Related Experiment Video

Updated: Jul 8, 2026

Cell-based Calcium Assay for Medium to High Throughput Screening of TRP Channel Functions using FlexStation 3
07:26

Cell-based Calcium Assay for Medium to High Throughput Screening of TRP Channel Functions using FlexStation 3

Published on: August 17, 2011

Activation of TRPA1 by farnesyl thiosalicylic acid

Michael Maher1, Hong Ao, Tue Banke

  • 1Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.

Molecular Pharmacology
|January 4, 2008
PubMed

Insights

Researchers identified novel potent and selective agonists for the TRPA1 channel, a key pain mediator. Farnesyl thiosalicylic acid shows a potentially unique mechanism, offering new avenues for pain research.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • The Transient Receptor Potential Ankyrin 1 (TRPA1) channel is implicated in pain signaling.
  • Existing TRPA1 activators often lack potency, selectivity, or are reactive, limiting their therapeutic potential.

Purpose of the Study:

  • To discover novel compounds with potent and selective TRPA1-activating properties.
  • To investigate the mechanism of action of newly identified TRPA1 agonists.

Main Methods:

  • Calcium fluorescent assays
  • Whole-cell electrophysiology
  • Patch-clamp recordings on excised patches
  • Site-directed mutagenesis (quadruple TRPA1 mutant)

Main Results:

  • Identified several potent and selective TRPA1 agonists, including lipid compounds (e.g., farnesyl thiosalicylic acid) and marketed drugs (disulfiram, chlordantoin).
  • Farnesyl thiosalicylic acid activates TRPA1 in excised patches and independently of calcium.
  • Demonstrated that farnesyl thiosalicylic acid's mechanism differs from reactive agonists like allylisothiocyanate.

Conclusions:

  • Novel TRPA1 agonists, including farnesyl thiosalicylic acid, have been identified.
  • Farnesyl thiosalicylic acid presents a potentially novel mechanism of action for TRPA1 activation.
  • These findings offer new tools for studying TRPA1 channel function and developing analgesics.

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