NameSR 95531 hydrobromide (Gabazine)
Short descriptionSelective, competitive GABAA receptor antagonist
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 namesGabazine | GBZ
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
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Chemical name6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridazinebutanoic acid hydrobromide
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 instructionsRoom temperature
Solubility overviewSoluble in water (25mM) and in DMSO (100mM)
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
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 dopamine neuronsKramer, P(2016) Scholar Archive : 3872
Context-Dependent Modulation of Excitatory Synaptic Strength by Synaptically Released ZincKalappa and Tzounopoulos(2017) eNeuro 10.1523 : 0011-17
Reviews & Product Guides
- 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).
- I am satisfied with the quality, quick delivery and follow-up of your product.
- 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.