The cannabinoid receptor 1 (CB1) is a G-protein-coupled receptor and has been recognized as a promising target for the treatment of many disorders, including pain, inflammation, metabolic syndromes, and neurodegenerative diseases.1 However, the CB1 receptor has been challenging as a druggable target because of central nervous system side effects associated with drug candidates that bind to the orthosteric site where the endogenous cannabinoids bind. Here, CNR1 is linked to metabolic syndrome.