Cryosim-3 is a water soluble, selective and potent agonist of TRPM8 (transient receptor potential melastatin 8) receptor. Cryosim-3 increases tear secretion in an animal model of dry eye disease. Also it relieves ocular discomfort in subjects diagnosed with DED without eye irritation.
Water soluble, selective and potent agonist of TRPM8 receptor
Science (New York, N.Y.), 378(6616), eadd1268-eadd1268 (2022-10-14)
The transient receptor potential melastatin 8 (TRPM8) channel is the primary molecular transducer responsible for the cool sensation elicited by menthol and cold in mammals. TRPM8 activation is controlled by cooling compounds together with the membrane lipid phosphatidylinositol 4,5-bisphosphate (PIP2).
Physical cooling of the eye surface relieves ocular discomfort, but translating this event to drug treatment of dry eye discomfort not been studied. Here, we synthesized a water-soluble TRPM8 receptor agonist called cryosim-3 (C3, 1-diisopropylphosphorylnonane) which selectively activates TRPM8 (linked