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