Valerenic acid  (Synonyms: (-)-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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

234.33

C₁₅H₂₂O₂

3569-10-6

Solid

White to off-white

O=C(O)/C(C)=C/[C@H]1C2=C(C)CC[C@]2([H])[C@H](C)CC1

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

• [1]. Benke D, et, al. GABA A receptors as in vivo substrate for the anxiolytic action of valerenic acid, a major constituent of valerian root extracts. Neuropharmacology. 2009 Jan;56(1):174-81.  [Content Brief]

  [2]. Dietz BM, et, al. Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro. Brain Res Mol Brain Res. 2005 Aug 18;138(2):191-7.  [Content Brief]

  [3]. Kara M, et, al. Ameliorative Effects of the Sesquiterpenoid Valerenic Acid on Oxidative Stress Induced in HepG2 Cells after Exposure to the Fungicide Benomyl. Antioxidants (Basel). 2021 May 8;10(5):746.  [Content Brief]

  [4]. Becker A, et, al. The anxiolytic effects of a Valerian extract is based on valerenic acid. BMC Complement Altern Med. 2014 Jul 28;14:267.  [Content Brief]