ channels. Quaternary local anesthetic analogs such as QX-314, which are permanently charged and membrane-impermeant, effectively block cardiac Na+ channels when applied from either side of the membrane but block neuronal Na+ channels only from the intracellular side. This difference in extracellular access to QX-314 is retained when rat brain rIIA Na+ channel alpha subunits and rat heart rH1 Na+ channel alpha subunits are expressed transiently in tsA-201 cells. Amino acid residues in transmembrane segment S6 of homologous domain IV (IVS6) of Na+ channel alpha subunits have important effects on block by local anesthetic drugs. Although five amino acid residues in IVS6 differ between brain rIIA and cardiac rH1, exchange of these amino acid residues by site-directed mutagenesis showed that only conversion of Thr-1755 in rH1 to Val as in rIIA was sufficient to reduce the rate and extent of block by extracellular QX-314 and slow the escape of drug from closed channels after use-dependent block. Tetrodotoxin also reduced the rate of block by extracellular QX-314 and slowed escape of bound QX-314 via the extracellular pathway in rH1, indicating that QX-314 must move through the pore to escape. QX-314 binding was inhibited by mutation of Phe-1762 in the local anesthetic receptor site of rH1 to Ala whether the drug was applied extracellularly or intracellularly. Thus, QX-314 binds to a single site in the rH1 Na+ channel alpha subunit that contains Phe-1762, whether it is applied from the extracellular or intracellular side of the membrane. Access to that site from the extracellular side of the pore is determined by the amino acid at position 1755 in the rH1 cardiac Na+ channel.
ISSN	00278424
e-ISSN	10916490
Journal	Proceedings of the National Academy of Sciences of the United States of America
Issue Number	25
Volume Number	92
Language	English
Publisher	National Academy of Sciences
Publisher Date	1995-01-01
Publisher Place	United States
Access Restriction	Open
Subject Keyword	Anesthetics, Local Pharmacology Anti-Arrhythmia Agents Lidocaine Analogs & Derivatives Myocardium Chemistry Sodium Channels Drug Effects Amino Acid Sequence Animals Binding Sites Brain Chemistry Electric Conductivity Electrophysiology Molecular Sequence Data Mutagenesis, Site-Directed Oocytes Protein Conformation Recombinant Proteins Sodium Channel Blockers Genetics Structure-Activity Relationship Transfection Xenopus Comparative Study Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, P.H.S. Multidisciplinary
Content Type	Text
Resource Type	Article
Subject	Multidisciplinary

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