Biological Activity
Selective, competitive GABAA receptor antagonist. Displaces [3H]-GABA from rat brain membranes with a Ki of 150 nM. Unlike bicuculline, selectively antagonizes GABA-induced Cl- currents with little action on pentobarbitone-induced currents. Also acts as a low affinity glycine receptor antagonist.
Compound Libraries
SR 95531 hydrobromide is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 368.23 |
| Formula | C15H17N3O3.HBr |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 104104-50-9 |
| PubChem ID | 11056106 |
| InChI Key | VVDXNJRUNJMYOZ-DHXVBOOMSA-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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| phosphate buffered saline | 1.84 | 5 | |
| DMSO | 36.82 | 100 | |
| ethanol | 7.36 | 20 | |
| water | 9.21 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 368.23. Batch specific molecular weights may vary from batch to batch due to solvent 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
References
References are publications that support the products' biological activity.
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
Keywords: SR 95531 hydrobromide, supplier, Selective, competitive, GABAA, receptor, antagonists, Receptors, SR95531, hydrobromide, Gabazine, GABAA, Receptors, GABAA, Receptors, Tocris Bioscience
