Figure 7.
The same residues confer differences in the kinetics and potency of allosteric modulation by LY404187. The concentration-response profile for LY404187 (0.1-30 μm) potentiation of 10 sec glutamate (100 μm) applications from HEK 293 cells expressing GluR2i, GluR2o, GluR2io,o,V779L,i, or GluR2oo,i,o were acquired. Because all of the mutated receptors were expressed in Flp-In -293 cells (catalog #R750-07; Invitrogen, Carlsbad, CA), for these potency studies, all of the receptors compared were expressed in these cells. The plot of the average EC50 for these four receptors is shown. Error bars represent the mean ± SEM; n = 10-20 (F(3,81) = 8.54; p < 0.0001).