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).
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| 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)
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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. |
Chemical Data
| Chemical name | 6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridazinebutanoic acid hydrobromide |
| Molecular Weight | 368.23 |
| Chemical structure |  |
| 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)
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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.
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Presynaptic inhibition upon CB1 or mGlu2/3 receptor activation requires ERK/MAPK phosphorylation of Munc18-1.
Schmitz et al (2016) EMBO J. 35(11) : 1236-50PubMedID: 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) : 3236PubMedID: 28607399
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