IPYD/IControl Mean ± S.E.M. % | EC50μM (%)a | IPYD/IControl Mean ± S.E.M. % | EC50μM (%)aμM (%)a | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
GluN2A | GluN2B | GluN2C | GluN2D | GluN2C | GluN2A | GluN2B | GluN2C | GluN2D | GluN2C | ||||
181c | 100 ± 1.5 | 96 ± 0.61 | 114 ± 2.3 | 99 ± 1.1 | N.D. (130) | 187b | 97 ± 1.8 | 95 ± 2.6 | 97 ± 1.4 | 94 ± 0.82 | N.D. | ||
182c | 96 ± 1.3 | 96 ± 0.93 | 108 ± 2.4 | 97 ± 0.70 | N.D. (114) | 188b | 95 ± 1.7 | 92 ± 1.9 | 89 ± 1.2 | 89 ± 0.86 | N.D. | ||
183c | 99 ± 4.2 | 96 ± 2.1 | 120 ± 2.2 | 83 ± 0.84 | N.D. (115) | 189b | 97 ± 0.56 | 94 ± 1.5 | 93 ± 0.45 | 91 ± 0.90 | N.D. | ||
184c | 92 ± 3.9 | 91 ± 1.9 | 134 ± 4.1 | 103 ± 6.1 | 9 (132) | 190d | 96 ± 6.2 | 65 ± 1.0 | 71 ± 0.27 | 67 ± 0.78 | N.D. | ||
185d | 97 ± 1.5 | 90 ± 1.5 | 93 ± 0.96 | 76 ± 2.2 | N.D. | 191b | 94 ± 1.6 | 94 ± 4.2 | 90 ± 1.4 | 90 ± 0.41 | N.D. | ||
186d | 76 ± 5.2 | 55 ± 4.5 | 48 ± 2.5 | 36 ± 1.9 | N.D. | 192c | 100 ± 6.9 | 90 ± 0.99 | 85 ± 0.37 | 84 ± 0.52 | N.D. |
All compounds were coapplied with 100 glutamate and 30 μM glycine. The concentration-effect curve was recorded for active compounds and fitted by the Hill equation (see Materials and Methods) to determine the EC50 value; parentheses show the response to 100 μM test compound as a percentage of the response to maximally effective concentrations of glutamate (100 μM) and glycine (30 μM) for compounds tested at multiple concentrations. Compounds were screened at b10 μM, c30 μM, and d100 μM depending on availability and solubility. N.D., not determined. For all compounds, data are from three to 12 oocytes from one to three different frogs.