Application

M8-B hydrochloride has been used as a transient receptor potential melastatin-8 (TRPM8) channel antagonist to study its therapeutic efficiency on a mouse model of severe dry eye disease (DED) induced by the excision of extra-orbital lacrimal and Harderian glands.

Biochem/physiol Actions

M8-B is a selective and potent antagonist of the transient receptor potential melastatin-8 (TRPM8) channel. M8-B blocked cold-induced and icilin or methol-induced activation of rat, human, and murine TRPM8 channels with IC₅₀ values in rat ranging from 7.8 nM to 64.3 nM, and it did not block other TRP channels (IC₅₀ values > 20 mM). M8-B decreased deep body temperature in both mice and rats, showing that blockade of TRPM8 receptor might be used to induce therapeutic hypothermia, an effective treatment in cardiac arrest.

Features and Benefits

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Packaging

5, 25 mg in glass bottle