Valerenic acid
Valerenic acid is a sesquiterpenoid constituent of the essential oil of the Valerian plant. Not to be confused with valeric acid or valproic acid, which are related to each other and are anticonvulsants.
Valerian is used as a herbal sedative which may be helpful in the treatment of insomnia.
The precise mechanism of this action has not been established. It is likely that several different components of the plant contribute to the effect. Valerenic acid is thought to be at least partly responsible for the sedative effects.
A study in 2004 found valerenic acid to act as a subtype-selective GABAA receptor positive allosteric modulator in neonatal rat brainstem preparations. The mechanism of this action could not be elucidated in this study.
A study in 2007 on GABA receptors of various composition, expressed in Xenopus oocytes (frog eggs), found valerenic acid to act mainly at α1β2 and α1β3 subtypes of these receptors. Only channels incorporating β2 or β3 subunits were stimulated by valerenic acid. Modulation of ion channel action was not significantly dependent on incorporation of α1, α2, α3 or α5 subunits.
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