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Etodolac blocks the allyl isothiocyanate-induced response in mouse sensory neurons by selective TRPA1 activation

Naoki Inoue1, Sunao Ito, Masaki Nogawa

  • 1Exploratory Department, Discovery Research Laboratories, Nippon Shinyaku Co., Ltd., Kyoto, Japan. n.inoue@po.nippon-shinyaku.co.jp

Pharmacology
|June 29, 2012
PubMed
Abstract

Insights

Etodolac, a nonsteroidal anti-inflammatory drug, acts as a selective agonist for the transient receptor potential cation channel, ankyrin subfamily, member 1 (TRPA1). This selective activation desensitizes nociceptors, offering potential for neuropathic pain treatment.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Pain Research

Background:

  • Nociceptor excitability is modulated by the transient receptor potential cation channel, ankyrin subfamily, member 1 (TRPA1).
  • Etodolac, a nonsteroidal anti-inflammatory drug, previously shown to attenuate neuropathic pain independently of cyclooxygenase inhibition.

Purpose of the Study:

  • To investigate the role of TRPA1 in the antinociceptive mechanism of etodolac.
  • To determine if etodolac acts as a TRPA1 agonist or antagonist.

Main Methods:

  • Measured calcium (Ca2+) influx in HEK-293 cells expressing mouse TRPA1 and in mouse dorsal root ganglion (DRG) neurons.
  • Assessed the effect of etodolac on nociceptive behavior induced by the TRPA1 agonist allyl isothiocyanate (AITC) in mice.

Main Results:

  • Etodolac induced Ca2+ influx in cells expressing TRPA1, which was blocked by a TRPA1-specific antagonist.
  • Etodolac did not induce Ca2+ influx in cells expressing TRPV1, TRPV2, or TRPM8.
  • Etodolac inhibited Ca2+ influx induced by the TRPA1 agonist AITC.

Conclusions:

  • Etodolac exhibits selective TRPA1 agonist activity.
  • Etodolac desensitizes nociceptors via selective TRPA1 activation.
  • Etodolac demonstrates potential clinical utility for treating neuropathic pain.

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