The transient receptor potential ankyrin 1 (TRPA1) ion channel integrates the nociception and transmission of diverse potentially damaging and noxious stimuli, including cold, electrophilic compounds, divalent cations, and mechanical stimulation. A-967079 is a potent, selective, and bioavailable inhibitor of the TRPA1 channel, with IC50 values of 67 and 289 nM for the human and rat isoforms, respectively. It attenuates cold allodynia following nerve injury without producing locomotor or cardiovascular side effects. A-967079 also suppresses neuronal activity in response to mechanical stimulation and diminishes postoperative pain due to mechanical stimuli.
