Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives
Ellen C. Gleeson, Janease E. Graham, Sandro Spiller and 4 more
Marine Drugs · 2015
doi:10.3390/md13042030 (opens in a new tab)
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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.
Abstract licence: CC BY
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