Valerenic acid_product_DataBase

Bioactivity

Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties[1][2][3].

Invitro

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-HT5a receptor, with an IC50 of 17.2 μM (Ki=10.7 μM)[2].[3H]Valerenic acid binds to brain membranes reveals both a high affinity binding site (KD=25 nM) and a low affinity site (KD=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].

Name

Valerenic acid

CAS

3569-10-6

Formula

C15H22O2

Molar Mass

234.33

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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. [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. [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. [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.

PeptideDB

Valerenic acid

CAS: 3569-10-6 F: C15H22O2 W: 234.33