A cell-permeable and selective TRPA1 antagonist that reversibly antagonizes AITC- and formalin-evoked calcium influx (IC50 = 6.2 µM and 5.3 µ M, respectively), and blocks AITC- and formalin-induced inward and outward currents in TRPA1-expressing HEK293 cells in a patch-clamp assay. It demonstrates activity towards rat and mouse TRPA1 orthologues, but does not block currents mediated by TRPV1, TRPV3, TRPV4, hERG, or NaV1.2 channels. This compound is also shown to block TRPA1 activation induced by formalin in cultured rat DRG neurons, and attenuate pain-related responses to formalin in rats (300 mg/kg, i.p.), in vivo.
Toxicity: Standard Handling (A)
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