Skip to main content
GutCited
Mechanisms of Action

Kavalactone

The class of psychoactive compounds in kava responsible for anxiolytic and sedative effects.

Kavalactones are a group of 18 lactone compounds found in the roots of kava (Piper methysticum). Six major kavalactones account for approximately 96% of the active content: kavain, dihydrokavain, methysticin, dihydromethysticin, yangonin, and desmethoxyyangonin. They produce anxiolytic effects through multiple mechanisms: enhancing GABA-A receptor binding, inhibiting voltage-gated sodium and calcium channels, modulating dopamine and norepinephrine reuptake, and reducing MAO-B activity. Different kavalactone ratios in various kava cultivars produce different effect profiles (more sedating vs. more euphoric). Standardized extracts typically contain 30-70% kavalactones.