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Mar. Drugs 2015, 13(4), 2030-2045; doi:10.3390/md13042030

Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives

1
School of Chemistry, Monash University, Clayton VIC 3800, Australia
2
CSIRO Manufacturing Flagship, Clayton South, VIC 3169, Australia
3
Institute for Molecular Bioscience, The University of Queensland, St Lucia QLD 4072, Australia
4
School of Chemical and Physical Sciences, Flinders University, Adelaide SA 5042, Australia
On exchange from Fakult
*
Authors to whom correspondence should be addressed.
Academic Editor: Alejandro M. Mayer
Received: 21 February 2015 / Revised: 18 March 2015 / Accepted: 26 March 2015 / Published: 13 April 2015
(This article belongs to the Special Issue Marine Peptides and Their Mimetics)
View Full-Text   |   Download PDF [481 KB, uploaded 21 April 2015]   |  

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. View Full-Text
Keywords: N-type calcium channel; Cav2.2; channel blocker; pain; FLIPR N-type calcium channel; Cav2.2; channel blocker; pain; FLIPR
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Gleeson, E.C.; Graham, J.E.; Spiller, S.; Vetter, I.; Lewis, R.J.; Duggan, P.J.; Tuck, K.L. Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives. Mar. Drugs 2015, 13, 2030-2045.

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