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Ginkgolide B

An Antagonist of 5-HT3A Channels

Cat #: G-170
Lyophilized Powder yes
  • Bioassay Tested
  • Origin Ginkgo biloba.
    Source Natural
    MW: 424.4
    Purity: >98%
    Effective concentration 500-1000 µM.
    Structure
    Chemical name ((1R,3R,6R,7S,8S,10R,11R,12R,13S,16S,17R)-8-tert-butyl-6,12,17-trihydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.0^{1,11}.0^{3,7}.0^{7,11}.0^{13,17}]nonadecane-5,15,18-trione.
    Molecular formula C20H24O10.
    CAS No.: 15291-77-7
    PubChem CID 6324617
    Activity Ginkgolide B is a 5-HT3A channel blocker1.
    References-Activity
    1. Tompson, A.J. et al. (2011) Neuropharmacology 60, 488.
    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 200 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 Ginkgolide B blocks 5-HT3A receptors expressed in HEK 293T cells. 
      Alomone Labs Ginkgolide B blocks 5-HT3A receptors expressed in HEK 293T cells. 
      5-HT3A receptor currents were elicited by 10 µM 5-HT, delivered every 3 minutes. Ginkgolide B  (#G-170) was applied 30 seconds before stimulation at 50, 200 and 500 µM,  as indicated and inhibited the 5-HT induced current in a dose dependent and reversible manner.
    References - Scientific background
    1. Hannon, J. et al. (2008) Behav. Brain Res. 195, 198.
    2. Tompson, A.J. et al. (2011) Neuropharmacology 60, 488.
    Scientific background

    Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine neurotransmitter synthesized from the amino acid tryptophan by the enzyme tryptophan-decarboxylase. 5-HT3 channel is a ligand gated ion channel receptor of the cys-loop channel family. It is a pentamer with five subunits surrounding a central channel1.

    Ginkgolide B is a natural non-selective blocker of 5-HT3A channel. Ginkgolide is extracted from the leaves, roots and bark of the tree Ginkgo biloba. Ginkgolide B has an effective concentration of 500-1000 μM and an IC50 of 730 μM for the 5-HT3A receptor and an IC50 of 3.9 mM for the 5-HT3B receptor thus enabling discrimination between the two. Ginkgolide also binds to anion Cys-loop receptors such as GABA and glycine receptors. Ginkgolide does not displace the specific 5-HT3 receptor antagonist granisetron, thus confirming that it does not act at the agonist binding site. In addition, inhibition by Ginkgolide at 5-HT3A receptors is weakly use-dependent, and recovery of the receptor is also activity dependent, indicating channel block as the mechanism of inhibition. Ginkgolide is widely used in traditional medicine and has a wide spectrum of beneficial properties such as anti-convulsion, neuro-protection and reducing anxiety2.

    Target 5-HT3A receptors
    Last update: 12/08/2021

    Ginkgolide B (#G-170) is a highly pure, natural, and biologically active compound.

    For research purposes only, not for human use
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