Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives

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(v)2.2 channel is a validated target for the treatment of refractor...

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Autores principales: Gleeson, Ellen C., Graham, Janease E., Spiller, Sandro, Vetter, Irina, Lewis, Richard J., Duggan, Peter J., Tuck, Kellie L.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2015
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4413198/
https://www.ncbi.nlm.nih.gov/pubmed/25871286
http://dx.doi.org/10.3390/md13042030
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author Gleeson, Ellen C.
Graham, Janease E.
Spiller, Sandro
Vetter, Irina
Lewis, Richard J.
Duggan, Peter J.
Tuck, Kellie L.
author_facet Gleeson, Ellen C.
Graham, Janease E.
Spiller, Sandro
Vetter, Irina
Lewis, Richard J.
Duggan, Peter J.
Tuck, Kellie L.
author_sort Gleeson, Ellen C.
collection PubMed
description 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(v)2.2 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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spelling pubmed-44131982015-05-07 Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives Gleeson, Ellen C. Graham, Janease E. Spiller, Sandro Vetter, Irina Lewis, Richard J. Duggan, Peter J. Tuck, Kellie L. Mar Drugs Article 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(v)2.2 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. MDPI 2015-04-13 /pmc/articles/PMC4413198/ /pubmed/25871286 http://dx.doi.org/10.3390/md13042030 Text en © 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/).
spellingShingle Article
Gleeson, Ellen C.
Graham, Janease E.
Spiller, Sandro
Vetter, Irina
Lewis, Richard J.
Duggan, Peter J.
Tuck, Kellie L.
Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives
title Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives
title_full Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives
title_fullStr Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives
title_full_unstemmed Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives
title_short Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives
title_sort inhibition of n-type calcium channels by fluorophenoxyanilide derivatives
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4413198/
https://www.ncbi.nlm.nih.gov/pubmed/25871286
http://dx.doi.org/10.3390/md13042030
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