Novel gabaa receptor with steroid binding sites

Details Novel gabaa receptor with steroid binding sites Novel gabaa receptor with steroid binding sites

C - Chemistry, Metallurgy

12

Q

C12Q 1/68 (2006.01) A61K 31/56 (2006.01) C07K 14/705 (2006.01) C07K 14/72 (2006.01) G01N 33/53 (2006.01) G01N 33/566 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2118938

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.

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