Inhibition of N-type calcium channels by fluorophenoxyanilide derivatives

Ellen Gleeson, Janease Erin Graham, Sandro Spiller, Irina Vetter, Richard J Lewis, Peter J Duggan, Kellie Louise Tuck

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)


A set of fluorophenoxyanilides, designed to be simplified analogues of previously reported ω-conotoxin GVIA mimetics, were prepared and tested for N-type calcium channel inhibition in a SH-SY5Y neuroblastoma FLIPR assay. N-type or Cav2.2 channel is a validated target for the treatment of refractory chronic pain. Despite being significantly less complex than the originally designed mimetics, up to a seven-fold improvement in activity was observed
Original languageEnglish
Pages (from-to)2030-2045
Number of pages16
JournalMarine Drugs
Issue number4
Publication statusPublished - 2015


  • N-type calcium channel
  • Cav2.2
  • channel blocker
  • pain

Cite this