Potent and selective TRPM8 channel blocker. Blocks cold- and icilin
-induced TRPM8 activation in vitro
values are 7.8 and 26.9 nM respectively). Exhibits no effect at other TRP channels (IC50
> 20 μ
M). Reduces body temperature in vivo
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Pharmacological blockade of the cold receptor TRPM8 attenuates autonomic and behavioral cold defenses and decreases deep body temperature.
Almeida et al.