Gabazine

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Gabazine
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Identifiers
CAS Number
PubChem CID
E number{{#property:P628}}
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Chemical and physical data
FormulaC15H18BrN3O3
Molar mass368.226

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.[1]

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.

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