Gabazine Explained

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 hyperpolarization. While phasic (synaptic) inhibition is gabazine-sensitive, tonic (extrasynaptic) inhibition is relatively gabazine-insensitive.[3]

Gabazine has been found to bind to and antagonize α4βδ subunit-containing GABAA receptors, which may represent the GHB receptor.[4]

Notes and 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 . The European Journal of Neuroscience . 25 . 7 . 2170–2181 . April 2007 . 17419756 . 10.1111/j.1460-9568.2007.05462.x . 85328190 .
  2. Ueno S, Bracamontes J, Zorumski C, Weiss DS, Steinbach JH . Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor . The Journal of Neuroscience . 17 . 2 . 625–634 . January 1997 . 8987785 . 6573228 . 10.1523/jneurosci.17-02-00625.1997 .
  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 . 63 . 1 . 2–8 . January 2003 . 12488530 . 10.1124/mol.63.1.2 . 6827514 .
  4. Absalom N, Eghorn LF, Villumsen IS, Karim N, Bay T, Olsen JV, Knudsen GM, Bräuner-Osborne H, Frølund B, Clausen RP, Chebib M, Wellendorph P . 6 . α4βδ GABA(A) receptors are high-affinity targets for γ-hydroxybutyric acid (GHB) . Proceedings of the National Academy of Sciences of the United States of America . 109 . 33 . 13404–13409 . August 2012 . 22753476 . 3421209 . 10.1073/pnas.1204376109 . free . 2012PNAS..10913404A .

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Gabazine".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.