Gabazine

Drugbox
IUPAC_name = 4- [6-imino-3-(4-methoxyphenyl)pyridazin-1-yl] butanoic acid hydrobromide


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CAS_number=104104-50-9
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PubChem=107895
DrugBank=
C=15 | H=18 | Br=1 | N=3 | O=3
molecular_weight = 368.226
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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. [Behrens CJ, van den Boom LP, Heinemann U. Effects of the GABA(A) receptor antagonists bicuculline and gabazine on stimulus-induced sharp wave-ripple complexes in adult rat hippocampus in vitro. "European Journal of Neuroscience" 2007 Apr;25(7):2170-81.]

Gabazine binds to the GABA recognition site of the receptor-channel complex and acts as an allosteric inhibitor of channel opening. [Ueno S, Bracamontes J, Zorumski C, Weiss DS, Steinbach JH. Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor. "Journal of Neuroscience" 1997 Jan 15;17(2):625-34.] The net effect is to reduce GABA-mediated synaptic inhibition by inhibiting chloride flux across the cell membrane, and thus inhibiting neuronal depolarisation. While phasic (synaptic) inhibition is gabazine-sensitive, tonic (extrasynaptic) inhibition is gabazine-insensitive. [Yeung JY, Canning KJ, Zhu G, Pennefather P, MacDonald JF, Orser BA. Tonically activated GABAA receptors in hippocampal neurons are high-affinity, low-conductance sensors for extracellular GABA. "Molecular Pharmacology" 2003 Jan;63(1):2-8.]

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