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A Potent Antagonist of GABA(A) Receptors

Cat #: B-135
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 367.4
    Purity: >99% (HPLC)
    Effective concentration 1-100 µM.
    Chemical name [R-(R*,S*)]-6-(5,6,7,8-Tetrahydro-6-methyl-1,3-dioxolo[4,5-g]isoquinolin-5-yl)furo[3,4-e]-1,3-benzodioxol-8(6H)-one.
    Molecular formula C20H17NO6.
    CAS No.: 485-49-4
    Activity (+)-Bicuculline inhibits (IC50 = 9 µM) recombinant α1β1γ2 GABA(A) channels that were activated with 3 µM GABA1.
    1. Horne, A.L. et al. (1992) Br. J. Pharmacol. 107, 732.
    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 DMSO (with gentle warming), DMF, chloroform. 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 (+)-Bicuculline inhibits GABA(A) α2/β1/γ2 currents activated by γ-Aminobutyric acid in heterologously expressing Xenopus oocytes.
      Alomone Labs (+)-Bicuculline inhibits GABA(A) α2/β1/γ2 currents activated by γ-Aminobutyric acid in heterologously expressing Xenopus oocytes.
      Time course of γ-Aminobutyric acid (#G-110) (100 µM) activated GABA(A) α2/β1/γ2 currents and their inhibition by 20 µM (+)-Bicuculline (#B-135), which was perfused for 100 seconds as indicated by the horizontal bar. Holding membrane potential was -60 mV and γ-aminobutyric acid was applied every 100 seconds.
    References - Scientific background
    1. Briggs, S.W. and Galanopoulou, A.S. (2011) Neural Plast. 2011, 527605.
    2. Khakhalin, A.S. (2011) J. Neurophysiol. 106, 1065.
    3. Esmaeili, A. et al. (2009) J. Neurophysiol. 101, 341.
    4. Ueno, S. et al. (1997) J. Neurosci. 17, 625.
    5. Walker, J. et al. (2012) PLoS One 7, e31415.
    6. Paine, T.A. et al. (2011) Neuropsychopharmacology 36, 1703.
    Scientific background

    γ-Aminobutyric acid (GABA) is an amino acid derivate, synthesized from glutamate by the pyridoxal-L-phosphate (PLP)-dependent enzyme, glutamate decarboxylase (GAD)1. GABA provides the primary inhibitory signaling in the adult mammalian brain (CNS), and, to some degree of controversy, exerts a depolarizing response in the developing brain2.

    GABA is an agonist of two main receptor classes in the CNS: GABAA, an ionic ligand-gated channel, and GABAB, a metabotrophic, G-protein coupled receptor. GABAA is assembled by 5 out of 16 possible subunits with α, β and either a γ or a δ (2:2:1 stoichiometry) being the most common. With an EC50 between 3 to 12 μM it interacts with GABA to allow either an influx or an efflux of Cl- ions into and out of the cell, respectively3.

    Bicuculline (BIC) is a competitive allosteric inhibitor of GABAA-induced currents with an IC50 of 1-3 μM4. BIC has been employed to model epileptic seizures in hippocampal slices5, to induce schizophrenia-like symptoms in the pre-frontal cortex6, and is an essential research tool in the study of various psychomotor and behavioral defects4-6.

    Target GABA(A) receptors
    Last update: 06/11/2022

    (+)-Bicuculline (#B-135) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use



    Product citations
    1. Tang, Y. et al. (2018) Eur. J. Neurosci. 47, 866.


    Scientific Background

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