Table 3.
Agonist and co-agonist | GluN2A | GluN2B | GluN2C | GluN2D | GluN3A | GluN3B |
EC50 (µM) | ||||||
Glutamate | 7.7 | 2.3 | 1 | 0.39 | ||
Glycine | 1.2 | 0.38 | 0.32 | 0.12 | 57 | 95 |
Competitive antagonists | GluN2A | GluN2B | GluN2C | GluN2D | GluN3A | GluN3B |
Ki (µM) | ||||||
(R)-AP5 | 0.28 | 0.46 | 1.6 | 3.7 | ||
UBP141 | 14 | 19 | 4.2 | 2.8 | ||
Channel blockers | GluN2A | GluN2B | GluN2C | GluN2D | GluN3A | GluN3B |
IC50 (µM) | ||||||
(+)MK801 | 0.015 | 0.0099 | 0.024 | 0.038 | ||
Ketamine | 5.4 | 5.1 | 1.2 | 2.9 | ||
Phencyclidine | 0.82 | 0.16 | 0.16 | 0.22 | ||
Noncompetitive antagonists | GluN2A | GluN2B | GluN2C | GluN2D | GluN3A | GluN3B |
IC50 (µM) | ||||||
Ifenprodil | 39 | 0.15 | 29 | 76 | ||
Ro25-6981 | 52 | 0.009 | ||||
Allosteric potentiators | GluN2A | GluN2B | GluN2C | GluN2D | GluN3A | GluN3B |
EC50 (µM) | ||||||
CIQ | NE | NE | 2.8 | 3.0 |
NE, no detectable effect.