SR95531 (Gabazine), GABAA antagonist (ab120042)
- Datasheet
- References (111)
Overview
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Product name
SR95531 (Gabazine), GABAA antagonist -
Description
GABAA antagonist -
Alternative names
- Gabazine
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Biological description
Selective, competitive GABAA receptor antagonist. Allosteric inhibitor of channel opening of the GABAA receptor. Displaces [3H]-GABA from rat brain membranes with a Ki of 150 nM.
Also available in simple stock solutions (ab144487) - add 1 ml of water to get an exact, ready-to-use concentration. -
Purity
> 98% -
CAS Number
104104-50-9 -
Chemical structure
Properties
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Chemical name
2-(3-Carboxypropyl)-3-amino-6-(4 methoxyphenyl)pyridazinium bromide -
Molecular weight
368.23 -
Molecular formula
C15H17N3O3.HBr -
PubChem identifier
107895 -
Storage instructions
Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months. -
Solubility overview
Soluble in water to 25 mM -
Handling
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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SMILES
[Br-].COc1ccc(cc1)C=2C=CC(=[NH2+])N(CCCC(=O)O)N=2 -
Source
Synthetic
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Research areas
Associated products
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Related Products
Images
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Other - SR95531 (Gabazine), GABAA antagonist (ab120042)Image from Maher BJ, LoTurco JJ, Plos One, 7(3), e34053. Fig 1,; doi: 10.1371/journal.pone.0034053Expression of DISC1ΔC is induced by postnatal administration of 4-OHT as seen by expression of GFP fused to DISC1ΔC in this P28 brain slice. No GFP expression is observed in vehicle treated animals (- 4-OHT). Scale bar equals 100 µm. Performed in the presence of gabazine (5 µM) and TTX (1 µM).
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Functional Studies - SR95531 (Gabazine), GABAA antagonist (ab120042)Image from Brady JD et al., Neuroscience. 2010;168(1):108-17. Fig 3.; doi: 10.1016/j.neuroscience.2010.03.009 with permission from Elsevier.A. Purkinje cell response to simulated ischemia (OGD only) in the continuous presence of the GABAA antagonist GABAzine (ab120042, 10 μM), and during subsequent block of glutamate receptors with AP5 (ab120003, 50 μM) + NBQX (ab120045, 25 μM). B. Bar charts summarize the timing and magnitude of ischemia-induced glutamate currents (for both methods of simulating ischemia) with and without GABAA receptors blocked. Iglu is the magnitude of current blocked by AP5 (ab120003, 50 μM) + NBQX (ab120045, 25 μM).
References
This product has been referenced in:
- Ueno S et al. Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor. J Neurosci 17:625-34 (1997). Read more (PubMed: 8987785) »
- Ito Y et al. Characterization of antagonistic activity and binding properties of SR 95531, a pyridazinyl-GABA derivative, in rat brain and cultured cerebellar neuronal cells. Synapse 10:326-33 (1992). Read more (PubMed: 1585261) »
- Wermuth CG et al. Synthesis and structure-activity relationships of a series of aminopyridazine derivatives of gamma-aminobutyric acid acting as selective GABA-A antagonists. J Med Chem 30:239-49 (1987). Read more (PubMed: 3027337) »
