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.
高效的选择性TRPM8通道阻断剂。在体外阻断感冒药和丝虫蛋白诱导的TRPM8激活（IC50值分别为7.8和26.9 nM）。在其他TRP通道（IC50>20μM）上无影响。在体内降低体温。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.
C2316272
危险品化学品经营许可证（带存储）