期刊论文详细信息
Marine Drugs | |
Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives | |
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; Cav2.2; 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 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.
【 授权许可】
CC BY
© 2015 by the authors; licensee MDPI, Basel, Switzerland.
【 预 览 】
Files | Size | Format | View |
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RO202003190013951ZK.pdf | 480KB | download |