TABLE 1

Known compounds targeting TRPV3 channels

CompoundActivateInhibitDescription/UseReference
2-APBTRPV1/TRPV2/TRPV3/TRPV6TRPC6/TRPM8Inhibitor of store-operated Ca2+ influx and IP3-mediated Ca2+ release; common regulator of TRP channelsChung et al., 2004; Hu et al., 2004
CamphorTRPV1/TRPV3TRPA1Modulate sensations of warmth in humansMoqrich et al., 2005; Xu et al., 2005
MentholTRPV3/TRPM8/TRPA1TRPA1Cooling effect; modulation of warm sensationMacpherson et al., 2006
CinnamaldehydeTRPV3/TRPA1TRPM8Used as a spiceMacpherson et al., 2006
CarvacrolTRPV3/TRPA1Rapidly desensitizes TRPA1; present in oregano, which is used as a spiceXu et al., 2006
EugenolTRPV3/TRPA1Present in clove, which is used as a spice; lingual irritation; innocuous warmth and pain in response to heatSchöll and Jensen-Jarolim, 2004; Xu et al., 2006
ThymolTRPV3/TRPA1/TRPM8Derived from thyme, which is used as a spiceXu et al., 2006
Incensole acetateTRPV3A novel anxiolytic and antidepressive agentMoussaieff et al., 2008
FPP TRPV3First identified endogenous TRPV3 activator; causes nociceptionBang et al., 2010
IPPTRPV3/TRPA1Endogenous inhibitor; a precursor molecule for FPP synthesis in the mevalonate pathwayBang et al., 2011
DrofenineTRPV3Antispasmodic agent; 2-APB analog; improved selectivity for TRPV3Deering-Rice et al., 2014
DPBATRPV1/TRPV2/TRPV3/TRPV42-APB structural analogsChung et al., 2005
DPTHFTRPV1/TRPV2/ TRPV32-APB structural analogsChung et al., 2005
Nicotinic acidTRPV1/TRPV3TRPV2/TRPV4Used to treat dyslipidemias but causes a side effect of cutaneous vasodilation, commonly called flushingMa et al., 2015
17R-RvD1TRPV3Proresolving lipidBang et al., 2012
IcilinTRPM8TRPV3Super cooling agentSherkheli et al., 2012
  • DPBA, diphenylboronic anhydride; DPTHF, diphenyltetrahydrofuran; FPP, farnesyl pyrophosphate; IP3, inositol trisphosphate; IPP, isopentenyl pyrophosphate.