Cannabinoids act through specific receptors CB1 and CB2. The CB1 receptors are mainly localized in the brain (hippocampus, cerebellum and cerebrum) while CB2 receptors are mainly situated in the periphery (spleen, tonsilla and cells of the immunological system). Natural cannabinoids exhibit more affinity to CB1 receptors which bind for anandamide. These receptors reduce the activity of several intracellular enzymes decreasing the amount of neurotransmitters released. In effect, neuronal excitability of the brain is reduced. In the reward system of the brain cannabinoids activate dopamine neurons by withdrawal of inhibitory effects of GABA. Cannabinoids have been used for treatment of rheumatism, malaria, headache and constipation. Synthetic THC (dronabinol) found application in the medical treatment of anorexia, nausea and vomiting associated with cancer chemotherapy. However, with the development of modern drugs the therapeutic meaning of cannabinoids declines.

Cannabis is widely used for its altering mood and relaxation properties. They have demotivating effects on training and sport competition. Lack of scientific evidence for performance enhancing properties of cannabis is associated with the strong evidence of its adverse effects on psychomotor skills and cognitive function in the user. In sports that entail speed, agility and attention (skiing, motor sports, etc.) the decreased psychomotor performance raises the problem of safety. There is a growing number of young athletes using cannabinoids independent of the sport discipline. This fact suggests that cannabinoids are not used for doping purpose but rather for social reasons. Personality may have some impact on cannabinoids use since competitors of extreme and combat sports are more susceptible for those substances than other athletes.

Banning of cannabinoids in sport bases on safety concern during training and competition, to positively idolize elite athletes in society and to back up illegality of cannabinoids use in many countries. According to WADA regulation, out-of-competition samples are not tested for narcotics and cannabinoids. In the period 2001-2005 opioids were detected only in 0.1% of total samples (760 808)  analyzed by all IOC and WADA accredited laboratories while the relative contribution of positive samples with cannabinoids were 0.27%. Considering that this type of samples account for approximately 50% of the total samples analyzed the real number of cannabinoids cases can be much greater than that reported. This fact illustrates the scale of cannabinoids use in sport.