Potency and intrinsic activity of ligands acting at the glycineB site of expressed NMDA receptor subtypes
| Ligand | Potency (μM) | References; species, NR1 splice variant | |||
|---|---|---|---|---|---|
| NR1/NR2A | NR1/NR2B | NR1/NR2C | NR1/NR2D | ||
| Glycine | 1.2 | 0.16 | Buller and Monaghan, 1997; NR1a | ||
| Glycine | 0.97 | 0.84 | 0.76 | 0.56 | Matsui et al., 1995; mouse |
| Glycine | 1.9 | 1.4 | Hesset al., 1996; human, NR1a | ||
| Glycine | 2.1 | 0.3 | 0.2 | Kutsuwada et al.,1992; mouse | |
| Glycine | 0.84 | 0.19 | 0.15 | 0.096 | Woodwardet al., 1995a,b; rat, NR1a |
| Glycine | 0.53 (100%)5-a | 0.06 (100%) | Priestley et al., 1995; human, NR1a | ||
| Glycine | 3.7 | 2.1 | 0.36 | 2.3 | Laurie and Seeburg, 1994a; binding |
| d-Serine | 0.32 (88%) | 0.26 (102%) | 0.21 (118%) | 0.17 (100%) | Matsui et al., 1995; mouse |
| d-Serine | 2.2 | 0.6 | Hess et al., 1996; human, NR1a | ||
| d-Serine | 0.22 (99%) | 0.15 (113%) | Priestley et al., 1995; human, NR1a | ||
| d-Serine | 0.79 (100%) | 0.72 (100%) | 1.24 (110%) | 0.75 (100%) | Krueger et al., 1997; human, NR1a |
| ACPC | 0.6 (100%) | 0.3 (100%) | 3.2 (150%) | 0.08 (110%) | Krueger et al., 1997; mouse |
| d-Cycloserine | 15.2 (20%) | 8.4 (20%) | 1.6 (120%) | 2 (100%) | Kruegeret al., 1997; mouse |
| d-Cycloserine | 3.2 (93%) | 1.3 (88%) | Priestley et al., 1995; human, NR1a | ||
| R(+)HA-966 | 121 (12%) | 4.6 (14%) | Priestley et al., 1995; human, NR1a | ||
| ACBC | 45 (13%) | 6.6 (33%) | Priestley et al., 1995; human, NR1a | ||
| 7-Cl-KYN | 0.63 (0%) | 0.2 (0%) | Priestley et al., 1995; human, NR1a | ||
| 5,7-diCl-KYN (K d) | 0.059 (0%) | 0.097 (0%) | 0.058 (0%) | 0.113 (0%) | Laurie and Seeburg, 1994a; binding, rat |
| ACEA 1011 (K b) | 0.33 | 0.46 | 0.21 | 0.74 | Woodwardet al., 1995a; rat, NR1a |
| ACEA 1021 (K b) | 0.0028 | 0.0059 | 0.0019 | 0.011 | Woodwardet al., 1995a; rat, NR1a |
| GV 156526A | 0.05 (0%) | 0.07 (0%) | Bunnermann et al., 1996; HEK cells | ||
| L-687,414 | 4.0 (5%) | 1.1 (3%) | Priestley et al., 1995; human, NR1a | ||
| L-701,324 | 0.005 (0%) | 0.005 (0%) | Priestleyet al., 1995; human, NR1a | ||
Data refer to electrophysiological studies unless stated otherwise. The species of mRNA and the type of NR1 splice variant are also shown.
↵5-a Values in parentheses are intrinsic activities (with respect to glycine).