2118938 9305786 PCTABS00021 There is disclosed a GABAA receptor-chloride ionophore complex (GRC), where GABA represents gamma-aminobutyric acid, having a novel binding site, the GNR, independent of other known sites on the GRC. There is also disclosed a method for screening for agonists of the GNR by forming an expressed GRC by co-expression cDNA encoding the GRC subunits in cells and determining the ability of a steroid to modulate allosterically benzodiazepine binding to the expressed receptor complex. The figure shows the enhancement of the binding of a benzodiazepine analog to the GRC as a function of the concentration of a steroid modulator which binds to the GNR.
NOVEL GABAA RECEPTOR WITH STEROID BINDING SITES