Table 1 Summary of glutamate and GABA receptor interaction assays. ‘↑’ or ‘↓’ arrows indicate agonist or antagonist activity, respectively. The number of arrows indicates IC50/EC50 in the range of 10–100 μM (one arrow), 1–10 μM (two arrows), or < 1 μM (three arrows). Interactions with EC50 or IC50 above 100 μM are marked as “–”.
Receptor name | Receptor type | Assay type | (R)-2MeGlu | (S)-2MeGlu |
|---|---|---|---|---|
GluN2A | Ionotropic | Functional | ↓ | – |
GluN2B | Ionotropic | Functional | – | – |
GluN2C | Ionotropic | Functional | – | – |
GluN2D | Ionotropic | Functional | – | – |
GluA2 | Ionotropic | Functional | – | – |
mGluR1 | Metabotropic | Binding | – | – |
mGluR2 | Metabotropic | Binding | – | – |
mGluR5 | Metabotropic | Binding | – | – |
NMDA nonspecific | Ionotropic | Binding | – | – |
AMPA nonspecific | Ionotropic | Binding | – | – |
kainate nonspecific | Ionotropic | Binding | – | – |
GABAA α1β1γ2 | Ionotropic | Functional | – | – |
GABAA α1β2γ2 | Ionotropic | Functional | – | – |
GABAA α1β3γ2 | Ionotropic | Functional | – | – |
GABAA α2β1γ2 | Ionotropic | Functional | – | – |
GABAA α2β2γ2 | Ionotropic | Functional | – | – |
GABAA α2β3γ2 | Ionotropic | Functional | – | – |
GABAA α3β1γ2 | Ionotropic | Functional | – | – |
GABAA α3β2γ2 | Ionotropic | Functional | – | – |
GABAA α3β3γ2 | Ionotropic | Functional | – | – |
GABAA α4β1γ2 | Ionotropic | Functional | – | – |
GABAA α4β2γ2 | Ionotropic | Functional | – | – |
GABAA α4β3γ2 | Ionotropic | Functional | – | – |
GABAA α4β3δ | Ionotropic | Functional | – | – |
GABAA α5β1γ2 | Ionotropic | Functional | – | – |
GABAA α5β2γ2 | Ionotropic | Functional | – | – |
GABAA α5β3γ2 | Ionotropic | Functional | – | – |
GABAA α6β1γ2 | Ionotropic | Functional | – | – |
GABAA α6β2γ2 | Ionotropic | Functional | – | – |
GABAA α6β3γ2 | Ionotropic | Functional | – | – |
GABAB (B1/B2) | Metabotropic | Binding | – | – |
GABAB (B1a/B2) | Metabotropic | Binding | – | – |
GABAB (B1b/B2) | Metabotropic | Binding | – | – |
GABAB (B1/B2) | Metabotropic | Functional | – | – |
