TRPV1 Signaling: Mechanistic Understanding and Therapeutic Potential

Title: TRPV1 Signaling: Mechanistic Understanding and Therapeutic Potential

Volume: 11 Issue: 17

Author(s): Rong Xia, Tarek A. Samad, Joan Btesh, Lin-Hua Jiang, Ibrahim Kays, Louise Stjernborg and Niek Dekker

Affiliation:

Keywords: TRP, Ion channel, therapy, thermoregulation, hyperthemia, agonist, antagonist, TRPV1 Signaling, TRPV1, noxious heat, vanilloids and extracellular protons, sensory nociceptors, inflammation, neuropathy, TRPV1 agonists and antagonists

Abstract: Transient receptor potential vanilloid 1 (TRPV1) is a non-selective cation channel gated by noxious heat, vanilloids and extracellular protons. TRPV1 acts as an important signal integrator in sensory nociceptors under physiological and pathological conditions including inflammation and neuropathy. Because of its integrative signaling properties in response to inflammatory stimuli, TRPV1 agonists and antagonists are predicted to inhibit the sensation of ongoing or burning pain that is reported by patients suffering from chronic pain, therefore offering an unprecedented advantage in selectively inhibiting painful signaling from where it is initiated. In this article, we summarize recent advances in the understanding of the role of TRPV1 in pain signaling, including an overview of clinical pharmacological trials using TRPV1 agonists and antagonists. Finally, we also present an update on the mechanistic understanding and controlling of hyperthermia caused by TRPV1 antagonists, and provide perspectives for future studies.

Cite this article as:

Xia Rong, A. Samad Tarek, Btesh Joan, Jiang Lin-Hua, Kays Ibrahim, Stjernborg Louise and Dekker Niek, TRPV1 Signaling: Mechanistic Understanding and Therapeutic Potential, Current Topics in Medicinal Chemistry 2011; 11 (17) . https://dx.doi.org/10.2174/156802611796904843