Marine Drugs (Apr 2015)

Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives

  • Ellen C. Gleeson,
  • Janease E. Graham,
  • Sandro Spiller,
  • Irina Vetter,
  • Richard J. Lewis,
  • Peter J. Duggan,
  • Kellie L. Tuck

DOI
https://doi.org/10.3390/md13042030
Journal volume & issue
Vol. 13, no. 4
pp. 2030 – 2045

Abstract

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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.

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