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(-)-Bicuculline methochloride

An Antagonist of GABA(A) Receptors
Cat #: B-137
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 417.84
    Purity: >97% (HPLC)
    Effective concentration 1-10 µM.
    Structure
    Chemical name (6R)-6-[(5S)-6,6-dimethyl-7,8-dihydro-5H-[1,3]dioxolo[4,5-g]isoquinolin-6-ium-5-yl]-6H-furo[3,4-g][1,3]benzodioxol-8-one;chloride.
    Molecular formula C21H20ClNO6.
    CAS No.: 53552-05-9.
    PubChem CID 10047593
    Activity (-)-Bicuculline methochloride is a water soluble quaternary salt of Bicuculline, a competitive antagonist of the GABAA receptors (IC50 = 8.4 µM)1. Quaternary salts of Bicuculline were shown to have effects not mediated by GABA receptors2.
    References-Activity
    1. Horne, A.L. et al. (1992) Br. J. Pharmacol107, 732.
    2. Seutin, V. and Johnson S.W. (1999) Trends Pharmacol. Sci. 20, 268.
    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 +4°C.
    Solubility Soluble in water. Centrifuge all product preparations before use (10000 x g, 5 min).
    Storage of solutions Up to three months at -20°C.
    Our bioassay
    • Alomone Labs (-)-Bicuculline methochloride inhibits GABA(A) receptors expressed in Xenopus oocytes.
      Alomone Labs (-)-Bicuculline methochloride inhibits GABA(A) receptors expressed in Xenopus oocytes.
      Time course of GABA(A) α1/β2 currents, activated by a continuous application (top dotted line) of 1 µM γ-Aminobutyric acid (#G-110), and reversibly inhibited by 10 µM (-)-Bicuculline methochloride (#B-137), as indicated (bar), at a holding potential of -60 mV.
    References - Scientific background
    1. Seutin, V. and Johnson S.W. (1999) Trends Pharmacol. Sci. 20, 268.
    2. Pomara, N. et al. (2015) Prog. Neuropsychopharmacol. Biol. Psychiatry 56, 35.
    3. Iqbal, F. et al. (2011) Bioorg. Med. Chem. Lett. 21, 4252.
    Scientific background

    (-)-Bicuculline methochloride is a synthetic compound that acts as water soluble GABA(A) receptor antagonist. The compound is a quaternary salt of bicuculline (BIC), a competitive antagonist of the GABA(A) receptors. (-)-Bicuculline methochloride is more stable at physiological pH and more soluble in aqueous solutions than bicuculline. The compound was shown to affect other neurotransmitter systems such as the cholinergic system1.

    GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. They mediate GABA (gamma-aminobutyric acid) action, a major inhibitory neurotransmitter, through the central nervous system (CNS). They play an important role in inhibiting cell excitation in the CNS. They are considered to be a major target of antiseizure drugs2,3.

    Target GABA(A) receptors
    Last update: 23/11/2020

    (-)-Bicuculline methochloride (#B-137) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

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    Scientific Background

    Citations

    Citations
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