TABLE 3.
Stereoselective potentiation of GluN2C- and GluN2D-containing NMDARs
Values for current ratio and EC50 are mean ± S.E.M. from 8–22 oocytes obtained from at least two different frogs.
| Compound | I (30 µM) / I (Control) (%) |
EC50 (µM) [CI]a (% Max. Modulation) |
||||
|---|---|---|---|---|---|---|
| GluN2A | GluN2B | GluN2C | GluN2D | GluN2C | GluN2D | |
| (+)-FIQ | 100 ± 2.9 | 102 ± 2.1 | 192 ± 6.4 | 177 ± 3.5 | NA | NA |
| (-)-FIQ | 97 ± 0.9 | 96 ± 0.9 | 102 ± 3.5 | 106 ± 4.9 | NE | NE |
| (+)-CIQ | 118 ± 1.9 | 98 ± 1.3 | 250 ± 15 | 285 ± 11 | 7.8 [6.8, 9.0] (286 ± 23) | 10.5 [9.5, 11.7] (322 ± 18) |
| (-)-CIQ | 105 ± 2.7 | 88 ± 2.7 | 125 ± 4.7 | 117 ± 5.6 | NE | NE |
| (+)-BIQ | 87 ± 0.5 | 99 ± 0.8 | 318 ± 28 | 326 ± 16 | 3.8 [3.2, 4.5] (352 ± 47) | 5.5 [5.1, 6.0] (354 ± 21) |
| (-)-BIQ | 89 ± 5.7 | 84 ± 0.6 | 100 ± 5.0 | 96 ± 3.2 | NE | NE |
| (+)-IIQ | 98 ± 1.4 | 97 ± 0.7 | 197 ± 14 | 273 ± 15 | 2.1 [1.9, 2.2] (204 ± 16) | 3.5 [3.1, 4.0] (289 ± 16) |
| (-)-IIQ | 88 ± 3.6 | 85 ± 1.3 | 98 ± 5.4 | 85 ± 3.8 | NE | NE |
Mean half-maximally effective concentration of modulators (see Materials and Methods). The value [95% CI] was determined from fitting individual concentration-effect curves, averaging the fitted values on the log scale, and presented on linear scale. The Hill slopes ranged between 0.5 and 1.5. The fitted maximal response as a percentage of control is given in parentheses.
CI, confidence interval; NA, not analyzed; the concentration-effect curve could not be fitted by the Hill equation; NE, no effect; the ratio of current in 30 µM test compound to control current was less than 130%, which was our threshold for further analysis.