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. 2012 Mar;10(1):12–48. doi: 10.2174/157015912799362805

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.

HHS Vulnerability Disclosure