Featured Review Cellscience Reviews Vol 3 No 4 ISSN 1742-8130

Neurosteroid interactions with the GABA_A receptor

The mammalian nervous system relies on multiple effects of various steroids that are synthesized in the brain and produce rapid, non-genomic actions on ligand- and voltage-gated channels. The GABAA receptor has attracted intensive research efforts as an important target of neurosteroids as this receptor is the key player in regulating neuronal inhibition and often provides a link to the pathophysiology of mental disorders. Two different binding sites have recently been mapped to the receptor’s transmembrane domains, one of them mediating the modulatory effects on GABA elicited currents, the other responsible for the direct activation of the channel by neurosteroids. As the effects depend not only on the type of steroid, but also on the GABA receptor subunit composition and post-translational modifications, a detailed understanding of the molecular and subcellular determinants is necessary to develop new strategies in the management of pathological states.

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