TRPM8 antagonist 2 is a potent and selective TRPM8 antagonist with an IC50 of 0.2 nM. TRPM8 antagonist 2 is used in the research of neuropathic pain syndromes.

TRPM8:0.2 nM

TRPM8 antagonist 2 (Compound 14) is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes. TRPM8 antagonist 2 potently inhibits menthol-induced increase in intracellular Ca2+ levels in Ca2+ fluorimetric assays in HEK293 cells stably expressing the rat isoform of TRPM8 channels (IC50, 40 nM).

TRPM8 antagonist 2 (1, 10, and 30 mg/kg, s.c.) exhibits a marked, dose-dependent antinociceptive activity, and inhibits wet-dog shakes (WDS)-like cold hypersensitivity in mice by 63% at 30 mg/kg. Moreover, TRPM8 antagonist 2 (0.1 and 1 μg, s.c.) attenuates Oxaliplatin (OXP)-induced cold allodynia in mice.