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

doi:10.3390/md13042030

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

School of Chemistry

Research output: Contribution to journal › Article › Research › peer-review

12 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 language	English
Pages (from-to)	2030-2045
Number of pages	16
Journal	Marine Drugs
Volume	13
Issue number	4
DOIs	https://doi.org/10.3390/md13042030
Publication status	Published - 2015

Keywords

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

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10.3390/md13042030Licence: CC BY

3582834-oaFinal published version, 481 KBLicence: CC BY

Cite this

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AU - Vetter, Irina

AU - Lewis, Richard J

AU - Duggan, Peter J

AU - Tuck, Kellie Louise

PY - 2015

Y1 - 2015

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AB - 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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KW - pain

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JO - Marine Drugs

JF - Marine Drugs

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Inhibition of N-type calcium channels by fluorophenoxyanilide derivatives

Abstract

Keywords

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