SR 95531 hydrobromide

Product Description

SR 95531 hydrobromide is a selective, competitive GABA_A receptor antagonist and allosteric inhibitor (IC₅₀ = 200 nM). SR 95531 displaces [³H]-GABA from rat brain membranes with a K_i 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 GABA_A 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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Bright and Smart Methods for recording and measuring tonic GABAA receptor-mediated inhibition. Front.Neural Circuits 2013 PMID: 24367296
• Ueno Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor. J.Neurosci. 1997 PMID: 8987785
• Wang and Slaughter Effects of GABA receptor antagonists on retinal glycine receptors and on homomeric glycine receptor alpha subunits. J.Neurophysiol. 2005 PMID: 15728760
• Uchida The differential antagonism by bicuculline and SR95531 of pentobarbitone-induced currents in cultured hippocampal neurons. Eur.J.Pharmacol. 1996 PMID: 8831109
• Heaulme Biochemical characterization of the interaction of three pyridazinyl-GABA derivatives with the GABA_A receptor site. Brain Res. 1986 PMID: 3022866
• Beato The kinetics of inhibition of rat recombinant heterotrimeric α1β glycine receptors by the low affinity antagonist SR-95531. J.Physiol. 2007 PMID: 17218350