Puerarin is an isoflavone derivative of daidzein found in Pueraria (Radix); it exhibits anxiolytic, cardioprotective, neuroprotective, and antioxidative activities. This compound also acts as a phytoestrogen. Puerarin acts as an antagonist at 5-HT2C receptors and at the benzodiazepine site on GABA-A receptors. Puerarin increases social interaction time and locomotor activity in animal models of substance withdrawal and inhibits cognitive impairment in the Morris water maze paradigm in animal models of Alzheimer’s disease. Additionally, puerarin decreases systolic blood pressure and heart rate and downregulates expression of P2X3 receptors in animal models of myocardial ischemia/reperfusion. This compound also protects neurons against H2O2-induced oxidative stress in vitro.