A diterpenoid with TRPC6 inhibitory and analgesic activities
Larixyl acetate is a diterpenoid that has been found in Larix and has transient receptor potential canonical 6 (TRPC6) inhibitory and analgesic activities.1,2 It inhibits the activity of TRPC6 (IC50 = 0.58 µM) and is selective for TRPC6 over TRPC3 (IC50 = 6.83 µM), as well as over nine additional TRP channels at 10 µM.1 Intrathecal administration of larixyl acetate reduces mechanical and cold allodynia in a rat model of neuropathic pain induced by spared nerve injury (SNI).
1.Urban, N., Wang, L., Kwiek, S., et al.Identification and validation of larixyl acetate as a potent TRPC6 inhibitorMol. Pharmacol.89(1)197-213(2016) 2.Wang, J., Zhao, M., Jia, P., et al.The analgesic action of larixyl acetate, a potent TRPC6 inhibitor, in rat neuropathic pain model induced by spared nerve injuryJ. Neuroinflammation17(1)118(2020)
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