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. TCS 5861528 is a selective TRPA1 blocker that antagonizes TRPA1-mediated calcium influx induced by allyl isothiocyanate and 4-hydroxy nonenal with IC50 values of 14.3 and 18.7 μM, respectively. At 30 mg/kg twice daily in rats, TCS 5861528 has been used to attenuate pain-related behavior in models of diabetic hypersensitivity and postoperative pain.
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