Selective TRPM8 blocker (IC50
= 103 nM). Exhibits >100-fold selectivity for TRPM8 over a panel of receptors, ion channels and enzymes, including TRPV1 and TRPA1 ion channels. Reduces body temperature in rats and reverses cold-induced bladder capacity reduction in guinea pigs. Orally bioavailable.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Sold for research purposes under agreement from Pfizer Inc
Discovery of a selective TRPM8 antagonist with clinical efficacy in cold-related pain.
Andrews et al.
ACS Med.Chem.Lett., 2015;6:419
Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans.
Winchester et al.