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.
    Structure
    • 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.
    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 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.
    Our bioassay
    • 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.
    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: 24/01/2020

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

    For research purposes only, not for human use

    Applications

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    Scientific Background

    Citations

    Citations
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