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. 2014 May 23;3(2):517-45.
doi: 10.3390/cells3020517.

TRPV1: A Potential Drug Target for Treating Various Diseases

Rafael Brito  1 , Sandeep Sheth  2 , Debashree Mukherjea  3 , Leonard P Rybak  4 , Vickram Ramkumar  5
Affiliations

TRPV1: A Potential Drug Target for Treating Various Diseases

Rafael Brito et al. Cells. .

Abstract

Transient receptor potential vanilloid 1 (TRPV1) is an ion channel present on sensory neurons which is activated by heat, protons, capsaicin and a variety of endogenous lipids termed endovanilloids. As such, TRPV1 serves as a multimodal sensor of noxious stimuli which could trigger counteractive measures to avoid pain and injury. Activation of TRPV1 has been linked to chronic inflammatory pain conditions and peripheral neuropathy, as observed in diabetes. Expression of TRPV1 is also observed in non-neuronal sites such as the epithelium of bladder and lungs and in hair cells of the cochlea. At these sites, activation of TRPV1 has been implicated in the pathophysiology of diseases such as cystitis, asthma and hearing loss. Therefore, drugs which could modulate TRPV1 channel activity could be useful for the treatment of conditions ranging from chronic pain to hearing loss. This review describes the roles of TRPV1 in the normal physiology and pathophysiology of selected organs of the body and highlights how drugs targeting this channel could be important clinically.

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Figures

Figure 1
Figure 1
Chemical structures of natural and endogenous transient receptor potential vanilloid 1 (TRPV1) receptor agonists.
Figure 2
Figure 2
Chemical structures of competitive TRPV1 receptor antagonists.
Figure 3
Figure 3
Chemical structures of non-competitive TRPV1 receptor antagonists.
See this image and copyright information in PMC

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