Description
WS-12 is an agonist of transient receptor potential melastatin 8 (TRPM8). It induces currents in Xenopus oocytes expressing mouse TRPM8 (EC50 = 12 μM) and is selective for TRPM8 over transient receptor potential vanilloid 1-4 (TRPV1-4) and transient receptor potential ankyrin 1 (TRPA1) at 1 mM. WS-12 (6 nmol, i.c.v.) reduces nocifensive behavior induced by capsaicin in wild-type, but not Trpm8-/-, mice. It induces analgesia in the hot plate test, an effect that can be reversed by the opioid receptor antagonist naloxone, in mice.
Chemical Properties
WS 12 is a odorless white crystalline solid,mp 178 °C, displaying
a strong initial cooling effect and a long-lastingness. It is used particularly is oral
care flavors.
Uses
WS 12 is a potent TRPM8 agonist.
Trade name
Winsense WS-12 (Renessenz)
Biological Activity
Potent TRPM8 agonist that acts as a cooling agent (EC 50 = 193 nM).
Biochem/physiol Actions
WS-12 is a menthol derivative, that shows a specific binding affinity towards TRPM8 (transient receptor potential cation channel subfamily M member 8) receptor. TRPM8 is associated with prostate cancer and thus, WS-12 might be useful in reducing the progression of cancer.
References
[1] SHERKHELI MA. Menthol derivative WS-12 selectively activates transient receptor potential melastatin-8 (TRPM8) ion channels.[J]. Pakistan journal of pharmaceutical sciences, 2008, 21 4: 370-378.
[2] BOYI LIU . TRPM8 is the principal mediator of menthol-induced analgesia of acute and inflammatory pain[J]. PAIN, 2013, 154 10: Pages 2169-2177. DOI:
10.1016/j.pain.2013.06.043
