Ligand affinity for NR3A S1S2 and NR1 S1S2
| NR3A S1S2 | NR1 S1S2 | NR1/NR3A ratio | |
|---|---|---|---|
| NR1 agonists | |||
| Glycine | 40.4 ± 3.7 nm | 26.4 μma | 653 |
| d-Serine | 643 ± 47 nm | 7.02 μma | 10.9 |
| l-Serine | 158 ± 17 μm | 2.3 mma | 14.6 |
| DCS | 277 ± 8 μm | 241 μma | 0.87 |
| ACPC | 97.7 ± 5.5 μm | 4.8 μmb | 0.049 |
| ACBC | 14.4 ± 1.2 μm | 830 μmb | 57.6 |
| NR2 agonists | |||
| l-Glutamate | 9.6 ± 1.7 mm | ≫300 mmc | ≫30 |
| NMDA | >10 mm | ND | ND |
| NR1 antagonists | |||
| CNQX | 2.51 ± 0.35 μm | 6.33 ± 1.64 μm | 2.52 |
| CGP78608 | 5.52 ± 0.13 μm | 6.40 ± 0.89 nm | 1.2 × 10−3 |
| L689560 | 305 ± 41 μm | 29.3 ± 1.4 nm | 9.6 × 10−5 |
| Kynurenic acid | 14.7 ± 7.7 mm | 53 ± 29 μm | 3.6 × 10−3 |
| 7-CKA | 620 ± 115 μm | 2.6 ± 0.3 μm | 4.2 × 10−3 |
| 5,7-DCKA | 647 ± 61 μm | 0.54 μma | 8.4 × 10−4 |
| L701324 | >100 μmd | 941 ± 151 nm | < 9.4 × 10−3 |
| Cycloleucine | >100 mm | 15.3 mmb | <0.15 |
Kd values are mean ± SEM for three to six observations per ligand. ND, Not determined.
↵aWhere indicated, values for NR1 were taken from Furukawa and Gouaux (2003).
↵bWhere indicated, values for NR1 were taken from Inanobe et al. (2005).
↵cl-Glutamate solubility was <2.5 m in LBB.
↵dL701324 solubility was <3.6 × 10−4 m in ligand binding buffer.