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Updated: Mar 7, 2026

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

Published on: December 31, 2013

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Modulation of the TRPV4 ion channel as a therapeutic target for disease

Megan S Grace1, Sara J Bonvini2, Maria G Belvisi2

  • 1Baker Heart and Diabetes Institute, Melbourne, Australia; School of Health and Biomedical Sciences, RMIT University, Bundoora, Melbourne, Australia; Department of Physiology, School of Medicine, Nursing and Health Sciences, Monash University, Melbourne, Australia.

Pharmacology & Therapeutics
|February 17, 2017
PubMed

Insights

Targeting the Transient Receptor Potential Vanilloid 4 (TRPV4) ion channel shows therapeutic promise for various conditions. Research indicates TRPV4 antagonism may treat edema, pain, GI disorders, and lung diseases, with human trials underway.

Area of Science:

  • Physiology
  • Pharmacology
  • Molecular Biology

Background:

  • Transient Receptor Potential Vanilloid 4 (TRPV4) is a polymodal ion channel with widespread physiological and pathophysiological roles.
  • TRPV4's involvement in numerous diseases has been identified, making it a potential therapeutic target.

Purpose of the Study:

  • To review the known roles of TRPV4 in disease.
  • To highlight the therapeutic potential of targeting TRPV4 for various pathologies.

Main Methods:

  • Utilizing data from TRPV4 knockout mouse models.
  • Analyzing results from synthetic pharmacological compounds targeting TRPV4.
  • Reviewing findings from in vivo studies and first-in-human trials.

Main Results:

  • TRPV4 antagonism shows therapeutic potential in preclinical models for edema, pain, gastrointestinal disorders, and lung diseases (cough, bronchoconstriction, pulmonary hypertension, acute lung injury).
  • A lack of observed in vivo side-effects has led to a first-in-human trial for a TRPV4 antagonist.
  • The trial includes healthy participants and patients with stable heart failure.

Conclusions:

  • TRPV4 antagonism represents a promising therapeutic strategy for a range of TRPV4-related diseases.
  • Successful clinical trials could establish TRPV4 as a significant new target for drug development.
  • Further research into TRPV4-mediated pathologies is warranted.
Keywords:
Gastrointestinal diseaseInflammationOedemaPainRespiratory diseaseTRPV4Vascular tone

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