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.
Sharan K Bagal  1 ,  Mark L Chapman  2 ,  Brian E Marron  3 ,  Rebecca Prime  4 ,  R Ian Storer  5 ,  Nigel A Swain  5
Affiliations
  • 1. Worldwide Medicinal Chemistry, Pfizer Neusentis, The Portway Building, Granta Park, Great Abington, Cambridge CB21 6GS, UK. Electronic address: [email protected].
  • 2. Electrophysiology, Pfizer Neusentis, 4222 Emperor Blvd., Durham, NC, USA.
  • 3. Chemistry, Pfizer Neusentis, 4222 Emperor Blvd., Durham, NC, USA.
  • 4. Electrophysiology, Pfizer Neusentis, The Portway Building, Granta Park, Great Abington, Cambridge CB21 6GS, UK.
  • 5. Worldwide Medicinal Chemistry, Pfizer Neusentis, The Portway Building, Granta Park, Great Abington, Cambridge CB21 6GS, UK.
PMID: 25060923 DOI: 10.1016/j.bmcl.2014.06.038
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.
Products