GABAA receptor

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GABAA receptors, which are considered ligand-gated ion channels as the binding of GABA results in the opening of ion channels leading to the inhibition of a neuronal signal. Excitatory neurosteroids have excitatory effects on neurotransmission. They act as potent negative allosteric modulators of the GABAA receptor. Major examples include the pregnanes pregnenolone sulfate (PS), epipregnanolone, and isopregnanolone (sepranolone).

  • Pregnenolone alone.
  • Pregnanolone binds beta3-alpha5 GABAA receptor (5o8f).
  • Pregnanolone binding site is situated between 2 monomers.

See also:

PDB ID 5o8f

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GABAA receptor 3D structures

See GABA receptor 3D structures

References

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Alexander Berchansky, Michal Harel

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