Inhibition of N-type calcium channels by fluorophenoxyanilide derivatives

Ellen Gleeson; Janease Erin Graham; Sandro Spiller; Irina Vetter; Richard J Lewis; Peter J Duggan; Kellie Louise Tuck

doi:10.3390/md13042030

Inhibition of N-type calcium channels by fluorophenoxyanilide derivatives

Ellen Gleeson, Janease Erin Graham, Sandro Spiller, Irina Vetter, Richard J Lewis, Peter J Duggan, Kellie Louise Tuck

School of Chemistry

Research output: Contribution to journal › Article › Research › peer-review

10 Citations (Scopus)

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

Original language	English
Pages (from-to)	2030-2045
Number of pages	16
Journal	Marine Drugs
Volume	13
Issue number	4
DOIs	https://doi.org/10.3390/md13042030
Publication status	Published - 2015

Keywords

N-type calcium channel
Cav2.2
channel blocker
pain
FLIPR

Access to Document

10.3390/md13042030Licence: CC BY

3582834-oaFinal published version, 481 KBLicence: CC BY

Cite this

@article{ef5d2b644d884c319fe5b24a13b2ca7f,

title = "Inhibition of N-type calcium channels by fluorophenoxyanilide derivatives",

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",

author = "Ellen Gleeson and Graham, {Janease Erin} and Sandro Spiller and Irina Vetter and Lewis, {Richard J} and Duggan, {Peter J} and Tuck, {Kellie Louise}",

year = "2015",

doi = "10.3390/md13042030",

language = "English",

volume = "13",

pages = "2030--2045",

journal = "Marine Drugs",

issn = "1660-3397",

publisher = "MDPI AG",

number = "4",

}

TY - JOUR

T1 - Inhibition of N-type calcium channels by fluorophenoxyanilide derivatives

AU - Gleeson, Ellen

AU - Graham, Janease Erin

AU - Spiller, Sandro

AU - Vetter, Irina

AU - Lewis, Richard J

AU - Duggan, Peter J

AU - Tuck, Kellie Louise

PY - 2015

Y1 - 2015

N2 - 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

AB - 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

KW - N-type calcium channel

KW - Cav2.2

KW - channel blocker

KW - pain

KW - FLIPR

UR - http://search.proquest.com.ezproxy.lib.monash.edu.au/docview/1676104938/fulltextPDF/E2F3B2CE750842C5PQ/22?accountid=12528

U2 - 10.3390/md13042030

DO - 10.3390/md13042030

M3 - Article

SN - 1660-3397

VL - 13

SP - 2030

EP - 2045

JO - Marine Drugs

JF - Marine Drugs

IS - 4

ER -

Inhibition of N-type calcium channels by fluorophenoxyanilide derivatives

Abstract

Keywords

Access to Document

Other files and links

Cite this