TRPV1: a therapy target that attracts the pharmaceutical interests

TRPV1 is a non-selective cation channel gated by noxious heat, vanilloids and extracellular protons, and act as an important signal integrator in sensory nociceptors. Because of its integrative signaling properties in response to inflammatory stimuli, TRPV1 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 chapter, we firstly summarize the physiological and pathological roles of TRPV1 and then describe the pharmacology of TRPV1 agonists and antagonists. Finally, we give an update and the status on TRPV1 therapies that have progressed into clinical trials.