Acs Chem Neurosci
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The psychoactive plant kratom is a native plant to Southeast Asia, and its major bioactive alkaloid is mitragynine. Mitragynine exerts its analgesic properties by acting on the opioid receptors. One of its active metabolites, 7-hydroxymytraginine, is found to be 40 times more potent than mitragynine and 10 times more potent than morphine. ⋯ Kratom is currently marketed in the United States as a dietary or herbal supplement used to treat chronic pain, anxiety, and depression with over $207 million in annual sales in the United States alone. Here, we will review the traditional and medicinal uses of kratom along with the synthesis of its bioactive ingredients and their pharmacology, metabolism, and structure-activity relationships. The importance in society of this currently controversial substance will also be discussed.