Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives

Marine Drugs

Ellen C. Gleeson¹  Janease E. Graham¹  Sandro Spiller¹  Irina Vetter³  Richard J. Lewis³  Peter J. Duggan²  Kellie L. Tuck¹ 

[1] School of Chemistry, Monash University, Clayton VIC 3800, Australia; E-Mails:;CSIRO Manufacturing Flagship, Clayton South, VIC 3169, Australia;Institute for Molecular Bioscience, The University of Queensland, St Lucia QLD 4072, Australia; E-Mails:

关键词: N-type calcium channel;    Ca_v2.2;    channel blocker;    pain;    FLIPR;   

DOI  :  10.3390/md13042030

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.