Gabazine hydrobromide

SR 95531 hydrobromide
An Antagonist of GABA(A) and Glycine Receptors
    Cat #: G-216
    Alternative Name SR 95531 hydrobromide
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 368.23
    Purity: >99% (HPLC)
    Effective concentration 0.1-1 µM.
      • Gabazine hydrobromide
    Chemical name 4-[6-imino-3-(4-methoxyphenyl)pyridazin-1-yl]butanoic acid;hydrobromide.
    Molecular formula C15H17N3O3•HBr.
    CAS No.: 104104-50-9.
    PubChem CID 107895
    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.
      • Uchida, I. et al. (1996) Eur. J. Pharmacol. 307, 89.
      • 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 water, DMSO and methanol. Centrifuge all product preparations before use (10000 x g, 5 min).
    Storage of solutions Up to three months at -20°C.
      • Gabazine hydrobromide
        Alomone Labs Gabazine hydrobromide inhibits GABA(A) receptors expressed in Xenopus oocytes.
        Time course of GABAA α1/β2 currents, activated by a continuous application (top dotted line) of 1 µM γ-Aminobutyric acid (#G-110), and reversibly inhibited by 0.1 µM and 1 µM Gabazine hydrobromide (#G-216), as indicated (bars), at a holding potential of -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.
      • 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: 24/01/2020

    Gabazine hydrobromide (#G-216) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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