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 |
| |
| Affiliation: | 1.School of Chemistry, Monash University, Clayton VIC 3800, Australia; E-Mails: (E.C.G.); (J.E.G.); (S.S.);2.CSIRO Manufacturing Flagship, Clayton South, VIC 3169, Australia;3.Institute for Molecular Bioscience, The University of Queensland, St Lucia QLD 4072, Australia; E-Mails: (I.V.); (R.J.L.);4.School of Chemical and Physical Sciences, Flinders University, Adelaide SA 5042, Australia |
| |
| 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. |
| |
| Keywords: | N-type calcium channel Cav2.2 channel blocker pain FLIPR |
|
|
