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Gabazine

SR 95531
An Antagonist of GABA(A) and Glycine Receptors
Cat #: G-215
Alternative Name SR 95531
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 287.32
    Purity: >98% (HPLC)
    Effective concentration 0.1-10 µM.
    Structure
    Chemical name 4-[6-imino-3-(4-methoxyphenyl)pyridazin-1-yl]butanoic acid.
    Molecular formula C15H17N3O3.
    CAS No.: 105538-73-6.
    PubChem CID 107896
    Activity Gabazine is a competitive antagonist of the GABA(A) receptor, selectively inhibiting GABA-evoked currents (IC50 = 0.44 µM), but not currents evoked by pentobarbiton and etomidate1. It is also a low-affinity glycine receptor antagonist (KB = 191 µM)2.
    References-Activity
    1. Uchida, I. et al. (1996) Eur. J. Pharmacol. 307, 89.
    2. Beato, M. et al. (2007) J. Physiol. 580, 171.
    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 Soluble in methanol. 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 Gabazine inhibits GABA(A) receptors expressed in Xenopus oocytes.
      Alomone Labs Gabazine 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 0.1 µM γ-Aminobutyric acid (#G-110), and inhibited by 1 µM Gabazine (#G-215), as indicated, while membrane potential was held at -60 mV.
    References - Scientific background
    1. Uchida, I. et al. (1996) Eur. J. Pharmacol. 307, 89.
    2. Beato, M. et al. (2007) J. Physiol. 580, 171.
    3. Heaulme, M. et al. (1986) Brain Res. 384, 224.
    4. Pomara, N. et al. (2015) Prog. Neuropsychopharmacol. Biol. Psychiatry. 56, 35.
    5. Iqbal, F. et al. (2011) Bioorg. Med. Chem. Lett. 21, 4252.
    Scientific background

    Gabazine (SR-95531) is a specific, competitive and potent antagonist of GABA(A) receptors. The compound also blocks glycine receptors but with lower affinity. SR-95531 acts as an allosteric inhibitor of GABA(A) receptor channel opening1,2 and blocks GABA-evoked currents with an IC50 of 0.44 µM1. When SR 95531 was administered intravenously it was shown to cause seizures in mice3.

    GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. They mediate the GABA action, a major inhibitory neurotransmitter, throughout the central nervous system (CNS) and play an important role in inhibiting cell excitation in the CNS. The GABA(A) receptor is considered to be a major target of anti-seizure drugs4,5.

    Target GABA(A), Glycine receptors
    Last update: 23/08/2020

    Gabazine (#G-215) 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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