Target intelligence / Profile preview

Transient receptor potential vanilloid channel (TRPV) (TRPV)

Target
TRPV
Molecular classification
Ion channel, Non-selective cation channel, Calcium channel, Transient receptor potential channel family
01

Overview

Transient receptor potential vanilloid (TRPV) channels are a group of six non-selective cation channels (TRPV1–TRPV6) that function as versatile cellular sensors for various physical and chemical stimuli [PMID: 25323745]. These channels are primarily known for their roles in nociception and thermosensation, with TRPV1–TRPV4 acting as thermo-TRPs that respond to different temperature ranges [PMID: 30103444]. TRPV5 and TRPV6 are distinct as they are highly selective for calcium and are crucial for systemic calcium homeostasis in the kidneys and intestines [UniProt: Q9NQA5]. In disease, TRPV channels are heavily implicated in chronic pain, inflammation, and respiratory disorders, making them significant therapeutic targets [PMID: 28244311]. Pharmacological modulation involves both agonists, which can cause desensitization of sensory neurons (e.g., capsaicin), and antagonists designed to block pain signaling [PMID: 23406572]. However, clinical progress for some TRPV1 antagonists has been hindered by side effects such as hyperthermia and impaired heat perception [PMID: 18384730].

Other names
Vanilloid receptorTRP vanilloid subfamilyTRPV1-6OSM-9-like TRP channel
02

Mechanism of action

Agonism leading to receptor desensitization and Antagonism of channel activation

03

Biological functions

NociceptionThermosensationCalcium homeostasisMechanosensationOsmoregulationSignal transduction
04

Disease associations

Chronic painNeuropathic painInflammatory painOsteoarthritisMigraineOveractive bladderCancerDermatological disordersRespiratory disease
05

Safety considerations

Hyperthermia (fever-like response)Impaired perception of noxious heatParesthesiaRisk of burn injury
06

Interacting drugs

Capsaicin

7 more in the full profile.

07

Biomarkers

TRPV1 protein expression in skin biopsiesCalcitonin gene-related peptide (CGRP) levelsThermal pain threshold

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