Recent progress in sodium channel modulators for pain

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3690-9. doi: 10.1016/j.bmcl.2014.06.038. Epub 2014 Jun 21.

Abstract

Voltage-gated sodium channels (Navs) are an important family of transmembrane ion channel proteins and Nav drug discovery is an exciting field. Pharmaceutical investment in Navs for pain therapeutics has expanded exponentially due to genetic data such as SCN10A mutations and an improved ability to establish an effective screen sequence for example IonWorks Barracuda®, Synchropatch® and Qube®. Moreover, emerging clinical data (AZD-3161, XEN402, CNV1014802, PF-05089771, PF-04531083) combined with recent breakthroughs in Nav structural biology pave the way for a future of fruitful prospective Nav drug discovery.

Keywords: Electrophysiology screening; Sodium channel drugs; Sodium channel structure; Sodium channel toxins; Voltage-gated sodium channels.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Discovery
  • Humans
  • Pain / drug therapy*
  • Sodium Channel Blockers / chemistry
  • Sodium Channel Blockers / pharmacology*
  • Sodium Channel Blockers / therapeutic use*
  • Voltage-Gated Sodium Channels / chemistry
  • Voltage-Gated Sodium Channels / metabolism*

Substances

  • Sodium Channel Blockers
  • Voltage-Gated Sodium Channels