Product overview

• NameSR 95531 hydrobromide (Gabazine)
• Short descriptionSelective, competitive GABA_A receptor antagonist
• Biological description

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

  Displaces GABA from the GABA_AR agonist binding site to prevent receptor activation. Also acts as a negative allosteric inhibitor of channel opening to inhibit GABA_A 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
• Biological actionAntagonist
• 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

• Our products in action5 citationsSubmit Your Citation Now

Images

Properties

• Chemical name6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridazinebutanoic acid hydrobromide
• Molecular Weight368.23
• Chemical structure
• Molecular FormulaC₁₅H₁₇N₃O₃.HBr
• CAS Number104104-50-9
• PubChem identifier107895
• SMILESCOC1=CC=C(C=C1)C2=NN(C(=N)C=C2)CCCC(=O)O.Br
• SourceSynthetic
• InChiInChI=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
• InChiKeyGFZHNFOGCMEYTA-UHFFFAOYSA-N
• MDL numberMFCD00055135
• AppearanceWhite solid

Applications

• Application notes

  Gabazine (SR 95531) is commonly used to reduce levels of inhibition by antagonising GABA_A 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 GABA_A 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)
• ImportantThis 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