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. and Tuck, Kellie L. (2015) Inhibition of N-type calcium channels by fluorophenoxyanilide derivatives. Marine Drugs, 13 4: 2030-2045. doi:10.3390/md13042030

Author Gleeson, Ellen C.
Graham, Janease E.
Spiller, Sandro
Vetter, Irina
Lewis, Richard J.
Duggan, Peter J.
Tuck, Kellie L.
Title Inhibition of N-type calcium channels by fluorophenoxyanilide derivatives
Journal name Marine Drugs   Check publisher's open access policy
ISSN 1660-3397
Publication date 2015-04-01
Sub-type Article (original research)
DOI 10.3390/md13042030
Open Access Status DOI
Volume 13
Issue 4
Start page 2030
End page 2045
Total pages 16
Place of publication Basel, Switzerland
Publisher MDPI AG
Collection year 2016
Language eng
Formatted 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.
Keyword Cav2.2
Channel blocker
N-type calcium channel
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2016 Collection
Institute for Molecular Bioscience - Publications
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