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Bilobalide

An Antagonist of 5-HT3A and GABA(A) Receptors

Cat #: B-145
Lyophilized Powder yes
  • Bioassay Tested
  • Origin Ginkgo biloba.
    Source Natural
    MW: 326.3
    Purity: >99.5%
    Effective concentration 1-100 µM.
    Structure
    Chemical name (5aR- (3aS*,5aα,8b,8aS*,9a,10aα))- 9-(1,1-dimethylethyl)- 10,10a-dihydro- 8,9-dihydroxy- 4H,5aH,9H-furo[2,3-b]furo[3',2':2,3]cyclopenta[1,2-c]furan- 2,4,7(3H,8H)-trione.
    Molecular formula C15H18O8.
    CAS No.: 33570-04-6
    Activity Bilobalide is a 5-HT3A1 and GABAA2 channel blocker.
    References-Activity
    1. Tompson, A.J. et al. (2011) Neuropharmacology 60, 488.
    2. Huang, S.H. et al. (2003) Eur. J. Pharmacol. 464, 1.
    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 100 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 Bilobalide blocks 5-HT3A receptors expressed in HEK 293T cells. 
      Alomone Labs Bilobalide blocks 5-HT3A receptors expressed in HEK 293T cells. 
      5-HT3A receptor currents were elicited with 10 µM 5-HT, delivered every 3 minutes. Bilobalide (#B-145) was applied 30 seconds before stimulation at 100 and 200 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. Olsen, R.W. et al. (1990) FASEB J. 4, 1469.
    3. Tompson, A.J. et al. (2011) Neuropharmacology 60, 488.
    4. Huang, S.H. et al. (2003) Eur. J. Pharmacol. 464, 1.
    Scientific background

    Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine neurotransmitter synthesized from the amino acid tryptophan by the enzyme tryptophan-decarboxylase. The 5-HT3 channel is a ligand-gated ion channel receptor of the Cys-loop channel family1.

    The GABA(A) receptor is also a ligand-gated ion channel. It is the major receptor type for the GABA inhibitory neurotransmitter in the central nervous system2.

    Bilobalide is a natural non-selective blocker of the 5-HT3A and GABA(A) channels. Bilobalide is a sesquiterpene trilactone extracted from the leaves of the tree Ginkgo biloba. Bilobalide has an effective concentration of 1-100 μM and an IC50 of 470 μM for the 5-HT3A receptor3 and an IC50 of 4.6±0.5 μM for the GABA(A) receptor. Bilobalide also binds to other anion Cys-loop receptors such as glycine receptors with a much higher affinity than to the 5-HT3A receptor.

    Bilobalide inhibits direct GABA mediated currents from recombinant human GABA(A) receptors thus suggesting it enhances neuronal excitability. Bilobalide is used in traditional Japanese medicine as a memory enhancer, treating symptoms associated with mild-moderate dementia and improving cognitive functions related to old age and senility3.

    Target 5-HT3A, GABA(A) receptors
    Last update: 25/07/2021

    Bilobalide (#B-145) is a highly pure, natural, and biologically active compound.

    For research purposes only, not for human use
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