Overview
- De Petrocellis, L. et al. (2001) Br. J. Pharmacol. 163, 1479.
- Alomone Labs Cannabidiol activates TRPV1 channels expressed in C6 cells.mTRPV1-C6 cells were loaded with Fluo-3 AM. Changes in intracellular Ca2+ were detected via changes in Fluo-3 emission following agonist application. Normalized fluorescence before and after application (at 20 seconds) of control solution (dotted line), 10 and 100 µM Cannabidiol (#C-320), (grey and black lines, respectively).
- Alomone Labs Cannabidiol decreases Jurkat cells viability.Dose-response curve of Jurkat cell viability reduction by Cannabidiol (#C-320) as percentage of untreated control. Jurkat cells were cultured for 24 hours in serum-free medium in the presence of increasing concentrations of Cannabidiol with 0.5% BSA. Cell viability was determined by XTT colorimetric assay. IC50 was determined as 6.8 µM.
Transient receptor potential (TRP) channels are important mediators of sensory signaling with significant effect on signal transduction pathways and cellular activity. TRPV is a member of the Vanilloid subfamily of TRP channels1. TRPA1 is also a sub-member of TRP channels expressed in dorsal root ganglia, trigeminal ganglia and hair cells2.
Cannabis has been used for thousands of years as a medicinal agent for the relief of pain. Nonetheless, the exact pharmacology of cannabis and its active components remains mostly unknown. Cannabidiol (CBD) is an organic agonist of TRPV1, TRPV3 and TRPA1 channels synthesized from cannabis. It has an effective concentration of 0.1-10 μM and an IC50 of 0.16±0.05 μM for the TRPV1 channel. After binding to its target, CBD causes a desensitization of the target receptor. CBD is highly lipophilic which allows it to access intracellular sites of action. CBD exhibits significant anti-inflammatory properties.