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S246 and E465 of GB1 are critical for agonist potency at the heteromeric GABAB receptor. The effect of increasing concentrations of GABA on IP formation in cells coexpressing the wild-type (WT; ●), S246A (○), E465A (■), E465D (▵), or E465S (▴) GB1 subunit with the wild-type GB2 and Gαqi9 is shown. Data are expressed as the IP production over the radioactivity remaining in the membrane and are means ± SEM of triplicate determinations from a typical experiment.
