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Disease-Related Changes in TRPV1 Expression and Its Implications for Drug Development

[ Vol. 11 , Issue. 17 ]


Louis S. Premkumar and Mahendra Bishnoi   Pages 2192 - 2209 ( 18 )


The transient receptor potential vanilloid 1(TRPV1) channel has been a topic of great interest, since its discovery in 1997. It is a homotetrameric non-selective cation channel predominantly expressed in a population of sensory neurons and its involvement in different modalities of pain has been extensively studied. However, TRPV1 has also been shown to be expressed in non-sensory neurons and non-neuronal cells. TRPV1 is considered as a potential target for drug development, based on its tissue distribution and its role in physiological functions. Here, we summarize the evidences for disease-related alterations in TRPV1 expression and function and review the current perspectives for the therapeutic potential of TRPV1 agonists and antagonists in the treatment of a wide range of diseases.


TRPV1, nociceptors, inflammatory mediators, pain, nociceptive ion channels, Drug Development, homotetrameric non-selective cation channel, modalities of pain, non-sensory neurons, non-neuronal cells, tissue distribution, disease-related alterations in TRPV1 expression, ion channels, by pro-inflammatory agents, thermal inflammatory pain


Department of Pharmacology, Southern Illinois University School of Medicine Springfield, IL 62702, USA.

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