Protein / target
Transient receptor potential cation channel subfamily V member 1
Protein at a glance
Biological role
Extracellular ligand-gated monoatomic ion channel activity
Primary system
Nervous system
Strongest disease association
migraine disorder
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
3 approved · 16 in clinical development
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function
Non-selective calcium permeant cation channel involved in detection of noxious chemical and thermal stimuli (PubMed:11050376, PubMed:11243859, PubMed:11226139, PubMed:12077606). 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. Activated by vanilloids, like capsaicin, and temperatures higher than 42 degrees Celsius (PubMed:37117175). Upon activation, 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
Subcellular location
Domains and Gene Ontology detail (30)Hide
Gene Ontology
- Cdendritic spine membrane
- CGABA-ergic synapse
- Cmembrane
- Cplasma membrane
- Cpostsynaptic membrane
- FATP binding
- Fcalcium channel activity
- Fcalmodulin binding
- Fexcitatory extracellular ligand-gated monoatomic ion channel activity
- Fextracellular ligand-gated monoatomic ion channel activity
- Fintracellularly gated calcium channel activity
- Fmetal ion binding
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
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Synaptic signalling
- ·Postsynaptic cell membrane
- ·GABA-ergic synapse
- ·postsynaptic membrane
Ion channel gating
- ·excitatory extracellular ligand-gated monoatomic ion channel activity
- ·extracellular ligand-gated monoatomic ion channel activity
- ·temperature-gated ion channel activity
- ·calcium ion transmembrane transport
Ligand-gated signalling
- ·excitatory extracellular ligand-gated monoatomic ion channel activity
- ·extracellular ligand-gated monoatomic ion channel activity
- ·temperature-gated ion channel activity
Inhibitory neurotransmission
- ·GABA-ergic synapse
Transcriptional regulation
- ·negative regulation of transcription by RNA polymerase II
View underlying pathways (1)Hide underlying pathways
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Drugs targeting this protein
Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.
Vanilloid receptor opener
Appears in clinical studies involving Back pain, Pain, Myalgia, Muscle spasm
ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.
Translational evidence
Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.
Highest-confidence therapeutic associations
Diseases where a drug acting on this target has already reached clinical development.
Highest overall evidence
Remaining associations by Open Targets' aggregated evidence score.
Show all associationsHide all associations
Open Targets ranks 1,274 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.
Known drugs · 19 total
Chronic pain
Myalgia · Arthralgia · Pain
osteoarthritis · Pain
rhinitis · migraine disorder · Pain
atopic eczema · rosacea · rosacea
gastroesophageal reflux disease · osteoarthritis, knee · postherpetic neuralgia
Pain · toothache · Headache
Pain · overactive bladder · Ocular pain
Pain
neuropathic pain · postherpetic neuralgia
Tractability
Safety liabilities
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.
Show remaining trials (24)Hide
ClinicalTrials.gov via the drug-target graph.
Forefront confidence
Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.
The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.
What's happening now
Recent activity around this target, drawn from one canonical event stream. Every item is reached through a drug that targets this protein, so each event is news about that drug rather than about the protein directly.
- New publicationCapsaicin, The Vanilloid Receptor TRPV1 Agonist in Neuroprotection: Mechanisms Involved and Significance.
- Regulatory approval
Approval: Qutenza (EMA)
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.