TRPM8 Agonist

Icilin (AG-3-5) is a super-agonist of the transient receptor potential M8 (TRPM8) ion channel. Icilin activates TRPM8 in EGTA in a dose-dependent manner (EC₅₀=1.4 μM). Icilin is a "super-cooling agent" . Icilin attenuates autoimmune neuroinflammation through modulation of the T-cell response.

Acoltremon (WS-12; AR-15512) is a potent and selective TRPM8 agonist, the menthol derivative, as a cooling agent. Acoltremon shows analgesic effect, and can be used in chronic neuropathic pain research.

Vanillyl butyl ether is a major contributor to the characteristic flavor and fragrance of vanilla. Vanillyl butyl ether is one of the eco-friendly and nontoxic substances. Vanillyl butyl ether exhibits mutually inhibitory effects on mammalian TRPV1 and TRPM8 channels. Vanillyl butyl ether shows repellency activity against Tribolium castaneum, T. confusum and L. bostrychophila. Vanillyl butyl ether acts as a mild warming agent, providing a warming sensation and enhancing blood circulation.