Valerenic acid

Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABA_A receptors. Valerenic acid is also a partial agonist of the 5-HT_5a receptor. Valerenic acid mediates anxiolytic activity via GABA_A receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties^[1][2][3]. In Vitro: 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_5a receptor, with an IC₅₀ of 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]. In Vivo: 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].