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Valerenic acid

(-)-Valerenic Acid, (2E)-3-[(4S,7R,7aR)-3,7-dimethyl-2,4,5,6,7,7a-hexahydro-1H-inden-4-yl]-2-methylacrylic acid

A Positive Allosteric Modulator of the GABAA Receptors

Cat #: V-140
Alternative Name (-)-Valerenic Acid, (2E)-3-[(4S,7R,7aR)-3,7-dimethyl-2,4,5,6,7,7a-hexahydro-1H-inden-4-yl]-2-methylacrylic acid
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 234.33
    Purity: >98% (HPLC)
    Form Lyophilized Powder
    Effective concentration 10 - 200 µM
    Structure
    Chemical name (2E)-3-[(4S,7R,7aR)-2,4,5,6,7,7a-Hexadydro-3,7-dimethyl-1H-inden-4-yl]-2-methyl-2-propenoic acid
    Molecular formula C15H22O2
    CAS No.: 3569-10-6
    PubChem CID 6440940
    Activity Valerenic acid is a positive allosteric modulator of GABAA receptors that displays preference for β2 or β3 subunit receptors. Directly activates the receptor and also blocks the channel at high concentrations. Displays an anxiolytic and sedative activity in vivo1-3. Also acts as a partial agonist of 5-HT5A receptors4.
    References-Activity
    1. Khom, S. et al. (2007) Neuropharmacol., 53, 178.
    2. Benke, D. et al. (2008) Neuropharmacol. 56, 174.
    3. Khom, S. et al. (2016) J. Pharmacol. Exp. Ther. 357, 580.
    4. Dietz, B.M. et al. (2005) Brain Res. Mol. Brain Res., 138, 191.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Soluble in Ethanol and DMSO.
    Up to 200 mM in DMSO. Centrifuge all product preparations before use (5,000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Valerenic acid activates GABAA receptors expressed in Xenopus oocytes.
      Alomone Labs Valerenic acid activates GABAA receptors expressed in Xenopus oocytes.
      Representative time course of GABAA α1/β2 current, activated by a continuous application (top dotted line) of 0.1 µM γ-aminobutyric acid (#G-110), and enhanced by co-application of 10 µM Valerenic acid (#V-140), as indicated (bar), at a holding potential of -80 mV.
    • Alomone Labs Valerenic acid potentiates GABAA receptors expressed in Xenopus oocytes.
      Alomone Labs Valerenic acid potentiates GABAA receptors expressed in Xenopus oocytes.
      Representative time course of GABAA α1/β2 channel current activation by a continuous application of 200 µM Valerenic acid (#V-140), duration indicated by bar (bottom left), compared to activation by 0.1 µM γ-aminobutyric acid (#G-110), at a holding potential of -80 mV.
    References - Scientific background
    1. Ramharter, J. et al (2012) EurJOC., 10, 2041.
    2. Dietz, B.M. et al. (2005) Mol. Brain. Res., 138, 191.
    3. Lu, Q. et al. (2020) Int. J. Biol. Sci., 16, 2104.
    Scientific background

    Valerenic acid was first isolated in 1957 from the rhizome and roots of valerian (Valeriana offi-cinalis). Valerian is one of the oldest medicinal herbs in folk medicine and has been used for various afflictions like insomnia, anxiety, and pain. Valerenic acid was found to be pharmacologically active monoterpene acting through binding to the GABAA receptor1.

    Valerenic acid acts as an anti-inflammatory agent by inhibiting the transcription of NF-κB, one essential transcription factor controlling the expression of numerous inflammation-related genes. In addition, evidence suggests that Valerenic acid acts as an agonist for 5-HT receptors (serotonin receptors), which are G-coupled receptors that mediates neuronal activity via regulating cyclic adenosine monophosphate (cAMP) levels2.

    In-vivo studies that conducted on xenograft glioblastoma multiforme (GBM) mice models shown that Valerenic acid induce cell death of GBM cells by inducing AMPK activation. Therefore, Valerenic acid may serve as a potential anti-tumor agent towards GBM patients3.

    Target GABAA receptor
    Last update: 08/11/2021

    Valerenic acid (#V-140) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

    Applications

    Specifications

    Scientific Background

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