Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain

Jun Liang, Richard M. Brochu, Charles J. Cohen, Ivy E. Dick, John P. Felix, Michael H. Fisher, Maria L. Garcia, Gregory J. Kaczorowski, Kathryn A. Lyons, Peter T. Meinke, Birgit T. Priest, William A. Schmalhofer, McHardy M. Smith, Jason W. Tarpley, Brande S. Williams, William J. Martin, William H. Parsons

Research output: Contribution to journalArticlepeer-review

Abstract

A new series of voltage-gated sodium channel blockers with potential for treatment of chronic pain is reported. Systematic structure-activity relationship studies, starting with compound 1, led to identification of potent analogs that displayed use-dependent block of sodium channels, were efficacious in pain models in vivo, and most importantly, were devoid of activity against the cardiac potassium channel hERG.

Original languageEnglish (US)
Pages (from-to)2943-2947
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number11
DOIs
StatePublished - Jun 2 2005
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Fingerprint

Dive into the research topics of 'Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain'. Together they form a unique fingerprint.

Cite this