Capsaicin Receptor TRPV1: Biophysics, Physiology, and Pharmacology

The animal receptor for capsaicin, an important metabolite found in chili peppers that bestows the signature spiciness, is TRPV1 (Transient Receptor Potential Vanilloid 1). It is a cation channel that allows cations to permeate through cell membranes to initiate action potentials in nociceptive neurons. In addition to sensing pungent chemicals in plants, TRPV1 responds to extracellular protons, animal peptide toxins and membrane depolarization. It also serves as a thermosensor involved in controlling body core high-temperature protection from noxious high temperature hazards by initialing pain signals. Rapid developments of pharmacology, electrophysiology and structural biology yield high-resolution TRPV1 structures bound with different ligands and evolving mechanistic understanding of the activation mechanisms of TRPV1. In this chapter, we review the biophysics, physiology, and pharmacology of TRPV1.