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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Detalles Bibliográficos
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
Descripción
Sumario: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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