Overview
- Thomas, K.C. et al. (2011) J. Pharmacol. Exp. Ther. 337, 400.
Alomone Labs Nonivamide activates TRPV1 channels heterologously expressed in C-6 cells.Cells were loaded with Fluo-3 AM and changes in intracellular Ca2+ were detected. Normalized fluorescence before (control, gray dotted line) and after application of 0.1, 1 and 10 µM Nonivamide (#N-220), (as indicated).
Nonivamide is a synthetic analog of capsaicin, a pungent ingredient in chili peppers. It binds to TRPV1 channel and activates it with high potency (EC50 ≈ 10-7 M). Treatment with nonivamide activates TRPV1 channels, allowing non-selective cation flux into neurons, causing membrane depolarization and increase in cytosolic Ca2+ due to release of Ca2+ from the endoplasmic reticulum1.
TRPV1 is a member of the TRP family of ion-channels and found throughout the body in epithelial cells and in peripheral and central terminals in neurons. The TRPV family includes six mammalian ion channels, TRPV1-TRPV6. TRPV1 is a Ca2+-permeable channel which is activated and modulated by a variety of exogenous stimuli such as heat, changes in pH, and irritant and pungent compounds and by selected molecules released during inflammatory processes and tissue damage2.
