Capsaicin. A Powerful TRPV1 Agonist.
Vanilloid receptor 1 (VR1), also known as TRPV1, is a nonselective cation channel that is activated by heat and acid, as well as vanilloids.
Capsaicin is a TRPV1 agonist, which acts directly on TRPV1. Being small and hydrophobic, capsaicin crosses the plasma membrane readily to reach its intracellular ligand-binding site on TRPV1, leading to channel activation and cation permeation.
Capsaicin acts directly on TRPV1, with half-maximal effective concentration of 711.9�nM in Xenopus oocytes and 0.29 μM in HEK293 cells.
Ion Channel Modulators; TRP Channel Modulators.