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metabotropic glutamate receptor agonist
An agonist that selectively binds to and activates a metabotropic glutamate receptor.
ChEBI ID: 61966
Members (7)
| Member | Definition | Class |
|---|---|---|
| 2-amino-4-phosphonobutyric acid | A non-proteinogenc L-alpha-amino acid that is L-alpha-aminobutyric acid in which one of the hydrogens of the terminal methyl group has been replaced by a dihydroxy(oxido)-lambda(5)-phosphanyl group. It is a potent and selective agonist for the group III metabotropic glutamate receptors (mGluR4/6/7/8). | (2S)-2-amino-4-phosphonobutanoic acid |
| amn082 | A diamine that is ethane-1,2-diamine in which both amino groups are substituted by diphenylmethyl groups. It is an allosteric agonist of the metabotropic glutamate receptor 7 (mGluR7). | N,N'-bis(diphenylmethyl)ethane-1,2-diamine |
| cysteine sulfinic acid | The organosulfinic acid arising from oxidation of the sulfhydryl group of L-cysteine. | 3-sulfino-L-alanine |
| ly 379268 | An organic heterobicyclic compound that is (1R,5S)-2-oxabicyclo[3.1.0]hexane carrying amino, carboxy, and carboxy groups at positions 4R, 4R and 6R, respectively. It is a potent agonist of group II metabotropic glutamate receptors mGluR2 and mGluR3 (EC50 = 2.69 nM and 4.48 nM, respectively) that exhibits antipsychotic-like action in animal models of schizophrenia. | LY 379268 |
| ly 404039 | An organic heterobicyclic compound that is (1S,5R)-2-thiabicyclo[3.1.0]hexane carrying oxo, oxo, amino, carboxy, and carboxy groups at positions 2, 2, 4S, 4S, and 6S, respectively. It is a potent agonist of group II metabotropic glutamate receptors mGluR2 mGluR3 (Ki = 149 nM and 92 nM, respectively) and exhibits antipsychotic and anxiolytic efficacy in animal models. | LY404039 |
| n,n'-dibenzhydrylethane-1,2-diamine dihydrochloride | A hydrochloride obtained by combining N,N'-bis(diphenylmethyl)ethane-1,2-diamine with two molar equivalent of hydrochloric acid. | AMN082 dihydrochloride |
| xanthurenic acid | A quinolinemonocarboxylic acid that is quinoline-2-carboxylic acid substituted by hydroxy groups at C-4 and C-8. | xanthurenic acid |
Research
Studies (615)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 94 (15.28) | 18.7374 |
| 1990's | 62 (10.08) | 18.2507 |
| 2000's | 168 (27.32) | 29.6817 |
| 2010's | 253 (41.14) | 24.3611 |
| 2020's | 38 (6.18) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 5 (0.75%) | 5.53% |
| Reviews | 16 (2.41%) | 6.00% |
| Case Studies | 5 (0.75%) | 4.05% |
| Observational | 2 (0.30%) | 0.25% |
| Other | 635 (95.78%) | 84.16% |
Protein Targets (90)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 29.8816 | 1 | 2 |
| arylsulfatase A | Homo sapiens (human) | Potency | 0.3381 | 1 | 1 |
| Ataxin-2 | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 19.0115 | 1 | 1 |
| atrial natriuretic peptide receptor 1 precursor | Homo sapiens (human) | Potency | 26.8545 | 1 | 1 |
| atrial natriuretic peptide receptor 2 precursor | Homo sapiens (human) | Potency | 26.1216 | 1 | 1 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 21.0880 | 1 | 3 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 39.8107 | 1 | 1 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 31.6228 | 1 | 4 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 0.3162 | 1 | 1 |
| Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 9.9763 | 1 | 1 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 6.8556 | 1 | 2 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 57.5020 | 2 | 3 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 5.0119 | 2 | 3 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| D(1A) dopamine receptor | Sus scrofa (pig) | Potency | 13.0918 | 1 | 1 |
| DNA dC->dU-editing enzyme APOBEC-3F isoform a | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| dopamine D1 receptor | Homo sapiens (human) | Potency | 18.3564 | 1 | 1 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 15.0194 | 3 | 3 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 16.7496 | 1 | 4 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 19.9581 | 4 | 4 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 29.0929 | 1 | 1 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 7.0795 | 1 | 1 |
| GLS protein | Homo sapiens (human) | Potency | 3.5481 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 1.0000 | 1 | 2 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 10.0000 | 1 | 1 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 8.9125 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 22.2072 | 2 | 6 |
| Parkin | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 45.8939 | 1 | 5 |
| PINK1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 1.0000 | 1 | 1 |
| ras-related protein Rab-9A | Homo sapiens (human) | Potency | 58.0479 | 1 | 1 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 12.7032 | 1 | 3 |
| serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 15.7922 | 2 | 2 |
| Smad3 | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 24.8445 | 2 | 2 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 9.9438 | 1 | 2 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 7.9433 | 2 | 2 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Glutamate receptor 1 | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| Glutamate receptor 3 | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| Glutamate receptor 4 | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| Glutamate receptor ionotropic, kainate 1 | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| Glutamate receptor ionotropic, kainate 2 | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| Glutamate receptor ionotropic, kainate 3 | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| Glutamate receptor ionotropic, kainate 4 | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| Glutamate receptor ionotropic, kainate 5 | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| Metabotropic glutamate receptor 1 | Homo sapiens (human) | Ki | 700.0000 | 2 | 3 |
| Metabotropic glutamate receptor 1 | Rattus norvegicus (Norway rat) | Ki | 1,000.0000 | 1 | 1 |
| Metabotropic glutamate receptor 2 | Homo sapiens (human) | Ki | 236.8018 | 5 | 9 |
| Metabotropic glutamate receptor 3 | Homo sapiens (human) | Ki | 143.0232 | 3 | 7 |
| Metabotropic glutamate receptor 4 | Homo sapiens (human) | Ki | 5.6350 | 3 | 4 |
| Metabotropic glutamate receptor 4 | Rattus norvegicus (Norway rat) | Ki | 0.1600 | 2 | 2 |
| Metabotropic glutamate receptor 5 | Homo sapiens (human) | Ki | 700.0000 | 2 | 3 |
| Metabotropic glutamate receptor 6 | Homo sapiens (human) | Ki | 0.6500 | 1 | 2 |
| Metabotropic glutamate receptor 7 | Homo sapiens (human) | Ki | 137.5000 | 1 | 2 |
| Metabotropic glutamate receptor 8 | Homo sapiens (human) | Ki | 0.8805 | 1 | 2 |
| Metabotropic glutamate receptor 8 | Rattus norvegicus (Norway rat) | Ki | 1.9000 | 2 | 2 |
| Vesicular glutamate transporter 3 | Rattus norvegicus (Norway rat) | Ki | 190.0000 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Estrogen receptor | Rattus norvegicus (Norway rat) | EC50 | 12.0430 | 1 | 2 |
| Estrogen receptor beta | Rattus norvegicus (Norway rat) | EC50 | 12.0430 | 1 | 2 |
| Metabotropic glutamate receptor 1 | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |
| Metabotropic glutamate receptor 1 | Rattus norvegicus (Norway rat) | EC50 | 820.0000 | 5 | 5 |
| Metabotropic glutamate receptor 2 | Homo sapiens (human) | EC50 | 428.5759 | 6 | 7 |
| Metabotropic glutamate receptor 2 | Rattus norvegicus (Norway rat) | EC50 | 862.0000 | 3 | 4 |
| Metabotropic glutamate receptor 3 | Homo sapiens (human) | EC50 | 0.0154 | 3 | 4 |
| Metabotropic glutamate receptor 3 | Rattus norvegicus (Norway rat) | EC50 | 100.0000 | 1 | 1 |
| Metabotropic glutamate receptor 4 | Homo sapiens (human) | EC50 | 3.2900 | 7 | 7 |
| Metabotropic glutamate receptor 4 | Rattus norvegicus (Norway rat) | EC50 | 14.6229 | 15 | 16 |
| Metabotropic glutamate receptor 5 | Rattus norvegicus (Norway rat) | EC50 | 640.0000 | 4 | 5 |
| Metabotropic glutamate receptor 6 | Homo sapiens (human) | EC50 | 20.7712 | 5 | 5 |
| Metabotropic glutamate receptor 6 | Rattus norvegicus (Norway rat) | EC50 | 1.3945 | 10 | 10 |
| Metabotropic glutamate receptor 7 | Homo sapiens (human) | EC50 | 180.3084 | 7 | 7 |
| Metabotropic glutamate receptor 7 | Rattus norvegicus (Norway rat) | EC50 | 316.4889 | 8 | 9 |
| Metabotropic glutamate receptor 8 | Homo sapiens (human) | EC50 | 7.4790 | 6 | 7 |
| Metabotropic glutamate receptor 8 | Mus musculus (house mouse) | EC50 | 0.4000 | 1 | 1 |
| Metabotropic glutamate receptor 8 | Rattus norvegicus (Norway rat) | EC50 | 0.1513 | 6 | 6 |
| streptokinase A precursor | Streptococcus pyogenes M1 GAS | EC50 | 6.5460 | 2 | 2 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Asparagine synthetase [glutamine-hydrolyzing] | Homo sapiens (human) | Kis | 1,450.0000 | 1 | 1 |
| Metabotropic glutamate receptor 1 | Homo sapiens (human) | Activity | 100.0000 | 1 | 1 |
| Metabotropic glutamate receptor 2 | Homo sapiens (human) | Activity | 0.0030 | 1 | 1 |
| Metabotropic glutamate receptor 3 | Homo sapiens (human) | Activity | 0.0050 | 1 | 1 |
| Metabotropic glutamate receptor 4 | Homo sapiens (human) | Activity | 21.0000 | 1 | 1 |
| Metabotropic glutamate receptor 5 | Homo sapiens (human) | Activity | 100.0000 | 1 | 1 |
| Metabotropic glutamate receptor 6 | Homo sapiens (human) | Activity | 0.4000 | 1 | 1 |
| Metabotropic glutamate receptor 7 | Homo sapiens (human) | Activity | 100.0000 | 1 | 1 |
| Metabotropic glutamate receptor 8 | Homo sapiens (human) | Activity | 2.0000 | 1 | 1 |