Overview
- De Petrocellis, L. et al. (2011) Pharmacol. Res. 63, 294.
- Kort, M.E. and Kym, P.R. (2012) Prog. Med. Chem. 51, 57.
- Luongo, L. et al. (2012) Pharmacol. Res. 66, 243.
- Peppin, J.F. and Pappagallo, M. (2014) Ther. Adv. Neurol. Disord. 7, 22.
- Rossi, F. et al. (2014) Br. J. Pharmacol. 171, 2621.
- Alomone Labs Palvanil activates TRPV1 channels heterologously expressed in C6 cells.Cells were loaded with Fluo-3 AM and changes in intracellular Ca2+ were measured. Normalized fluorescence before (control, gray dotted line) and after application of 0.1 and 1 µM Palvanil (#P-205), (as indicated).
Transient receptor potential vanilloid receptor 1 (TRPV1) is a non-selective cation channel that is stimulated by capsaicin, protons, endogenous lipids, and hot temperature. Upon activation, TRPV1 initiates a signaling cascade that results in elevated levels of pain-inducing factors. It is located in sensory ganglia composed of neurons that send projection throughout the periphery1.
N-palmitoyl-vanillamide (palvanil) is a TRPV1 agonist, a non-poignant analogue to capsaicin (capsaicinoid). It has a slower kinetic opening-onset than capsaicin, but it activates the channel more potently. It induces significantly milder side effects – e.g. imbalanced thermal homeostasis and bronchoconstriction - than capsaicin, and it seems to be suitable as a topical anti-analgesic. It is effective in reducing edema2, and can inhibit inflammatory and neuropathic pain3, and interestingly, in vitro data have shown that at low concentrations it encourages the proliferation of osteoclasts, and does the opposite at high concentrations4.