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Submit ReviewSR 95531 hydrobromide
Description: Competitive and selective GABAA antagonist
Alternative Names: Gabazine
Chemical Name: 6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridazinebutanoic acid hydrobromide
Purity: ≥98% (HPLC)
Biological Activity for SR 95531 hydrobromide
SR 95531 hydrobromide is a selective, competitive GABAA receptor antagonist and allosteric inhibitor (IC50 = 200 nM). SR 95531 displaces [3H]-GABA from rat brain membranes with a Ki of 150 nM. Unlike Bicuculline (Cat. No. 0130), SR 95531 selectively antagonizes GABA-induced Cl- currents with little action on Pentobarbitone-induced currents (Cat. No. 4579). SR 95531 can act as an agonist at high concentrations (>100 μM) and is a weak agonist at GABAA receptors with α1β2(Y157S)γ2L subunits. SR 95531 also acts as a competitive antagonist of recombinant glycine receptors and exhibits greater potency at glycine receptors containing β subunits.
Compound Libraries for SR 95531 hydrobromide
SR 95531 hydrobromide is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for SR 95531 hydrobromide
| M. Wt | 368.23 |
| Formula | C15H17N3O3.HBr |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 104104-50-9 |
| PubChem ID | 107895 |
| InChI Key | GFZHNFOGCMEYTA-UHFFFAOYSA-N |
| Smiles | Br.COC1=CC=C(C=C1)C1=NN(CCCC(O)=O)C(=N)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SR 95531 hydrobromide
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 9.21 | 25 | |
| DMSO | 36.82 | 100 |
Preparing Stock Solutions for SR 95531 hydrobromide
The following data is based on the product molecular weight 368.23. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.72 mL | 13.58 mL | 27.16 mL |
| 5 mM | 0.54 mL | 2.72 mL | 5.43 mL |
| 10 mM | 0.27 mL | 1.36 mL | 2.72 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets for SR 95531 hydrobromide
References for SR 95531 hydrobromide
References are publications that support the biological activity of the product.
Beato et al (2007) The kinetics of inhibition of rat recombinant heterotrimeric α1β glycine receptors by the low affinity antagonist SR-95531. J.Physiol. 580 171 PMID: 17218350
Heaulme et al (1986) Biochemical characterization of the interaction of three pyridazinyl-GABA derivatives with the GABAA receptor site. Brain Res. 384 224 PMID: 3022866
Uchida et al (1996) The differential antagonism by bicuculline and SR95531 of pentobarbitone-induced currents in cultured hippocampal neurons. Eur.J.Pharmacol. 307 89 PMID: 8831109
Wang and Slaughter (2005) Effects of GABA receptor antagonists on retinal glycine receptors and on homomeric glycine receptor alpha subunits. J.Neurophysiol. 93 3120 PMID: 15728760
Ueno et al (1997) Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor. J.Neurosci. 17 625 PMID: 8987785
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Keywords: SR 95531 hydrobromide, SR 95531 hydrobromide supplier, Selective, competitive, GABAA, antagonists, receptors, SR95531, hydrobromide, gabazine, recombinant, glycine, allosteric, inhibitors, Gabazine, Receptors, Glycine, 1262, Tocris Bioscience
171 Citations for SR 95531 hydrobromide
Citations are publications that use Tocris products. Selected citations for SR 95531 hydrobromide include:
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SR95531 for slice electrophysiology.
By
Anonymous on 01/08/2018
Assay Type: Ex Vivo
Species: Mouse
I use SR95531 to block GABAA channels when performing slice electrophysiology.
I use this at a concentration of 10 uM in my aCSF bath.
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