Target intelligence / Profile preview

Transient Receptor Potential Vanilloid 1 (TRPV1)

Target
TRPV1
Molecular classification
Ion channel, TRP channel, Receptor
01

Overview

Transient receptor potential vanilloid 1 (TRPV1) is a nonselective cation channel primarily expressed in nociceptive sensory neurons, functioning as a molecular integrator for diverse noxious stimuli like heat, acidic pH, and chemical ligands such as capsaicin. Its activation leads to pain sensations and modulates both acute and chronic pain states. Dysregulation of TRPV1 is implicated in various conditions like chronic pain, IBS, hypertension, and asthma, making it a therapeutic target. Activation can also lead to long-term synaptic depression via calcium-dependent mechanisms.

Other names
Capsaicin receptorVanilloid receptor 1
02

Mechanism of action

TRPV1 antagonists inhibit the activity of the TRPV1 channel, reducing pain and inflammation.

03

Biological functions

Pain perceptionNociceptionThermosensationInflammatory responseRegulation of neuropeptide releaseGastrointestinal motility regulationTemperature homeostasisSensory integration
04

Disease associations

Chronic pain syndromesIrritable bowel syndromeHypertensionAsthmaInflammation
05

Safety considerations

Side effects with antagonists remain an issuePotential for altered thermosensationPotential for cardiovascular effects
06

Interacting drugs

Capsaicin

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