SR 95531 hydrobromide

Name: SR 95531 hydrobromide
Brand: Tocris Bioscience
SKU: 1262
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 1262

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Citations (268)

COA / SDS

Competitive and selective GABAA antagonist

Key Product Details

Description:	Competitive and selective GABA_A antagonist
Alternative Names:	Gabazine
Chemical Name:	6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridazinebutanoic acid hydrobromide
Purity:	≥98% (HPLC)
Molecular Weight:	368.23

View Full Technical Details for SR 95531 hydrobromide

Technical Data
Citations / Reviews (1)

Biological Activity for SR 95531 hydrobromide

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.

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 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.

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

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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References for SR 95531 hydrobromide

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