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Target intelligence / Profile preview
Transient receptor potential vanilloid subfamily member 1 (TRPV1)
- Target
- TRPV1
- Molecular classification
- Ion channel, Receptor, TRP channel, Non-selective cation channel
01
Overview
Transient receptor potential vanilloid subfamily member 1 (TRPV1) is a non-selective cation channel primarily expressed in sensory neurons. It acts as a polymodal sensor, detecting noxious heat (>43°C), acidic conditions, capsaicin, and other chemical irritants. Activation leads to calcium influx and neuronal excitation, mediating pain sensation and contributing to thermoregulation and inflammation. TRPV1 is a tetrameric assembly of subunits, each with six transmembrane domains. It is an important therapeutic target for pain management disorders, though side effects remain a challenge for drug development.
- Other names
- Capsaicin receptorVanilloid receptor 1Vanilloid receptor type I
02
Mechanism of action
Agonists activate the channel, leading to calcium influx and neuronal excitation. Antagonists block channel activation.
03
Biological functions
NociceptionThermoregulationPain perceptionDetection of noxious stimuliRegulation of body temperatureInflammatory responses
04
Disease associations
Chronic pain syndromesInflammatory diseases
05
Safety considerations
Side effects with TRPV1 antagonists limit clinical use.Potential for altered pain perception and thermoregulation
06
Interacting drugs
Capsaicin
2 more in the full profile.
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