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. 2013 Dec 17;170(8):1607–1651. doi: 10.1111/bph.12447
Nomenclature HGNC, UniProt Other chemical activators Physical activators Activators (EC50) Channel Blockers (IC50) Functional characteristics Comment
TRPM8 TRPM8, Q7Z2W7 agonist activities are temperature dependent and potentiated by cooling depolarization (V½ ∼ +50 mV at 15°C), cooling (< 22–26°C) icilin (requires intracellular Ca2+ as a co-factor for full agonist activity), (-)-menthol (inhibited by intracellular Ca2+), WS-12 2-APB, 5-benzyloxytryptamine, ACAA, AMTB 286, anandamide, BCTC, cannabidiol, capsazepine, clotrimazole, Δ9-tetrahydrocannabinol, La3+, linoleic acid, NADA γ = 40-83 pS at positive potentials; conducts mono- and di-valent cations non-selectively (PCa/PNa = 1.0–3.3); pronounced outward rectification; demonstrates densensitization to chemical agonists and adaptation to a cold stimulus in the presence of Ca2+; modulated by lysophospholipids and PUFAs cannabidiol and Δ9-tetrahydrocannabinol are examples of cannabinoids. TRPM8 is insensitive to ruthenium red