Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives

Ellen Gleeson; Janease Graham; Sandro Spiller; Irina Vetter; Richard Lewis; Peter Duggan; Kellie Tuck

doi:10.3390/md13042030

Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives

Ellen Gleeson, Janease Graham, Sandro Spiller, Irina Vetter, Richard Lewis, Peter Duggan, Kellie Tuck

Research output: Contribution to journal › Article › 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 Ca_v2.2 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 - 1 Apr 2015

Keywords

Cav2.2
Channel blocker
FLIPR
N-type calcium channel
Pain

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.3390/md13042030

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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.",

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AU - Gleeson, Ellen

AU - Graham, Janease

AU - Spiller, Sandro

AU - Vetter, Irina

AU - Lewis, Richard

AU - Duggan, Peter

AU - Tuck, Kellie

PY - 2015/4/1

Y1 - 2015/4/1

N2 - 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.

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 - Channel blocker

KW - FLIPR

KW - N-type calcium channel

KW - Pain

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JO - Marine Drugs

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IS - 4

ER -

Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives

Abstract

Keywords

UN SDGs

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