Table 8.
Optimization of linker A
 | ||||||||
|---|---|---|---|---|---|---|---|---|
| I10 µM / ICONTROL (mean ± SEM, %) |
EC50 (maximal potentiation) (µM, %)a |
|||||||
| R | X | Y | Z | GluN2C | GluN2D | GluN2C | GluN2D | |
| 1 | H | O | C | - | 116 ± 2.9 | 123 ± 2.3 | 12 (145%) | 11 (156%) |
| 216 | H | O | S | O | 92 ± 1.5 | 98 ± 0.6 | -- | -- |
| 141 | H | - | CH2 | - | 102 ± 3.4 | 92 ± 2.4 | -- | -- |
| 2 | Cl | O | C | - | 193 ± 7.3 | 179 ± 5.7 | 4.6 (233%) | 5.0 (215%) |
| 217 | Cl | O | S | O | 97 ± 1.8 | 96 ± 0.5 | -- | -- |
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) responses. Compounds 1 and 2 from preceding Tables are included here for comparison. Data are from between 6–25 oocytes from between 2–5 frogs for each compound and receptor tested.