SR-95531 Chemical Properties

Melting point:

200 °C(Solv: ethanol (64-17-5))

storage temp. 

Store at RT

solubility 

DMSO: 30 mg/mL

form 

solid

color 

white

Water Solubility 

water: 25mM

Safety Information

WGK Germany 

3

MSDS

• Language:English Provider:SigmaAldrich

SR-95531 Usage And Synthesis

Description

SR 95531 is a derivative of γ-aminobutyric acid (GABA) that acts as an antagonist of GABA_A receptors (K_i = 74-150 nM). When administered intravenously, it elicits seizures in mice. SR 95531 differs in action from bicuculline in that it antagonizes GABA-induced chloride currents but not those induced by pentobarbitone. It is effective against GABA_A receptor isoforms from mice, rats, and humans.

Uses

Gabazine Hydrobromide is a specific GABA receptor antagonist. Does not affect GABA-transaminase or glutamate-decarboxylase activitites.

Biological Activity

Selective, competitive GABA A receptor antagonist. Displaces [ 3 H]-GABA from rat brain membranes with a K i 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.

Biochem/physiol Actions

SR-95531 is a specific GABAA receptor antagonist that does not affect GABA-transaminase or glutamate-decarboxylase activities.

storage

Room temperature

References

[1] MICHEL HEAULME . Biochemical characterization of the interaction of three pyridazinyl-GABA derivatives with the GABAA receptor site[J]. Brain Research, 1986, 384 2: Pages 224-231. DOI: 10.1016/0006-8993(86)91158-3
[2] ANITA MELIKIAN. Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists[J]. Journal of Medicinal Chemistry, 1992, 35 22: 4092-4097. DOI: 10.1021/jm00100a015
[3] DORTE KREHAN. Potent 4-Arylalkyl-Substituted 3-Isothiazolol GABAA Competitive/Noncompetitive Antagonists: Synthesis and Pharmacology[J]. Journal of Medicinal Chemistry, 2006, 49 4: 1388-1396. DOI: 10.1021/jm050987l
[4] ICHIRO UCHIDA  Jay Y  Ismar N Cestari. The differential antagonism by bicuculline and SR95531 of pentobarbitone-induced currents in cultured hippocampal neurons[J]. European journal of pharmacology, 1996, 307 1: Pages 89-96. DOI: 10.1016/0014-2999(96)00156-2
[5] SURESH K MENDU. Different subtypes of GABA-A receptors are expressed in human, mouse and rat T lymphocytes.[J]. PLoS ONE, 2012: e42959. DOI: 10.1371/journal.pone.0042959

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