Drug/Receptor Subunits | IC50 | Slope | Kb(Leff-Dougall) | Oocytes Tested |
---|---|---|---|---|
μM | n | |||
LY235959 | ||||
NR 1a/2A | 0.30 ± 0.03 | 1.0 ± 0.09 | 0.05 | 3 |
NR 1a/2B | 0.51 ± 0.05 | 1.1 ± 0.12 | 0.09 | 4 |
NR 1a/2C | 0.34 ± 0.02 | 1.3 ± 0.08 | 0.04 | 3 |
NR 1a/2D | 0.25 ± 0.01 | 1.2 ± 0.06 | 0.08 | 3 |
NR 1e/2B | 0.60 ± 0.02 | 1.2 ± 0.04 | 0.1 | 1 |
MDL 100,453 | ||||
NR 1a/2A | 3.6 ± 0.4 | 1.0 ± 0.12 | 0.60 | 3 |
NR 1a/2B | 17 ± 1.7 | 1.3 ± 0.15 | 3.21 | 4 |
NR 1a/2C | 36 ± 1.7 | 1.2 ± 0.06 | 4.35 | 3 |
NR 1a/2D | 17 ± 1.0 | 1.2 ± 0.09 | 5.77 | 3 |
NR 1e/2B | 19 ± 2.0 | 1.4 ± 0.19 | 3.53 | 1 |
Co 101244/PD 174494 | ||||
NR 1a/2A | 230 ± 31 | 0.70 ± 0.08 | Allosteric antagonist | 3 |
NR 1a/2B | 0.026 ± 0.004 | 1.7 ± 0.03 | Allosteric antagonist | 3 |
NR 1a/2C | 590 ± 70 | 1.1 ± 0.11 | Allosteric antagonist | 3 |
NR 1a/2D | 500 ± 50 | 1.1 ± 0.10 | Allosteric antagonist | 3 |
NR 1e/2B | 0.048 ± 0.002 | 1.7 ± 0.10 | Allosteric antagonist | 1 |
Glutamate | ||||
NR 1a/2A | 2.01 ± 0.14 | 1.82 ± 0.21 | 3 | |
NR 1a/2B | 1.86 ± 0.18 | 1.92 ± 0.30 | 3 | |
NR 1a/2C | 1.22 ± 0.05 | 1.49 ± 0.09 | 3 | |
NR 1a/2D | 0.38 ± 0.01 | 1.87 ± 0.06 | 3 | |
NR 1e/2B | 1.76 ± 0.4 | 1.8 ± 0.5 | 1 |
Analysis of concentration-inhibition curves (Fig. 2). IC50 and slope values are from best fit of data to eq. 2, andKb values were estimated using a Leff-Dougal approach, as described in Materials and Methods. All experiments were performed in nominally Ca2+-free frog Ringers, with Ba2+ in place of Ca2+. Glycine was fixed at 1 μM for NR 1a/2B, NR 1e/2B, and NR 1a/2C, and at 10 μM for NR 1a/2A.