Biological Activity
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].
References
[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.
