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Cannabinoid receptor 1 (CB1) is highly important in the pathophysiology of several diseases due to their regulatory roles in central nervous system and peripheral tissues. Direct use of cannabinoids is limited mostly because of their psychoactive properties; therefore augmenting endocannabinoids by inhibiting the enzymes responsible for their degradation (e.g. FAAH, MAGL) appears as a valuable therapeutic strategy. Furthermore, peripherally restricted CB1 agonists and antagonists emerge as novel therapeutics. While activation of CB1 receptors can be used for the treatment of pain, anxiety, depression, PTSD, post-menopausal osteoporosis, cancer and neurodegenerative disorders; inhibition of this system can be used for the treatment of obesity, diabetes, liver and cardiometabolic disorders, postmenopausal osteoporosis and addiction. Here we summarized the therapeutical considerations for the cannabinoid system. [ABSTRACT FROM AUTHOR]