AMG333 (AMG-333) is a potent, highly selective TRPM8 antagonist with IC50 of 13 nM and 20 nM for hTRPM8 and rTRPM8, respectively.
AMG333 displays high selectivity over other TRP channels (IC50>20 uM, TRPV1/V3/V4/A1).
AMG333 exhibits statistically significant and dose-dependent prevention of icilin-induced rat WDS, at 0.6, 1 and 3 mg/kg, inhibits cold-induced increase in blood pressure in the rat CPT in a dose-dependent manner with 1 and 3 mg/kg producing significant inhibition with an ED90 of 1.1 mg/kg, also fully blocks the cold pressor response at 3 mg/kg.
