Trpv1

Domain

The association domain (AD) is necessary for self-association.

Function

Ligand-activated non-selective calcium permeant cation channel involved in detection of noxious chemical and thermal stimuli (PubMed:15194687, PubMed:15489017). Seems to mediate proton influx and may be involved in intracellular acidosis in nociceptive neurons. Involved in mediation of inflammatory pain and hyperalgesia (PubMed:10764638). Sensitized by a phosphatidylinositol second messenger system activated by receptor tyrosine kinases, which involves PKC isozymes and PCL. Activation by vanilloids, like capsaicin, and temperatures higher than 42 degrees Celsius, exhibits a time- and Ca(2+)-dependent outward rectification, followed by a long-lasting refractory state. Mild extracellular acidic pH (6.5) potentiates channel activation by noxious heat and vanilloids, whereas acidic conditions (pH <6) directly activate the channel. Can be activated by endogenous compounds, including 12-hydroperoxytetraenoic acid and bradykinin. Acts as ionotropic endocannabinoid receptor with central neuromodulatory effects. Triggers a form of long-term depression (TRPV1-LTD) mediated by the endocannabinoid anandamine in the hippocampus and nucleus accumbens by affecting AMPA receptors endocytosis (By similarity).

Post-translational modifications

Phosphorylation by PKA reverses capsaicin-induced dephosphorylation at multiple sites probably including Ser-117 as a major phosphorylation site. Phosphorylation by CAMKII seems to regulate binding to vanilloids. Phosphorylated and modulated by PRKCE, PRKCM and probably PRKCZ. Dephosphorylation by calcineurin seems to lead to receptor desensitization and phosphorylation by CAMKII recovers activity.

Sequence Similarities

Belongs to the transient receptor (TC 1.A.4) family. TrpV subfamily. TRPV1 sub-subfamily.

Tissue Specificity

Detected in neurons in the root ganglia (at protein level). Detected in dorsal root ganglia.

Cellular localization

• Postsynaptic cell membrane
• Multi-pass membrane protein
• Cell projection
• Dendritic spine membrane
• Multi-pass membrane protein
• Cell membrane
• Multi-pass membrane protein
• Mostly, but not exclusively expressed in postsynaptic dendritic spines.

Alternative names

Transient receptor potential cation channel subfamily V member 1, TrpV1, Osm-9-like TRP channel 1, Vanilloid receptor 1, OTRPC1, Trpv1

Database links

swissprot:Q704Y3 entrezGene:193034

Other research areas

• Immunology & Infectious Disease