TABLE 1

Potencies of GABA and GS39783 at key mutant GB2 subunits in the [³⁵S]GTPγS binding assay

Concentration-response curves for GABA and GS39783 in the absence or presence of 10 μM GS39783 and 10 μM GABA, respectively, were measured using membranes from transiently transfected HEK293FT cells. Data are shown for wild-type and key mutant rGB2 subunits after coexpression with rGB1 and for individually expressed rGB2 mutants in which agonistic activity of GS39793 was observed. The maximal effects were determined in GABA concentration-response curves in the presence 10 μM GS39783 and are expressed as the percentage of the maximal response obtained with GABA alone. The data are means ± S.E.M. from three to seven independent experiments (triplicate determinations).