TRPV1

Capsaicin, the main pungent ingredient in hot chili peppers, elicits a sensation of burning pain by selectively activating sensory neurons that convey information about noxious stimuli to the central nervous system. The protein encoded by this gene is a receptor for capsaicin and is a non-selective cation channel that is structurally related to members of the TRP family of ion channels. This receptor is also activated by increases in temperature in the noxious range, suggesting that it functions as a transducer of painful thermal stimuli in vivo. Four transcript variants encoding the same protein, but with different 5' UTR sequence, have been described for this gene. [provided by RefSeq]

transient receptor potential cation channel, subfamily V, member 1

Ligand-activated non-selective calcium permeant cation channel involved in detection of noxious chemical and thermal stimuli. Seems to mediate proton influx and may be involved in intracellular acidosis in nociceptive neurons. Involved in mediation of inflammatory pain and hyperalgesia. 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 Ca2+-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.

Biological Process behavioral response to pain Source:Ensembl
Biological Process calcium ion import across plasma membrane Source:UniProtKB1 Publication
Biological Process calcium ion transmembrane transport Source:UniProtKB
Biological Process cell surface receptor signaling pathway Source:ProtInc1 Publication
Biological Process cellular response to acidic pH Source:UniProtKB1 Publication
Biological Process cellular response to alkaloid Source:UniProtKB
Biological Process cellular response to ATP Source:UniProtKB
Biological Process cellular response to heat Source:UniProtKB1 Publication
Biological Process cellular response to nerve growth factor stimulus Source:Ensembl
Biological Process cellular response to temperature stimulus Source:Ensembl
Biological Process cellular response to tumor necrosis factor Source:Ensembl
Biological Process chemosensory behavior Source:ProtInc1 Publication
Biological Process detection of chemical stimulus involved in sensory perception of pain Source:Ensembl
Biological Process detection of temperature stimulus involved in sensory perception of pain Source:Ensembl
Biological Process detection of temperature stimulus involved in thermoception Source:Ensembl
Biological Process diet induced thermogenesis Source:Ensembl
Biological Process fever generation Source:Ensembl
Biological Process glutamate secretion Source:Ensembl
Biological Process lipid metabolic process Source:Ensembl
Biological Process microglial cell activation Source:Ensembl
Biological Process negative regulation of establishment of blood-brain barrier Source:Ensembl
Biological Process negative regulation of heart rate Source:Ensembl
Biological Process negative regulation of mitochondrial membrane potential Source:Ensembl
Biological Process negative regulation of systemic arterial blood pressure Source:Ensembl
Biological Process negative regulation of transcription by RNA polymerase II Source:Ensembl
Biological Process peptide secretion Source:Ensembl
Biological Process positive regulation of apoptotic process Source:Ensembl
Biological Process positive regulation of cytosolic calcium ion concentration Source:Ensembl
Biological Process positive regulation of gastric acid secretion Source:Ensembl
Biological Process positive regulation of nitric oxide biosynthetic process Source:Ensembl
Biological Process protein homotetramerization Source:UniProtKB
Biological Process response to capsazepine Source:UniProtKB1 Publication
Biological Process response to peptide hormone Source:Ensembl
Biological Process sensory perception of mechanical stimulus Source:Ensembl
Biological Process smooth muscle contraction involved in micturition Source:Ensembl
Biological Process thermoception Source:MGI1 Publication

Postsynaptic cell membrane
Cell projection, dendritic spine membrane
Cell membrane
Mostly, but not exclusively expressed in postsynaptic dendritic spines.

Cytoplasmic: 1-433
Helical: 434-454
Extracellular: 455-471
Helical: 472-497
Cytoplasmic: 498-510
Helical: 511-531
Extracellular: 532-535
Helical: 536-556
Cytoplasmic: 557-571
Helical: 572-599
Extracellular: 600-658
Helical: 659-687
Cytoplasmic: 688-839

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.