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Related Experiment Video

Updated: Apr 30, 2026

Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4

Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4

Published on: December 31, 2013

TRPV1.

Stuart Bevan¹, Talisia Quallo, David A Andersson

¹Wolfson Centre for Age Related Diseases, King's College London, London, SE1 1UL, UK, stuart.bevan@kcl.ac.uk.

Handbook of Experimental Pharmacology

|April 24, 2014

Summary

Transient Receptor Potential Vanilloid 1 (TRPV1) channels sense heat and pain. TRPV1 antagonists show therapeutic potential but raise concerns about hyperthermia and heat sensitivity loss.

Area of Science:

Molecular and Cellular Biology
Neuroscience
Physiology

Background:

Transient Receptor Potential Vanilloid 1 (TRPV1) is a channel protein expressed in sensory neurons and other mammalian tissues.
TRPV1 functions as a sensor for noxious heat (>42°C), acidic conditions (pH <6.5), and various chemical stimuli like capsaicin.
Its structure comprises six transmembrane domains with intracellular N- and C-termini, featuring regulatory sites for phosphorylation and lipid binding.

Purpose of the Study:

To review the structure, function, and physiological roles of the TRPV1 channel.
To discuss the implications of TRPV1 modulation in therapeutic contexts, particularly for pain management.
To highlight challenges and safety concerns associated with TRPV1 antagonist development.

Main Methods:

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Literature review of studies on TRPV1 structure, function, and pharmacology.
Analysis of data from in vitro and in vivo experiments, including studies with knockout mice.
Examination of clinical trial findings for TRPV1-targeting drugs.

Main Results:

TRPV1 forms a non-selective cation channel with specific kinetic properties and activation mechanisms.
TRPV1 plays roles in pain sensation, thermoregulation, osmoregulation, cough, and bladder control.
TRPV1 antagonists have shown promise but are associated with adverse effects like hyperthermia and reduced heat sensitivity.

Conclusions:

TRPV1 is a critical sensor involved in diverse physiological processes.
Targeting TRPV1 offers therapeutic avenues but requires careful consideration of safety profiles.
Further research is needed to balance efficacy and safety in TRPV1-based therapies.