TABLE 2 

Structural determinants of PYD action within the GluN2C ATD-S1 interface pocket

EC50 (95% CI)MaximumN
μM%
WT GluN2C16 (15, 17)257 ± 3.820
GluN2C-W162FN.D.N.D.9
GluN2C-S163Y25 (24, 26)*280 ± 8.110
GluN2C-R194I21 (20, 23)*250 ± 3.09
GluN2C-R194K8.0 (7, 9)*246 ± 5.08
GluN2C-D220RN.D.N.D.14
GluN2C-G249D13 (11, 15)*200 ± 3.610
GluN2C-G425F18 (17, 19)252 ± 6.711
GluN2C-V431F36 (34, 39)*258 ± 9.19
GluN2C-Y473F34 (32, 36)*258 ± 5.012
GluN2C-Y473I39 (29, 47)*228 ± 9.58
  • * P < 0.05 for log EC50 values compared with same day controls (ANOVA, Bonferroni post-hoc test; F8,86 = 97.14). Power to detect an effect size of 0.5 was 0.94.

  • Concentration-effect curves for PYD-106 were generated for GluN2C mutations and fitted by the Hill equation (see Materials and Methods). The mean EC50 and mean fitted maximum response as a percent of control (95% CI determined from log EC50) are given. N is the number of oocytes, which were isolated from two to four different frogs. N.D., the EC50 could not be determined because either there was no effect of PYD-106 or the maximal potentiation was not obtained in the concentration range tested.