Table 7.
Optimization of linker A
 | ||||||
|---|---|---|---|---|---|---|
| I10 µM / ICONTROL (mean ± SEM, %) |
EC50 (maximal potentiation) (µM, %)a |
|||||
| R | X | GluN2C | GluN2D | GluN2C | GluN2D | |
| 209 | H | O | 99 ± 3.7 | 99 ± 1.5 | -- | -- |
| 210 | Cl | O | 93 ± 1.9 | 90 ± 2.0 | -- | -- |
| 211 | H | S | 99 ± 2.6 | 89 ± 1.2 | -- | -- |
| 212 | Cl | S | 99 ± 1.1 | 98 ± 1.5 | -- | -- |
| 213 | F | S | 98 ± 1.9 | 103 ± 2.0 | -- | -- |
| 214 | Br | S | 99 ± 1.0 | 110 ± 6.0 | ||
| 215 | Me | S | 116 ± 2.0 | 126 ± 6.6 | 5.2 (126%) | 4.9 (130%) |
a
Fitted EC50 values are shown to two significant digits when potentiation at 10 µM test compound exceeds 115%; values in parentheses are the fitted maximum response as a percentage of the initial glutamate (100 µM) and glycine (30 µM) response. Data are from between 8–14 oocytes from between 2–3 frogs for each compound and receptor tested.