Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives

Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives Gleeson, Ellen C; Graham, Janease E; Spiller, Sandro; Vetter, Irina; Lewis, Richard J; Duggan, Peter; Tuck, Kellie L 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. © 2015 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/).