Heterogeneity Of Neurosteroid Binding Sites

A number of studies indirectly suggest that the neurosteroids differentiate between GABAA receptor isoforms. The evidence includes: multiphasic concentration-response curves for some steroids in both ligand binding and functional assays; the demonstration that the influence of neurosteroids in both radioligand binding and Cl- flux assays is brain region-dependent and the effect of binary combinations of certain steroids on the binding of [35S]TBPS and [3H] flunitrazepam to rat brain membranes (30-32). However, studies investigating the interaction of neurosteroids with recombinant receptors have provided a somewhat confusing picture. In the interests of clarity, the following discussion will be restricted mainly to functional (electrophysiological) assays.

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