Table 6.
I30μM / Icontrol (mean ± SEM, %) | EC50 (max.) (μM %)a | |||||||||
---|---|---|---|---|---|---|---|---|---|---|
# | R1 | R2 | R3 | R4 | GluN2B | GluN2C | GluN2D | GluN2B | GluN2C | GluN2D |
2b | OMe | H | H | Cl | 195 ± 11 | 233 ± 18 | 240 ± 29 | 5.2 (202%) | 2.0 (243%) | 3.0 (245%) |
110 | H | OMe | H | Cl | 99 ± 5.6 | 132 ± 3.8 | 125 ± 2.4 | -- | 6.2 (132%) | 5.4 (125%) |
111c | H | H | OMe | Cl | 108 ± 1.9 | 110 ± 3.6 | 99 ± 1.6 | -- | -- | -- |
112 | OCF3 | H | H | Cl | 130 ± 2.7 | 189 ± 8.5 | 150 ± 5.9 | 1.4(130%) | 1.5 (192%) | 1.7 (152%) |
92b | OEt | H | H | Cl | 145 ± 7.8 | 126 ± 2.8 | 102 ± 2.0 | 5.3 (158%) | 1.8 (128%) | -- |
113 | OiPr | H | H | Cl | 159 ± 7.5 | 134 ± 8.0 | 111 ± 3.8 | 3.8 (160%) | 1.7 (138%) | -- |
114 | OMe | H | H | F | 249 ± 7.6 | 271 ± 15 | 402 ± 19 | 29 (391%) | 5.9 (365%) | 11 (493%) |
115 | OCF3 | H | H | F | 124 ± 3.8 | 154 ± 5.8 | 136 ± 3.2 | 3.2 (123%) | 2.5 (157%) | 4.1 (137%) |
97b | OEt | H | H | F | 147 ± 3.7 | 104 ± 2.2 | 91 ± 1.7 | 7.2 (152%) | -- | -- |
116 | OiPr | H | H | F | 179 ± 4.1 | 133 ± 4.5 | 103 ± 2.2 | 7.1 (185%) | 2.7 (135%) | -- |
Fitted EC50 values are shown to two significant figures when potentiation at 30 μM exceeded 120%; values in parentheses are the fitted maximum response as a percentage of the initial glutamate (100 μM) and glycine (30 μM) current. Data are from between 7–15 oocytes from 2–3 frogs for each compound and receptor tested.
Compounds 2, 92, and 97 were shown in previous tables and were included here for comparison.
Current ratio reported for 10 μM due to precipitate at 30 μM.