Concentration–inhibition data for L-689,560 at NMDA receptor subtypes
| . | [Glycine] (µM) . | IC50 (µM) . | % Inhibition . | Hill slope . | n . |
|---|---|---|---|---|---|
| GluN1/2A | 10a | 0.25 ± 0.01 | 100 ± 1 | 1.3 | 14 |
| GluN1/3A | 30b | 0.53 ± 0.08 | 96 ± 1 | 1.3 | 8 |
| 30c | 3.8 ± 0.3 | 92 ± 1 | 0.94 | 6 | |
| GluN1/3B | 100b | 1.9 ± 0.1 | 87 ± 2 | 1.2 | 12 |
| 100c | 8.9 ± 0.6 | 75 ± 3 | 1.7 | 8 | |
| GluN1FA+TL/3A | 30 | 0.077 ± 0.046 | 95 ± 1 | 1.2 | 16 |
| 100d | 0.15 ± 0.01 | 75 ± 4 | 1.4 | 5 | |
| 1,000d | 0.30 ± 0.01 | 44 ± 1 | 1.2 | 5 | |
| 3,000d | 0.38 ± 0.03 | 41 ± 2 | 1.0 | 4 | |
| GluN1FH+RK/3A | 100 | 5.6 ± 0.2 | 85 ± 1 | 1.3 | 5 |
| GluN1FA+TL/3B | 100d | 0.14 ± 0.01 | 29 ± 1 | 1.8 | 8 |
| 1,000d | 0.20 ± 0.01 | 30 ± 1 | 2.1 | 6 | |
| 3,000d | 0.20 ± 0.01 | 40 ± 2 | 1.6 | 6 |
| . | [Glycine] (µM) . | IC50 (µM) . | % Inhibition . | Hill slope . | n . |
|---|---|---|---|---|---|
| GluN1/2A | 10a | 0.25 ± 0.01 | 100 ± 1 | 1.3 | 14 |
| GluN1/3A | 30b | 0.53 ± 0.08 | 96 ± 1 | 1.3 | 8 |
| 30c | 3.8 ± 0.3 | 92 ± 1 | 0.94 | 6 | |
| GluN1/3B | 100b | 1.9 ± 0.1 | 87 ± 2 | 1.2 | 12 |
| 100c | 8.9 ± 0.6 | 75 ± 3 | 1.7 | 8 | |
| GluN1FA+TL/3A | 30 | 0.077 ± 0.046 | 95 ± 1 | 1.2 | 16 |
| 100d | 0.15 ± 0.01 | 75 ± 4 | 1.4 | 5 | |
| 1,000d | 0.30 ± 0.01 | 44 ± 1 | 1.2 | 5 | |
| 3,000d | 0.38 ± 0.03 | 41 ± 2 | 1.0 | 4 | |
| GluN1FH+RK/3A | 100 | 5.6 ± 0.2 | 85 ± 1 | 1.3 | 5 |
| GluN1FA+TL/3B | 100d | 0.14 ± 0.01 | 29 ± 1 | 1.8 | 8 |
| 1,000d | 0.20 ± 0.01 | 30 ± 1 | 2.1 | 6 | |
| 3,000d | 0.20 ± 0.01 | 40 ± 2 | 1.6 | 6 |
Concentration–inhibition data for L-689,560 were recorded using two-electrode voltage-clamp electrophysiology at recombinant NMDA receptors expressed in Xenopus oocytes. Responses were activated by glycine at the indicated concentrations. The fitted maximal inhibition is shown as percentage inhibition of the response in the absence of antagonist. Data are presented as mean ± SEM of values from individual oocytes, and n is the number of oocytes used to generate the data.
Measured in the continuous presence of 300 µM glutamate.
Measured in the continuous presence of 1 µM CGP-78608.
Measured in the continuous presence of 10 µM CGP-78608.
Biphasic concentration–response relationships were observed, but only data for high-potency components are listed.