Kawain is a kavalactone originally found in Piper methysticum (kava plant). Kawain exhibits neuroprotective, hypnotic, sedative, anxiolytic, antiepileptic/anticonvulsant, antithrombotic, and antifungal activities. Kawain activates Nrf2 in neurons and astroglia, protecting against amyloid-β (Aβ)-induced neurotoxicity. This compound displays antimicrobial efficacy against species of Fusarium, Trichoderma, and Colletotrichum. In animal models, Kawain decreases sleep latency and time awake and increases non-REM sleep time and delta activity during REM sleep. Additionally, kawain binds receptor site 2 and inhibits voltage-gated Na+ channels. Kawain also inhibits L-type voltage-gated Ca2+ channels. This compound also inhibits arachidonic acid-induced platelet aggregation and COX expression.