Cannabidiol, short CBD, is a relatively late discovered cannabinoid from the hemp plant. Cannabidiol is classified as a so-called cannabinoid. Cannabinoids are active substances which were mainly found in the hemp plant (Cannabis sativa or Cannabis indica). The best known cannabinoids are cannabidiol (CBD) and tetrahydrocannabinol (THC). The latter is responsible for the intoxicating effects of hemp plants. Cannabidiol is the cannabinoid that is thought to have the most medicinal potential. In comparison to many other plant active substances, cannabinoids were only researched relatively late. It was not until the 1970s that researchers succeeded in deciphering the structure of cannabidiol and THC.
Contrary to popular belief, CBD does not primarily bind to the classical receptors CB1 and CB2, but interacts mainly with the G-protein Coupled Receptor GPR55, the Peroxisome Proliferator-Activated Receptor gamma (PPARγ) and ion channels such as the vanilloid Transient Receptor Potential Channels (TRPV1, TRPA1).
CBD is a complete agonist of Transient Receptor Potential Vanilloid Type 1 (TRPV1), which plays an important role in the reaction to hot (e.g. boiling water) and harmful substances. TRPV1 is a nociceptor: when the receptor is sufficiently stimulated, signals are sent to the brain. This triggers a number of automatic responses, including pain sensation.
Various cannabinoids, including the endocannabinoids anandamide and N-arachidonyl-dopamine (an agonist of the CB1 receptor), affect the TRPV1 receptor. Conversely, several vanilloids influence the cannabinoid receptors, including olvanil and pseudocapsaicin (nonivamide), but not capsaicin itself. The close chemical relationship between many vanilloids and cannabinoids has led researchers to conclude that research into vanilloid cannabimimetics (substances that mimic cannabinoids) has great therapeutic potential.
In addition, CBD has been shown to act as an agonist of the 5HT1a receptor(24). This receptor controls the expression of serotonin (5HT) in the central nervous system, and this may explain many of the anxiety and depression-relieving properties of CBD. In addition, CBD has a regulatory effect on the M- and delta opioid receptors that are responsible for the narcotic and euphoric response during cannabis use, which is likely to increase this effect in the consumer as a whole.
On CB1 and CB2 receptors (major formation sites of THC), CBD acts as a non-competitive nagative-allosteric modulator of CB1. CBD is neither an agonist nor an antagonist, but impedes the binding of THC to these receptors(23). This explains the absence of psychoactive side effects and supports the thesis that CBD is the antagonist of THC in its mode of action.
(23) R B Laprairie, A M Bagher, M E M Kelle, E M Denovan-Wright. Cannabidiol is a negative allosteric modular of the cannabinoid CB1 receptor. British Journal of Pharmacology, 27. July 2015 Link
(24) Russo EB, Burnett A, Hall B, Parker KK. Agonistic properties of cannabidiol at 5-HT1a receptors. Neurochempcal Res. August 2005 Link
It is relatively new that athletes can benefit at all from the positive properties of CBD. It was not until 1 January 2018 that WADA (World Anti-Doping Agency) removed cannabidiol from the doping list as the only cannabinoid. The second known cannabinoid, THC, remains on the list of banned substances.
Even if the intake of THC would not make sense for athletes anyway due to its psychoactive and tiring effect, the intake is and remains illegal and could become a problem in a doping test if the established limit value is exceeded. Therefore, it is important for competitive athletes to pay attention to the quality of the product. According to the law, CBD products may contain up to 1% THC in some countries in order to be sold legally and as "THC-free". Therefore, the phrase "THC-free" should be used with caution.
Since THC is a very lipophilic (fat-loving) substance, it stores itself in the body and it takes relatively long to break it down again. Since athletes use CBD regularly, it is quite possible that even at low concentrations of 0.2% THC the doping relevant limit value is exceeded. Therefore, we advise you to be very cautious when buying CBC. Before selling CBD products, athletes should make sure that the products are free of THC. Serious suppliers have each batch checked for THC content by an accredited laboratory.
Cannabidiol is said to have the following properties, among others: