Transient receptor potential vanilloid 1 ion channel (TRPV1)

The Transient receptor potential vanilloid 1 (TRPV1) ion channel, also called the capsaicin receptor or vanilloid receptor 1, is a non-selective cation channel predominantly expressed in sensory neurons. It acts as a polymodal detector of noxious heat (above 42–43°C), chemical irritants (such as capsaicin and resiniferatoxin), acidic conditions, and endogenous lipids. TRPV1 mediates detection and modulation of pain and heat and is involved in inflammatory responses and tissue injury, especially in the gastrointestinal tract, nerves, muscles, and other organs. In the stomach, TRPV1 activation promotes the release of substance P and other neuropeptides, contributing to inflammation and mucosal damage. Drugs and natural products targeting TRPV1 are used for pain relief, gastrointestinal modulation, and other indications, but therapeutic modulation is limited by safety concerns related to body temperature regulation and inflammation.

Other names

Capsaicin receptorVanilloid receptor 1

Agonists activate TRPV1 to induce cation influx and pain sensation. Antagonists block activation, reducing pain and heat sensation but potentially causing hyperthermia. Resiniferatoxin desensitizes TRPV1, reducing acute pain but distorting thermal regulation.