TRPV2 channel

Channel name TRPV21,2,3,4,5,6
Description Noxious heat thermosensor channel
Other names VRL-1, GRC, OTRPC2
Molecular information Human unigene: Hs0.279746, chr. 17p11.2
Mouse unigene: Mm0.288064, chr. 11 B2
Associated subunits Not established
Functional assays Patch-clamp, calcium imaging
Current Outwardly rectifying nonselective cation current
Conductance Erev in saline solution ∼0 mV
Ion selectivity PNa/PCa = 1:3
Ca2+ > Mg2+ > Na+, K+, Cs+
Activation High temperature (>52°C), PKA modulation of surface expression
Inactivation Not established
Activators Heat (threshold = 52°C), IGF-I
Gating inhibitors None
Blockers Ruthenium red, La3+, SKF96365
Radioligands None
Channel distribution Mainly dorsal root ganglion neurons, brain, spinal cord, spleen, and lung
Physiological functions Calcium entry in thermal pain sensation
Mutations and pathophysiology Not established
Pharmacological significance Potential target for pain-relieving agents
Comments Insensitive to capsaicin
  • chr., chromosome; PKA, protein kinase A; IGF-I, insulin-like growth factor-I.

  • 1. Caterina MJ, Rosen TA, Tominaga M, Brake AJ, and Julius D (1999) A capsaicin-receptor homologue with a high threshold for noxious heat. Nature (Lond) 398:436-441

  • 2. Hu HZ, Gu Q, Wang C, Colton CK, Tang J, Kinoshita-Kawada M, Lee LY, Wood JD, and Zhu MX (2004) 2-Aminoethoxydiphenyl borate is a common activator of TRPV1, TRPV2 and TRPV3. J Biol Chem 279:35741-35748

  • 3. Muraki K, Iwata Y, Katanosaka Y, Ito T, Ohya S, Shigekawa M, and Imaizumi Y (2003) TRPV2 is a component of osmotically sensitive cation channels in murine aortic myocytes. Circ Res 93:829-838

  • 4. Stokes AJ, Shimoda LM, Koblan-Huberson M, Adra CN, and Turner H (2004) A TRPV2-PKA signaling module for transduction of physical stimuli in mast cells. J Exp Med 200:137-147

  • 5. Woodbury CJ, Zwick M, Wang S, Lawson JJ, Caterina MJ, Koltzenburg M, Albers KM, Koerber HR, and Davis BM (2004) Nociceptors lacking TRPV1 and TRPV2 have normal heat responses. J Neurosci 24:6410-6415

  • 6. Stokes AJ, Wakano C, Del Carmen KA, Koblan-Huberson M, and Turner HJ (2005) Formation of a physiological complex between TRPV2 and RGA protein promotes cell surface expression of TRPV2. J Cell Biochem 94:669-683