gabazine bromide

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Research

27 papers

Central GABAA and GABAB receptor modulation of basal and stress-induced plasma interleukin-6 levels in mice.The Journal of pharmacology and experimental therapeutics · 1998
Subtype specificity of gamma-aminobutyric acid type A receptor antagonism by clozapine.Naunyn-Schmiedeberg's archives of pharmacology · 1995
GABAA receptor antagonism in the extended amygdala decreases ethanol self-administration in rats.European journal of pharmacology · 1995
The differential antagonism by bicuculline and SR95531 of pentobarbitone-induced currents in cultured hippocampal neurons.European journal of pharmacology · 1996
Evidence for a non-GABAergic action of quaternary salts of bicuculline on dopaminergic neurones.Neuropharmacology · 1997

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Wikidata facts

Mass: 367.053

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chemical formula: C₁₅H₁₈BrN₃O₃
canonical SMILES: COC1=CC=C(C=C1)C2=NN(C(=N)C=C2)CCCC(=O)O.Br
Commons category: Gabazine

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Contents

References

Gabazine (SR-95531) is a drug that acts as an antagonist at GABAA receptors. It is used in scientific research and has no role in medicine, as it would be expected to produce convulsions if used in humans.

Gabazine binds to the GABA recognition site of the receptor-channel complex and acts as an allosteric inhibitor of channel opening. The net effect is to reduce GABA-mediated synaptic inhibition by inhibiting chloride flux across the cell membrane, and thus inhibiting neuronal hyperpolarization. While phasic (synaptic) inhibition is gabazine-sensitive, tonic (extrasynaptic) inhibition is relatively gabazine-insensitive.