Overview
- Melck, D. et al. (1999) Biochem. Biophys. Res. Commun. 262, 275.
- Di Marzo, V. et al. (2000) Eur. J. Pharmacol. 406, 363.
- Di Marzo, V. et al. (2002) J. Pharmacol. Exp. Ther. 300, 984.
Alomone Labs Arvanil activates TRPV1 channels expressed in rat C6 glioma cells.mTRPV1-C6 cells were loaded with Fluo-3 AM. Changes in intracellular Ca2+ were detected as changes in Fluo-3 signal following agonist application. Normalized fluorescence before and after application (at 20 seconds, arrow) of control solution, 5 nM and 500 nM Arvanil (#A-335), as indicated.
Arvanil (N-Vanillylarachidonamide) is an agonist of TRPV1 channels and a ligand of CB1 cannabinoid receptors. Arvanil is a structural hybridization between the arachidonoyl group of anandamide (CB1 receptor ligand) and the vanillyl moiety of capsaicin1,2. Arvanil shows an EC50 value of 0.5 nM for TRPV1 receptors, and an IC50 value of 3.6 µM as an inhibitor of anandamide accumulation1.
Studies have found that arvanil has the ability to induce dose-dependent apoptosis in the lymphoid Jurkat T-cell line2.
CB1 receptors are important regulators of excitatory and inhibitory synaptic transmission in different areas in the brain. The receptor plays a crucial role in multiple sclerosis disease course and in mood control3.
TRPV1 receptors are highly expressed in primary nociceptors. These channels can be activated by several stimuli such as heat, acid, certain arachidonic acid derivatives and direct phosphorylation via PKC4.
