Pharmacology · April 2026

Kavalactones — the six major compounds.

Direct answer

Kava's effects come from 6 major kavalactones: desmethoxyyangonin (1), dihydrokavain (2), yangonin (3), kavain (4), dihydromethysticin (5), methysticin (6). Noble cultivars lead with kavain (#4) — uplifting and anxiolytic. Tudei cultivars are disproportionately dihydromethysticin (#5) — heavy and linked to hepatic concerns.

The six major kavalactones

#1

Desmethoxyyangonin

MAO-B inhibitor. Believed to potentiate dopamine. Mildly euphoric character.

#2

Dihydrokavain

Local anesthetic properties (the mouth-numbing sensation). Relaxing. Common in heavy relaxation cultivars.

#3

Yangonin

CB1 receptor activity observed in vitro. Mood-elevating; contributor to kava's anxiolytic profile.

#4

Kavain

The anxiolytic centerpiece. Voltage-gated sodium channel blocker. Uplifting, clear-headed relaxation. Noble kava leads with kavain.

#5

Dihydromethysticin

Sedating. Elevated in tudei cultivars and linked to the two-day lethargy and nausea. Avoid-high profile for daily drinking.

#6

Methysticin

Sedating; slightly less problematic than dihydromethysticin but still heavy. Noble cultivars keep this at lower ranks.

How to read a chemotype

Kava chemotype is a 6-digit number listing the six major kavalactones in descending order of abundance. For example, Borogu's chemotype 462531 means:

  1. Most-abundant: kavain (#4) — uplifting
  2. Second: dihydromethysticin (#6) — balanced
  3. Third: methysticin (#2) — (note, this is kavain-second variants — always read the exact ranking)

Rule of thumb: the leading number tells you the character. Leading 4 = kavain-forward = uplifting. Leading 2 = dihydrokavain-forward = body-relaxing. Leading 5 = dihydromethysticin = sedating and likely tudei — avoid.

Mechanism of action

Kavalactones modulate several neurotransmitter systems:

  • GABA-A receptors — allosteric modulation without benzodiazepine-like tolerance or dependence.
  • Voltage-gated sodium and calcium channels — similar to anticonvulsants; contributes to anxiolysis.
  • MAO-B inhibition (desmethoxyyangonin) — dopamine-sparing effect.
  • CB1 cannabinoid receptors (yangonin) — mood and relaxation.

The combined multi-target profile is why isolated kavain or extracts do not fully replicate the experience of whole-root aqueous preparation.

Why flavokavains matter

Flavokavains (A, B, C) are non-kavalactone compounds present at higher levels in tudei cultivars and in solvent-extracted products (acetone or ethanol extraction pulls them out; water prep does not). Flavokavain B has been associated with hepatotoxicity in in-vitro studies. This is the likely explanation for the 2002 FDA advisory — modern WHO reviews correlate the hepatotoxicity reports with solvent-extracted and tudei products rather than traditional noble aqueous preparations.

See our noble vs tudei comparison for the practical buying implications.