Background:

WS 3 is an agonist of TRPM8 receptor with EC50 value of 3.7 μM [1].

Transient receptor potential cation channel subfamily M member 8 (TRPM8) is a Ca2+- and Na+-permeable ion channel and is activated by cooling agents and cold temperatures. TRPM8 belongs to TRP family and is expressed in sensory neurons.

WS 3 is an agonist of TRPM8 receptor and a cooling agent. In HEK293 cells expressed recombinant mouse TRPM8, WS 3 (30 μM) increased [Ca2+]i. WS 3 exhibited potency with EC50 value of 3.7 μM and induced 86% efficacy of the maximal response to icilin, the most potent agonist [1]. In HEK cells stably expressing either hTRPM8 or hTRPA1, WS 3 activated hTRPM8 and hTRPA1 with EC50 values of 2.2 and 120.6 μM, respectively. WS 3 was efficacious in eliciting cooling sensation [2].

参考文献:
[1].  Behrendt HJ, Germann T, Gillen C, et al. Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay. Br J Pharmacol, 2004, 141(4): 737-745.
[2].  Klein AH, Iodi Carstens M, McCluskey TS, et al. Novel menthol-derived cooling compounds activate primary and second-order trigeminal sensory neurons and modulate lingual thermosensitivity. Chem Senses, 2011, 36(7): 649-658.