Channelpedia

PubMed 25871286


Referenced in Channelpedia wiki pages of: none

Automatically associated channels: Cav2.2



Title: Inhibition of N-type calcium channels by fluorophenoxyanilide derivatives.

Authors: Ellen C Gleeson, Janease E Graham, Sandro Spiller, Irina Vetter, Richard J Lewis, Peter J Duggan, Kellie L Tuck

Journal, date & volume: Mar Drugs, 2015 Apr , 13, 2030-45

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/25871286


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.