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GABA A receptors are important for inhibition in the CNS where neurosteroids and protein kinases are potent endogenous modulators. Acting individually, these can either enhance or depress receptor function, dependent upon the type of neurosteroid or kinase and the receptor subunit combination. However, in vivo, these modulators probably act in concert to fine-tune GABA A receptor activity...
This study addresses whether the potentiation site for neurosteroids on GABA A receptors is conserved amongst different GABA A receptor isoforms. The neurosteroid potentiation site was previously identified in the α1β2γ2S receptor by mutation of Q241 to methionine or leucine, which reduced the potentiation of GABA currents by the naturally occurring neurosteroids, allopregnanolone...
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