SR 95531 hydrobromide (Gabazine)

(HB0901)
Technical documents: SDS CoA Datasheet

Product overview

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

SR 95531 hydrobromide (Gabazine) is a selective and competitive GABAA receptor antagonist (Ki = 150 nM for displacement of [3H]-GABA from rat membranes).


SR 95531 (Gabazine) displaces GABA from the GABAAR agonist binding site to prevent receptor activation. It also acts as a negative allosteric inhibitor of channel opening to inhibit GABAA receptor activation by anaesthetic agents. It also displays low affinity glycine receptor inhibition.


SR 95531 (Gabazine) inhibits GABA-induced Cl- currents to reduce GABA-mediated synaptic inhibition.


SR 95531 additionally shows convulsive actions.

Alternative names Gabazine | GBZ
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

Good compound. This compound is routinely used in our lab to isolate AMPA and NMDA currents. So we are using it a lot every day. There are no complaints about it! Verified customer, Karolinska Institutet

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Biological Data

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.

Solubility & Handling

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.

Calculators

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Dilution

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Chemical Data

Chemical name 6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridazinebutanoic acid hydrobromide
Molecular Weight 368.23
Chemical structure Product image
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

References for SR 95531 hydrobromide (Gabazine)

References are publications that support the biological activity of the product
  • 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.
  • Sequential steps underlying neuronal plasticity induced by a transient exposure to gabazine.

    Pegoraro S et al (2010) J Cell Physiol 222(3) : 713-28.
  • 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.
  • 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.
  • 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.
Publications
These publications cite the use of SR 95531 hydrobromide (Gabazine) purchased from Hello Bio:
  • 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 dop 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

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