Table 1.
Compounds with mGluR Affinity Cited in the Text with their Chemical Names, Main Target and Action
Compound Abbreviation | Chemical Name | Target | Action |
---|---|---|---|
A794278 | 9-dimethylamino-3-cycloheptyl-3H-5-thia-1,3,6-triazafluoren-4-one | Group I, mGluR1 | Antagonist |
A794282 | 9-dimethylamino-3-(4-ethylphenyl)-3H-5-thia-1,3,6-triazafluoren-4-one | Group I, mGluR1 | Antagonist |
A841720 | 9-dimethylamino-3-(N-hexamethyleneiminyl)-3H-5-thia-1,3,6-triazafluoren-4-one | Group I, mGluR1 | Antagonist |
A850002 | 9-dimethylamino-3-(4-methylphenyl)-3H-5-thia-1,3,7-triazafluoren-4-one | Group I, mGluR1 | Antagonist |
ACPT-I | (1S,3R,4S)-1-aminocyclopentane-1,3,4-tricarboxylic acid | Group III | Agonist |
ADX47273 | (S)-(4-fluorophenyl)-(3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]piperidin-1-yl) methanone | Group I, mGluR5 | PAM |
AIDA | 1-aminoindan-1,5-dicarboxylic acid | Group I, mGluR1 | Antagonist |
AMN082 | N,N'-dibenzhydrylethane-1,2-diamine dihydrochloride | Group III, mGluR7 | Agonist |
APDC | (2R,4R)-4-aminopyrrolidine-2,4-dicarboxylate | Group II | Agonist |
(1S,3S)-APDC | aminopyrrolidine-2,4-dicarboxylate | Group II | Agonist |
BAY367620 | [(3aS,6aS)-6a-naphtalen-2-yl-methyl-5-methyliden-hexahydro-cyclopental[c]furan-1-on] | Group I, mGluR1 | Antagonist |
BINA | biphenyl-indanone A | Group II, mGluR2 | PAM |
Compound 5 | 1-(2-Hydroxy-3-methyl-4-{4-[4-(2H-tetrazol-5-yl)phenoxy]butoxy}phenyl)ethanone | Group II, mGluR2 | PAM |
Compound 8q | 3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide | Group I, mGluR5 | NAM |
CDPPB | 3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide | Group I, mGluR5 | PAM |
(S)-4C3HPG | 4-[(1S)-1-amino-2-hydroxy-2-oxoethyl]-2-hydroxybenzoic acid | Group I; Group II | Antagonist; Agonist |
CPCCOEt | 7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxylate ethyl ester | Group I, mGluR1 | Antagonist |
(S)-4CPG | (S)-4-carboxyphenylglycine | Group I | Antagonist |
DCG-IV | (2S,2'R,3'R)-2-(2',3'-dicarboxycyclopropyl)glycine | Group II | Agonist |
(S)-3,4-DCPG | (S)-3,4-dicarboxyphenylglycine | Group III, mGluR8 | Agonist |
DHPG | (S)-3,5-dihydroxyphenylglycine | Group I | Agonist |
EMQMCM | 3-ethyl-2-methyl-quinolin-6-yl)-(4-methoxy-cyclohexyl)-methanone methanesulfonate | Group I, mGluR1 | Antagonist |
Fenobam | 1-(3-chlorophenyl)-3-(3-methyl-5-oxo-4H-imidazol-2-yl) urea | Group I, mGluR5 | Antagonist |
JNJ16259685 | 3,4-dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-(cis-4-methoxycyclohexyl) methadone | Group I, mGluR1 | Antagonist |
L-AP4 | L-(+)-2-amino-4-phosphonobutyric acid | Group III | Agonist |
L-SOP | L-serine-O-phosphate | Group III | Agonist |
LSP1-2111 | Undisclosed | Group III | Agonist |
LY339764 | (R.S)-2-amino-2-(4-carboxycyclobutyl-3-(9-xanthen-9-yl)propanoic acid | Group I, mGluR5 | Antagonist |
LY339840 | (S)-(+)-a-amino-4-carboxy-2-methylbenzeneacetic acid | Group I, mGluR1 | Antagonist |
LY341495 | 1S,2S)-2-[(2S)-2-amino-3-(2,6-dioxo-3H-purin-9-yl)-1-hydroxy-1-oxopropan-2-yl]cyclopropane-1-carboxylic acid | Group II | Antagonist |
LY354740 | (1S,2S,5R,6S)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid | Group II | Agonist |
LY367335 | 2-amino-2-(3-cis and trans-carboxycyclobutyl)-3(9H-xanthen-9-yl)propionic acid | Group I | Antagonist |
LY367366 | (R,S)-2-amino-2-(4-carboxyphenyl)-3-(9H-thioxanthen-9-yl) propanoic acid | Group I, mGluR5 | Antagonist |
LY367385 | (+)-2-methyl-4-carboxyphenylglycine | Group I, mGluR1 | Antagonist |
LY379268 | (2R,6R)-2-amino-4-oxabicyclo[3.1.0]hexane-2,6-dicarboxylic acid | Group II | Agonist |
LY389795 | 1R,4R,5S,6R)-4-amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid | Group II | Agonist |
LY393053 | 2-amino-2(S)-(3-cis-carboxycyclobutyl-3-(9-thioxanthen-9-yl)propionic acid) | Group I | Antagonist |
LY404039 | (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic acid | Group II | Agonist |
LY456066 | 2-[4-(In-dan-2-ylamino)-5,6,7,8-tetrahydro-quinazolin-2-ylsulfanyl]-ethanol | Group I, mGluR5 | Antagonist |
LY456236 | 4-methoxy-phenyl)-(6-methoxy-quinazolin-4-yl)-amine | Group I, mGluR1 | Antagonist |
LY487379 | 2,2,2-trifluoro-N-[4-(2-methoxyphenoxy)phenyl]-N-(3-pyr idinylmethyl)ethanesulfonamide | Group II, mGluR2 | PAM |
MAP4 | α-methyl-aminophosphonobutyrate | Group III | Antagonist |
(+)-MCPG | 4-[(2S)-2-amino-1-hydroxy-1-oxopropan-2-yl]benzoic acid | Group I and II | Antagonist |
MGS00391 | R,2R,3R,5R,6R)-2-amino-3-(3,4-dichlorobenzyloxy)-6 fluorobicyclo [3.1.0]hexane-2,6-dicarboxylic acid | Group II | Antagonist |
MPEP | 2-methyl-6-(2-phenylethynyl)pyridine | Group I, mGluR5 | Antagonist |
MPPG | 2-amino-2-(4-phosphonophenyl)propanoic acid | Group II | Antagonist |
MPTP | 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine | Group I, mGluR5 | Antagonist |
MTEP | 3-((2-methyl-1,3-thiazol-4-yl)ethynyl)pyridine hydrochloride | Group I, mGluR5 | Antagonist |
MTPG | 2-amino-2-[4-(tetrazol-1-yl)phenyl]propanoic acid | Group II | Antagonist |
NAAG | N-acetylaspartylglutamate | Group II,mGluR3 | Agonist |
PHCCC | N-phenyl-7-(hydroxyimino)cyclopropa[b]chromen-1ac-arbox amide | Group II, mGluR4 | PAM |
(R,S)-PPG | (RS)-4-phosphonophenylglycine | Group III | Agonist |
R214127 | 1-(3,4-dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-2-phenyl-1-ethanone | Group I, mGluR1 | NAM |
SIB1757 | 6-methyl-2-(phenylazo)-3-pyridinol | Group I, mGluR1 | Antagonist |
SIB1893 | (E)-2-methyl-6-styrylpyridine | Group I, mGluR5 | Antagonist |
Abbreviations and symbols: PAM, positive allosteric modulator; NAM, negative allosteric modulator.