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Category: Ion ChannelsarrowLigand-gated Ion ChannelsarrowGABAA and GABAC ReceptorsarrowGABAA ReceptorsarrowAntagonists
Cat.No. Product Name
1262 SR 95531 hydrobromide
Alternative name(s): Gabazine
Price and Availability

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SR 95531 hydrobromide
Chemical Name: 6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridazinebutanoic acid hydrobromide

Biological Activity:

Selective, competitive GABAA receptor antagonist.  Displaces [3H]-GABA from rat brain membranes with a Ki of 150 nM. Unlike bicuculline, selectively antagonises GABA-induced Cl- currents with little action on pentobarbitone-induced currents.

Technical Data:

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M.Wt: 368.23
Formula: C15H17N3O3.HBr
Storage: Store at RT
Solubility: Soluble to 25 mM in Water and to 5 mM in Phosphate buffered saline and to 100 mM in DMSO
Purity: >98%
CAS No: [104104-50-9]

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    References:

    Wermuth et al (1987) Synthesis and structure-activity relationships of a series of aminopyridazine derivatives of γ-aminobutyric acid acting as selective GABA-A antagonists. J.Med.Chem. 30 239. Luddens and Korpi (1995) GABAA antagonists differentiate between recombinant GABAA/benzodiazepine receptor subtypes. J.Neurosci. 15 6957. Ito et al (1992) Characterization of antagonistic activity and binding properties of SR95531, a pyridazinyl-GABA derivative in rat brain and cultured cerebellar neuronal cells. Synapse 10 326. Uchida et al (1996) The differential antagonism by bicuculline and SR95531 of pentobarbitone-induced currents in cultured hippocampal neurons. Eur.J.Pharmacol. 307 89.
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    Keywords: SR 95531 Hydrobromide, Ligand-gated Ion Channels, Selective, Competitive GABAA Receptor Antagonist, Gabazine, SR95531 Hydrobromide, Tocris Bioscience
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