Table 7. Pharmacology and response time course for substitution of GluN2A-ProP552 with Ala, Gly, Lys, Gln, Ile, or Leu.
| WT 2A | P552Q | P552K | WT 2A | P552G | P552A | P552I | P552L | |
|---|---|---|---|---|---|---|---|---|
| Glutamate, EC50, μM (n) | 4.0 ± 0.27 (7) | 3.1 ± 0.30 (6) | 0.66 ± 0.07 (6)# | 8.2 ± 0.51 (6)# | 6.9 ± 0.74 (6)# | 13 ± 0.3 (6)# | 2.4 ± 0.12 (6) | |
| Glycine, EC50, μM (n) | 1.4 ± 0.20 (9) | 0.80 ± 0.13 (14)# | 0.19 ± 0.02 (15)# | 2.1 ± 0.14 (16)# | 1.4 ± 0.08 (13) | 2.8 ± 0.24 (13)# | 0.94 ± 0.06 (6) | |
| Amplitude (peak, pA/pF) | 131 ± 23 | 35 ± 6.4# | 5.8 ± 2.9# | 96 ± 17 | 101 ± 21 | 115 ± 21 | 46 ± 13 | 61 ± 23 |
| Amplitude (SS, pA/pF) | 74 ± 15 | 5.4 ± 0.9# | --- | 52 ± 9.5 | 21 ± 5.5# | 33 ± 7.7# | 14 ± 3.9# | 0.7 ± 0.13# |
| ISS/IPEAK% | 56 ± 5.0% | 18 ± 2.1%# | --- | 58 ± 3.7% | 20 ± 2.3%# | 29 ± 4.8%# | 29 ± 2.7%# | 1.5 ± 0.1%# |
| τW desensitization (ms) | 735 ± 76 | 211 ± 21# | --- | 769 ± 52 | 235 ± 32# | 374 ± 59# | 742 ± 120 | 91 ± 4.5# |
| Rise time (ms) | 7.7 ± 0.51 | 5.7 ± 0.7 | 1063 ± 14# | 10 ± 0.9 | 5.2 ± 0.4# | 11 ± 1.1 | 8.3 ± 0.9 | 11 ± 1.5 |
| τFAST (ms) | 36 ± 3.3 | 32 ± 2.0 | 555 ± 47# | 37 ± 2.9 | 16 ± 1.5# | 26 ± 1.3 | 17 ± 1.4# | 21 ± 4.4# |
| τSLOW (ms) | 271 ± 85 | 315 ± 60 | --- | 583 ± 85 | 416 ± 138 | 705 ± 188 | 384 ± 118 | 123 ± 32# |
| %τFAST | 94 ± 1.9% | 86 ± 2.1% | 95 ± 3.7% | 91 ± 4.4% | 90 ± 2.7% | 96 ± 1.3% | 92 ± 6.8% | 79 ± 6.8% |
| τW(ms) | 47 ± 5.7 | 65 ± 6.5 | 610 ± 40# | 55 ± 4.2 | 37 ± 6.1 | 46 ± 5.8 | 25 ± 2.8# | 40 ± 5.7 |
| n | 8 | 11 | 9 | 22 | 12 | 10 | 8 | 12 |
Human GluN1 and GluN2 were diheteromeric receptors and rat GluN1 and GluN2 were used for triheteromeric experiments.
# p < 0.05 compared to GluN2A/GluN2A; one way ANOVA, Tukey post hoc.
See S8 Table for F statistics and p values.