A Potent Antagonist of GABA(A) Receptors
    Cat #: B-135
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 367.4
    Purity: >99% (HPLC)
    Effective concentration 1-100 µM.
      • (+)-Bicuculline
    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.
      • 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.
      • (+)-Bicuculline
        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
      • 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: 24/01/2020

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

    For research purposes only, not for human use
      • Tang, Y. et al. (2018) Eur. J. Neurosci. 47, 866.
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