Table 1.
Commonly used glutamatergic ligands in preclinical addiction research
| Ligand | Chemical Name | Mode of Action |
|---|---|---|
| AP5 (APV) | 2-amino-5-phosphonovaleric acid | NMDA antagonist (competitive) |
| Dizocilpine (MK-801) | (5S,10R)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine | NMDA antagonist (non-competitive) |
| Ifenprodil | 2-(4-benzylpiperidino)-1-(4-hydroxyphenyl)-1-propanol | NMDA antagonist (polyamine site) (some preference for NR2B) |
| GYKI 52466 | 4-(8-methyl-9H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)-benzenamine | AMPA antagonist (non-competitive) |
| NBQX | 2,3-dioxo-6-nitro-1,2,3,4-tetrahydrobenzo[f]quinoxaline-7-sulfonamide | AMPA/KA antagonist (competitive) |
| CNQX | 6-cyano-7-nitroquinoxaline-2,3-dione | AMPA/KA antagonist (competitive) (also NMDA glycine site antagonist) |
| DNQX | 6,7-dinitroquinoxaline-2,3-dione | AMPA/KA antagonist (competitive) |
| CPCCOEt | 7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxylate ethyl ester | mGluR1 antagonist (allosteric) |
| LY367385 | (S)-(+)- α-amino-4-carboxy-2-methylbenzeneacetic acid | mGluR1 antagonist (allosteric) |
| EMQMCM | (3-ethyl-2-methyl-quinolin-6-yl)-(4-methoxy-cyclohexyl)-methanone methane sulfonate | mGluR1 antagonist (allosteric) |
| MPEP | 2-methyl-6-(phenylethynyl)pyridine | mGluR5 antagonist (allosteric) |
| MTEP | 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine | mGluR5 antagonist (allosteric) |
| LY379268 | (1R,4R,5S,6R)-4-amino-2-oxabicyclo[3.1.0]hexane-4,6-dicarboxylic acid | mGluR2/3 agonist (orthosteric) |
| DCPG | (S)-3,4-dicarboxyphenylglycine | mGluR8 agonist (orthosteric) |
| TBOA | DL-threo-β-benzyloxyaspartic acid | EAAT inhibitor |
| MS-153 | (R)-(-)-5-methyl-1-nicotinoyl-2-pyrazoline | EAAT activator |