Effects of TB-3-4 at wild-type and mutant NMDA receptors
| Subunit combination | TB-3-4 | ||
|---|---|---|---|
| IC50 | nH | n | |
| μM | |||
| NR1/NR2A | 0.19 (0.16, 0.22) | 0.9 ± 0.04 | 7 |
| NR1(N616G)/NR2A | 0.49 (0.28, 0.64)1-a | 0.9 ± 0.03 | 5 |
| NR1(N616Q)/NR2A | 0.75 (0.62, 0.90)1-a | 1.0 ± 0.03 | 4 |
| NR1/NR2B | 0.28 (0.23, 0.33) | 0.8 ± 0.03 | 5 |
| NR1(N616G)/NR2B | 0.36 (0.27, 0.47) | 0.9 ± 0.03 | 4 |
| NR1(N616Q)/NR2B | 0.59 (0.55, 0.62)1-a | 1.1 ± 0.02 | 4 |
| NR1(N616R)/NR2B | 175 (173, 178)1-a | 1.2 ± 0.05 | 4 |
| NR1/NR2C | 5.4 (5.0, 5.8) | 0.9 ± 0.02 | 4 |
| NR1/NR2D | 9.7 (8.7, 10.8) | 1.1 ± 0.04 | 5 |
The effects of TB-3-4 were measured at NR1/NR2 receptors containing wild-type and mutant NR1 subunits in oocytes voltage-clamped at −70 mV. Values for the IC50, mean (−S.E.M., +S.E.M.), and Hill slope (nH; mean ± S.E.M.) were determined from concentration-inhibition curves with five or six concentrations of TB-3-4 at each receptor type.
↵1-a P < .05 compared with respective wild-type receptors (one-way analysis of variance with post hocDunnett’s test).