Protein / target
Transient receptor potential cation channel subfamily V member 1
Protein at a glance
Biological role
Extracellular ligand-gated monoatomic ion channel
Strongest disease association
Migraine Disorders
Therapeutic position
Established drug target
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function overview
Non-selective calcium permeant cation channel involved in detection of noxious chemical and thermal stimuli.
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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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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
Receptor tyrosine kinase signalling
- ·Non-selective calcium permeant cation channel involved in detection of noxious chemical…
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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.
Approved medicines with mapped indications
Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.
3 medicines meet Open Targets' target-level approved-medicine definition; the 2 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.
Drugs targeting this protein
How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.
Vanilloid receptor opener
Indicated for Arthritis, Back Pain, Contusions, Neuralgia
Vanilloid receptor opener
Indicated for Acute Pain, Arthritis, Back Pain, Common Cold
ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.
Translational evidence
Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.
Strongest disease associations · via encoding gene TRPV1
Gene-level evidence surfaced through the gene TRPV1 that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.
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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 per-type scores above show the calculation.
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Drug development
19 compounds recorded · 3 approved · 16 in clinical development
View all recorded compounds (10)Hide
Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.
Tractability
Small molecules — Strong
Antibodies — Emerging
Protein degraders — Emerging
Other modalities — Strong
View underlying tractability evidence (10)Hide
Raw Open Targets tractability assessment buckets, by modality.
Safety-related annotations
Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.
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. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.
View all trials (26)Hide
ClinicalTrials.gov via the drug-target graph.
What's happening now
Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 2 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.
- Supplemental approval
Supplemental approval: ACETAMINOPHEN AND CODEINE (ANDA040779)
- Supplemental approval
Supplemental approval: ACETAMINOPHEN AND CODEINE PHOSPHATE (ANDA040419)
- Supplemental approval
Supplemental approval: ACETAMINOPHEN AND CODEINE PHOSPHATE (ANDA087508)
- Supplemental approval
Supplemental approval: ACETAMINOPHEN AND CODEINE PHOSPHATE (ANDA089805)
- Supplemental approval
Supplemental approval: ACETAMINOPHEN AND CODEINE PHOSPHATE (ANDA089828)
- Supplemental approval
Supplemental approval: ACETAMINOPHEN AND CODEINE PHOSPHATE (ANDA089990)
- Supplemental approval
Supplemental approval: ACETAMINOPHEN AND CODEINE PHOSPHATE (ANDA202800)
- Supplemental approval
Supplemental approval: ACETAMINOPHEN AND CODEINE PHOSPHATE (ANDA211610)
- New publicationCapsaicin, The Vanilloid Receptor TRPV1 Agonist in Neuroprotection: Mechanisms Involved and Significance.
- New publicationComparison of clinical outcomes of acetaminophen IV vs PO in the peri-operative setting for laparoscopic inguinal hernia repair surgeries: A triple-blinded, randomized controlled trial.
- New publicationA randomized placebo-controlled trial of acetaminophen for prevention of post-vaccination fever in infants.
- New publicationA randomized, double-blind, placebo-controlled, multicenter, repeat-dose study of two intravenous acetaminophen dosing regimens for the treatment of pain after abdominal laparoscopic surgery.
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.