Cardiac Na+ channels as therapeutic targets for antiarrhythmic agents

I. W. Glaaser, C. E. Clancy

Research output: Chapter in Book/Report/Conference proceedingChapter


There are many factors that influence drug block of voltage-gated Na+ channels (VGSC). Pharmacological agents vary in conformation, charge, and affinity. Different drugs have variable affinities to VGSC isoforms, and drug efficacy is affected by implicit tissue properties such as resting potential, action potential morphology, and action potential frequency. The presence of polymorphisms and mutations in the drug target can also influence drug outcomes. While VGSCs have been therapeutic targets in the management of cardiac arrhythmias, their potential has been largely overshadowed by toxic side effects. Nonetheless, many VGSC blockers exhibit inherent voltage- and use-dependent properties of channel block that have recently proven useful for the diagnosis and treatment of genetic arrhythmias that arise from defects in Na+ channels and can underlie idiopathic clinical syndromes. These defective channels suggest themselves as prime targets of disease and perhaps even mutation specific pharmacological interventions.

Original languageEnglish (US)
Title of host publicationBasis and Treatment of Cardiac Arrhythmias
PublisherSpringer Science and Business Media, LLC
Number of pages23
ISBN (Print)9783540249672
StatePublished - 2006
Externally publishedYes

Publication series

NameHandbook of Experimental Pharmacology
ISSN (Print)0171-2004
ISSN (Electronic)1865-0325


  • Antiarrhythmic
  • Brugada Syndrome
  • CAST
  • Channelopathies
  • Conduction disorders
  • CYP
  • Cytochrome enzymes
  • Flecainide
  • Isoform specificity
  • Lidocaine
  • Local anesthetic
  • Long-QT Syndrome
  • Molecular determinants
  • Mutation
  • Pharmacodynamics
  • Pharmacokinetics
  • Polymorphism
  • Proarrhythmic
  • Recovery from block
  • SCN1A
  • SCN5A
  • Sicilian Gambit
  • Singh-Vaughan Williams
  • Structural determinants
  • Tonic block
  • TTX
  • Use-dependent block
  • VGSC

ASJC Scopus subject areas

  • Biochemistry
  • Pharmacology, Toxicology and Pharmaceutics(all)


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