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3',8''-Biapigenin, Didemethyl-ginkgetin

A Negative Allosteric Modulator of GABA(A) Receptors

Cat #: A-165
Alternative Name 3',8''-Biapigenin, Didemethyl-ginkgetin
Lyophilized Powder yes
  • Bioassay Tested
  • Origin Selaginella tamariscina.
    Source Natural
    MW: 538.46
    Purity: ≥98.5%
    Effective concentration 0.5 nM – 0.5 µM.
    Chemical name 8-[5-(5,7-dihydroxy-4-oxochromen-2-yl)-2-hydroxyphenyl]-5,7-dihydroxy-2-(4-hydroxyphenyl)chromen-4-one.
    Molecular formula C30H18O10.
    CAS No.: 1617-53-4
    PubChem CID 5281600
    Activity Amentoflavone is a negative allosteric modulator of GABA(A) receptor inhibitory activity, with EC50=4 µM on recombinant α1β2γ2L GABA(A) in oocytes1. In vitro, it potently displaces benzodiazepine binding to rat brain membranes with nM affinity2, and inhibits binding at other GPCRs3.
    1. Hanrahan, J.R. et al. (2003) Bioorg. Med. Chem. Lett. 13, 2281.
    2. Nielsen, M. et al. (1988) Biochem. Pharmacol. 37, 3285.
    3. Butterweck, V. et al. (2002) Psychopharmacology (Berl.) 162, 193.
    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 50 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Amentoflavone inhibits specific binding of Flunitrazepam to rat brain GABA(A) receptors.
      Alomone Labs Amentoflavone inhibits specific binding of Flunitrazepam to rat brain GABA(A) receptors.
      Percent inhibition of specific binding of 1 nM [3H]Flunitrazepam to membranes from whole rat brain (except cerebellum) was plotted against concentrations of Amentoflavone (#A-165), (green circles) and of Diazepam (assay standard, black squares) and used to calculate IC50 and Ki values for Amentoflavone (IC50 ≈ 4.95 nM, and Ki ≈ 4.03nM).
    References - Scientific background
    1. Hanrahan, J.R. et al. (2003) Bioorg. Med. Chem. Lett. 13, 2281.
    Scientific background

    Amentoflavone is a natural compound derived from the plant Selaginella tamariscina. It is a negative allosteric modulator of GABA(A) receptors. Amentoflavone can be found in a number of plants with medicinal properties including Ginkgo biloba and Hypercium perforatum. Amentoflavone is the first high affinity ligand known for the benzodiazepine receptor devoid of nitrogen in its structure. It has been hypothesized recently that amentoflavone can cross the blood brain barrier in vivo by passive diffusion. In addition to its effect on GABA receptors, amentoflavone inhibits binding at 5-HT, D3-dopamine and δ-opioid receptors. The action of amentoflavone on the GABA(A) receptor is independent of high affinity benzodiazepine modulatory sites on the receptor. Amentoflavone and other substances of the flavone class have been found to exert anxiolytic activity in mice without the side effect associated with the use of benzodiazepines1.

    Target GABA(A) receptors
    Last update: 08/06/2021

    Amentoflavone (#A-165) is a highly pure, natural, and biologically active compound.

    For research purposes only, not for human use



    Scientific Background


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