Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator ofGABA_Areceptors. Valerenic acid is also a partial agonist of the5-HT_5areceptor. Valerenic acid mediates anxiolytic activity via GABA_Areceptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties^[1][2][3].

Valerenic acid (1-100 μM) enhances the whole cell currents on GABAA receptors expressed in HEK 293 cells^[1].
Valerenic acid exhibits significant affinity for the 5-HT_5areceptor, with an IC₅₀of 17.2 μM (K_i=10.7 μM)^[2].
[³H]Valerenic acid binds to brain membranes reveals both a high affinity binding site (K_D=25 nM) and a low affinity site (K_D=16 μM)^[1].
[³H]Valerenic acid is displaced by Valerenol with high potency (IC₅₀=3 nM)^[1].

Valerenic acid (1-6 mg/kg i.p. or 10 mg/kg p.o.) decreases the aversion of wild type mice to the lit area^[2].
Valerenic acid (10 mg/kg; p.o.) increases the proportion of time 129X1/SvJ mice spent onto the open arms^[2].

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C₁₅H₂₂O₂

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