A-967079 (A 967079) is a potent, selective TRPA1 channel blocker with IC50 of 51 nM and 101 nM for hTRPA1 and rTRPA1, respectively.
A-967079 displays >1,000-fold selective over other TRP channels, and is >150-fold selective over 75 other ion channels, enzymes, and G-protein-coupled receptors.
A-967079 exhibits analgesic efficacy in allyl isothiocyanate-induced nocifensive response and osteoarthritic pain in rats (ED50=23.2 mg/kg), attenuates cold allodynia produced by nerve injury but does not alter noxious cold sensation in naive animals.
A-967079 is orally bioavailable.
