SR 95531 hydrobromide (Gabazine)

(HB0901)

Product overview

  • Name
    SR 95531 hydrobromide (Gabazine)
  • Short description
    Selective, competitive GABAA receptor antagonist
  • Biological description

    Selective and competitive GABAA receptor antagonist (Ki = 150 nM for displacement of [3H]-GABA from rat membranes).


    Displaces GABA from the GABAAR agonist binding site to prevent receptor activation. Also acts as a negative allosteric inhibitor of channel opening to inhibit GABAA receptor activation by anaesthetic agents.


    Inhibits GABA-induced Cl- currents to reduce GABA-mediated synaptic inhibition.


    Also displays low affinity glycine receptor inhibition.


    Shows convulsive actions.

  • Alternative names
    Gabazine | GBZ
  • Biological action
    Antagonist
  • Purity
    >98%
  • Customer comments

    We regularly use Hello Bio Gabazine (SR 95531) in the lab.We especially like the formulation where you only need to add 1ml of water to make a 10mM stock solution. Verified customer, The University of Newcastle

    I am satisfied with the quality, quick delivery and follow-up of your product. Verified customer, Shimane University

    We used our first aliquot of SR95531 (Gabazine) last week. The experiment was a critical one for us and the SR95531 worked exactly as expected – 100% block of a GABAergic IPSP (inhibitory postsynaptic potential). Verified customer, University of Michigan

  • Citations

Images

Properties

  • Chemical name
    6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridazinebutanoic acid hydrobromide
  • Molecular Weight
    368.23
  • Chemical structure
    SR 95531 hydrobromide (Gabazine)  [104104-50-9]
  • Molecular Formula
    C15H17N3O3.HBr
  • CAS Number
    104104-50-9
  • PubChem identifier
    107895
  • SMILES
    COC1=CC=C(C=C1)C2=NN(C(=N)C=C2)CCCC(=O)O.Br
  • Source
    Synthetic
  • InChi
    InChI=1S/C15H17N3O3.BrH/c1-21-12-6-4-11(5-7-12)13-8-9-14(16)18(17-13)10-2-3-15(19)20;/h4-9,16H,2-3,10H2,1H3,(H,19,20);1H
  • InChiKey
    GFZHNFOGCMEYTA-UHFFFAOYSA-N
  • MDL number
    MFCD00055135
  • Appearance
    White solid

Applications

  • Application notes

    Gabazine (SR 95531) is commonly used to reduce levels of inhibition by antagonising GABAA receptors. It is commonly used at concentrations between 10 – 200 μM.

    Gabazine (SR 95531) from Hello Bio blocks spontaneous inhibitory post synaptic currents (IPSC) and evoked IPSCs (see Fig 1 above). It was effective at 1 μM and completely blocked GABAA receptors at 20 μM.

     

    #Protocol 1: Evoked and spontaneous inhibitory post synaptic currents (IPSCs)

    • Whole cell voltage clamp recordings were obtained from layer V neurons of the mouse prelimbic cortex brain slice.
    • A stimulating electrode was placed in layers II/III and IPSCs were evoked by a single square (150 μs) pulse every 10 sec at a stimulus intensity that gave a reliable IPSC.
    • IPSCs were evoked at a range of neuron holding voltages to measure the reversal potential of the current to ensure it was GABAergic.
    • Neurons were held at 0mV and IPSCs continuously stimulated and recorded in response to 5 min applications of varying concentrations of Gabazine until complete receptor inhibition.
    • Spontaneous IPSCs were recorded before and after addition of Gabazine by holding the neuron at 0mV and recording for 10 sec.
    • All recordings for IPSCs were made in the presence of AMPAR antagonists.

Storing and Using Your Product

  • Storage instructions
    Room temperature
  • Solubility overview
    Soluble in water (25mM) and in DMSO (100mM)
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

References for SR 95531 hydrobromide (Gabazine)

  • Biochemical characterization of the interaction of three pyridazinyl-GABA derivatives with the GABAA receptor site.

    Heaulme M et al (1986) Brain Res 384(2) : 224-31.
    PubMedID: 3022866
  • Sequential steps underlying neuronal plasticity induced by a transient exposure to gabazine.

    Pegoraro S et al (2010) J Cell Physiol 222(3) : 713-28.
    PubMedID: 20027606
  • The kinetics of inhibition of rat recombinant heteromeric alpha1beta glycine receptors by the low-affinity antagonist SR-95531.

    Beato M et al (2007) J Physiol 580(Pt 1) : 171-9.
    PubMedID: 17218350
  • The differential antagonism by bicuculline and SR95531 of pentobarbitone-induced currents in cultured hippocampal neurons.

    Uchida I et al (1996) Eur J Pharmacol 307(1) : 89-96.
    PubMedID: 8831109
  • Tonically activated GABAA receptors in hippocampal neurons are high-affinity, low-conductance sensors for extracellular GABA.

    Yeung et al (2003) Mol Pharmacol 36(1) : 2-8.
    PubMedID: 12488530
The following papers have cited the use of SR 95531 hydrobromide (Gabazine) (HB0901) from Hello Bio. If you have published a paper using this product, and it is not shown here, then please tell us! We will send you a free gift as a thank you!
  • Presynaptic inhibition upon CB1 or mGlu2/3 receptor activation requires ERK/MAPK phosphorylation of Munc18-1.

    Schmitz et al(2016) EMBO J. 35(11) : 1236-50
    PubMedID: 27056679
  • Calcium Release from Stores Inhibits GIRK.

    Kramer and Williams(2016) Cell Rep. 3246-3255 : 17(12)
    PubMedID: 28009293
  • New roles for metabotropic glutamate receptor signaling in the physiology and pathology of dopamine neurons

    Kramer, P(2016) Scholar Archive : 3872
  • Context-Dependent Modulation of Excitatory Synaptic Strength by Synaptically Released Zinc

    Kalappa and Tzounopoulos(2017) eNeuro 10.1523 : 0011-17
  • RIM1/2 in retinal ganglion cells are required for the refinement of ipsilateral axons and eye-specific segregation.

    Assali et al(2017) Sci Rep. 7(1) : 3236
    PubMedID: 28607399

Reviews & Product Guides

Reviews

  • Verified customer, University of Michigan

    We used our first aliquot of SR95531 (Gabazine) last week. The experiment was a critical one for us and the SR95531 worked exactly as expected – 100% block of a GABAergic IPSP (inhibitory postsynaptic potential).
  • Verified customer, Shimane Universiy

    I am satisfied with the quality, quick delivery and follow-up of your product.
  • Verified customer, The University of Newcastle

    We regularly use Hello Bio Gabazine in the lab.We especially like the formulation where you only need to add 1ml of water to make a 10mM stock solution.