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

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5 Citations (Scopus)

Abstract

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
Volume13
Issue number4
DOIs
Publication statusPublished - 2015

Keywords

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

Cite this

Gleeson, E., Graham, J. E., Spiller, S., Vetter, I., Lewis, R. J., Duggan, P. J., & Tuck, K. L. (2015). Inhibition of N-type calcium channels by fluorophenoxyanilide derivatives. Marine Drugs, 13(4), 2030-2045. https://doi.org/10.3390/md13042030