Gabazine

Gabazine (SR-95531) is a drug that acts as an antagonist at GABA_A 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.^[1]

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Gabazine binds to the GABA recognition site of the receptor-channel complex and acts as an allosteric inhibitor of channel opening.^[2] 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.^[3]

References

1. ^ 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.
2. ^ 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.
3. ^ 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.