Valerenic acid
(2E)-3-[(2R,8aR)-4,7-dimethyl-1-oxo-2,3,4,6,7,8-hexahydroazulen-2-yl]-2-methylprop-2-enoic acid
Chemical Class
Sesquiterpene / Iridoid
Molecular Formula
C15H22O2
Molecular Weight
234.33 g/mol
Half-Life
Plasma half-life approximately 1–2 hours. Metabolised via hepatic pathways including glucuronidation.
Bioavailability
Good oral bioavailability. Rapidly absorbed, with peak plasma levels within 30–60 minutes. Crosses the blood-brain barrier, contributing to central nervous system effects.
Known Effects
Sedative, anxiolytic, anticonvulsant, and muscle relaxant activity. Primary marker compound for standardisation of valerian preparations. Responsible for many of valerian's CNS effects.
Mechanism of Action
Positive allosteric modulator of GABA-A receptors, enhancing GABAergic neurotransmission without direct receptor activation. Inhibits GABA transaminase (GABA-T), reducing GABA catabolism. Potential affinity for adenosine A1 receptors, contributing to sedative effects. 5-HT receptor interactions may contribute to anxiolytic activity.
Safety Data
No significant toxicity reported at standard therapeutic doses. Valerian preparations generally well-tolerated. Mild morning drowsiness reported in some individuals. Long-term safety data limited.