The Function of TRPV1
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 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.
Protein names
Recommended name:
Transient receptor potential cation channel subfamily V member 1Alternative name(s):
TrpV1Capsaicin receptor
Osm-9-like TRP channel 1
OTRPC1
Vanilloid receptor 1
- RS222747 (TRPV1) ??
- RS222749 (TRPV1) ??
- RS224534 (TRPV1) ??
- RS8065080 (TRPV1) ??
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Top Gene-Substance Interactions
TRPV1 Interacts with These Diseases
| Disease | Score |
Substances That Increase TRPV1
| Substances | Interaction | Organism | Category |
Substances That Decrease TRPV1
| Substances | Interaction | Organism | Category |
Conditions with Increased Gene Activity
| Condition | Change (log2fold) | Comparison | Species | Experimental variables | Experiment name |
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Conditions with Decreased Gene Activity
| Condition | Change (log2fold) | Comparison | Species | Experimental variables | Experiment name |
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Technical
The following transcription factors affect gene expression:
Tissue specificity:
Widely expressed at low levels. Expression is elevated in dorsal root ganglia. In skin, expressed in cutaneous sensory nerve fibers, mast cells, epidermal keratinocytes, dermal blood vessels, the inner root sheet and the infundibulum of hair follicles, differentiated sebocytes, sweat gland ducts, and the secretory portion of eccrine sweat glands (at protein level).
Enzyme Regulation:
Channel activity is activated via the interaction with PIRT and phosphatidylinositol 4,5-bisphosphate (PIP2). Both PIRT and PIP2 are required to activate channel activity (By similarity). The channel is sensitized by ATP binding. Repeated stimulation with capsaicin gives rise to progressively smaller responses, due to desensitization. This desensitization is triggered by the influx of calcium ions and is inhibited by elevated ATP levels. Ca(2+) and CALM displace ATP from its binding site and trigger a conformation change that leads to a closed, desensitized channel. Intracellular PIP2 inhibits desensitization. The double-knot toxin (DkTx) from the Chinese earth tiger tarantula activates the channel and traps it in an open conformation.
Molecular Function:
- Transmembrane Signaling Receptor Activity
- Extracellular Ligand-Gated Ion Channel Activity
- Excitatory Extracellular Ligand-Gated Ion Channel Activity
- Calcium Channel Activity
- Atp Binding
- Calcium-Release Channel Activity
- Chloride Channel Regulator Activity
- Phosphatidylinositol Binding
- Metal Ion Binding
- Phosphoprotein Binding
- Temperature-Gated Ion Channel Activity
Biological Processes:
- Negative Regulation Of Transcription From Rna Polymerase Ii Promoter
- Fever Generation
- Microglial Cell Activation
- Diet Induced Thermogenesis
- Peptide Secretion
- Lipid Metabolic Process
- Transport
- Cell Surface Receptor Signaling Pathway
- Chemosensory Behavior
- Glutamate Secretion
- Cellular Response To Heat
- Positive Regulation Of Apoptotic Process
- Response To Peptide Hormone
- Positive Regulation Of Nitric Oxide Biosynthetic Process
- Behavioral Response To Pain
- Sensory Perception Of Mechanical Stimulus
- Thermoception
- Detection Of Temperature Stimulus Involved In Thermoception
- Detection Of Temperature Stimulus Involved In Sensory Perception Of Pain
- Detection Of Chemical Stimulus Involved In Sensory Perception Of Pain
- Protein Homotetramerization
- Smooth Muscle Contraction Involved In Micturition
- Positive Regulation Of Gastric Acid Secretion
- Calcium Ion Transmembrane Transport
- Cellular Response To Alkaloid
- Cellular Response To Atp
- Cellular Response To Tumor Necrosis Factor
- Cellular Response To Acidic Ph
- Cellular Response To Temperature Stimulus
- Negative Regulation Of Establishment Of Blood-Brain Barrier
- Response To Capsazepine
- Calcium Ion Import Into Cell
- Cellular Response To Nerve Growth Factor Stimulus
Drug Bank:
- Icosapent
- Aspartame
- Capsaicin
- Alpha-Linolenic Acid