Page last updated: 2024-08-05 15:26:52

metabotropic glutamate receptor agonist

An agonist that selectively binds to and activates a metabotropic glutamate receptor.

ChEBI ID: 61966

Members (7)

MemberDefinitionClass
2-amino-4-phosphonobutyric acidA 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L-alpha-amino acid that is L-alpha-aminobutyric acid in which one of the hydrogens of the terminal methyl group has been replaced by a dihydroxy(oxido)-lambda(5)-phosphanyl group.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
amn082A 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 acidThe organosulfinic acid arising from oxidation of the sulfhydryl group of L-cysteine.3-sulfino-L-alanine
ly 379268An 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 404039An 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 dihydrochlorideA hydrochloride obtained by combining N,N'-bis(diphenylmethyl)ethane-1,2-diamine with two molar equivalent of hydrochloric acid.AMN082 dihydrochloride
xanthurenic acidA quinolinemonocarboxylic acid that is quinoline-2-carboxylic acid substituted by hydroxy groups at C-4 and C-8.xanthurenic acid

Research

Studies (615)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199094 (15.28)18.7374
1990's62 (10.08)18.2507
2000's168 (27.32)29.6817
2010's253 (41.14)24.3611
2020's38 (6.18)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials5 (0.75%)5.53%
Reviews16 (2.41%)6.00%
Case Studies5 (0.75%)4.05%
Observational2 (0.30%)0.25%
Other635 (95.78%)84.16%

Protein Targets (90)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-lipoxygenase, partialHomo sapiens (human)Potency39.810711
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency29.881612
arylsulfatase AHomo sapiens (human)Potency0.338111
Ataxin-2Homo sapiens (human)Potency28.183811
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency19.011511
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency26.854511
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency26.121611
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency21.088013
Chain A, CruzipainTrypanosoma cruziPotency39.810711
Chain A, Ferritin light chainEquus caballus (horse)Potency31.622814
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency28.183811
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency0.316211
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency9.976311
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency6.855612
chromobox protein homolog 1Homo sapiens (human)Potency57.502023
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency5.011923
D(1A) dopamine receptorHomo sapiens (human)Potency11.220211
D(1A) dopamine receptorSus scrofa (pig)Potency13.091811
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency35.481311
dopamine D1 receptorHomo sapiens (human)Potency18.356411
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency15.019433
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency16.749614
EWS/FLI fusion proteinHomo sapiens (human)Potency19.958144
GABA theta subunitRattus norvegicus (Norway rat)Potency5.011911
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency5.011911
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency5.011911
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency5.011911
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency5.011911
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency5.011911
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency5.011911
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency5.011911
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency5.011911
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency5.011911
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency5.011911
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency5.011911
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency5.011911
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency5.011911
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency5.011911
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency5.011911
gemininHomo sapiens (human)Potency29.092911
glp-1 receptor, partialHomo sapiens (human)Potency7.079511
GLS proteinHomo sapiens (human)Potency3.548111
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency1.000012
lethal factor (plasmid)Bacillus anthracis str. A2012Potency10.000011
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency8.912511
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency22.207226
ParkinHomo sapiens (human)Potency39.810711
phosphopantetheinyl transferaseBacillus subtilisPotency45.893915
PINK1Homo sapiens (human)Potency39.810711
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency1.000011
ras-related protein Rab-9AHomo sapiens (human)Potency58.047911
regulator of G-protein signaling 4Homo sapiens (human)Potency12.703213
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency15.792222
Smad3Homo sapiens (human)Potency15.848911
TDP1 proteinHomo sapiens (human)Potency24.844522
thioredoxin reductaseRattus norvegicus (Norway rat)Potency9.943812
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency31.622811
thyroid stimulating hormone receptorHomo sapiens (human)Potency7.943322
USP1 protein, partialHomo sapiens (human)Potency31.622811

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Glutamate receptor 1Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor 2Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor 3Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor 4Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor ionotropic, kainate 1Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor ionotropic, kainate 2Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor ionotropic, kainate 4Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor ionotropic, kainate 5Rattus norvegicus (Norway rat)IC50100.000011
Metabotropic glutamate receptor 1Homo sapiens (human)Ki700.000023
Metabotropic glutamate receptor 1Rattus norvegicus (Norway rat)Ki1,000.000011
Metabotropic glutamate receptor 2Homo sapiens (human)Ki236.801859
Metabotropic glutamate receptor 3Homo sapiens (human)Ki143.023237
Metabotropic glutamate receptor 4Homo sapiens (human)Ki5.635034
Metabotropic glutamate receptor 4Rattus norvegicus (Norway rat)Ki0.160022
Metabotropic glutamate receptor 5Homo sapiens (human)Ki700.000023
Metabotropic glutamate receptor 6Homo sapiens (human)Ki0.650012
Metabotropic glutamate receptor 7Homo sapiens (human)Ki137.500012
Metabotropic glutamate receptor 8Homo sapiens (human)Ki0.880512
Metabotropic glutamate receptor 8Rattus norvegicus (Norway rat)Ki1.900022
Vesicular glutamate transporter 3Rattus norvegicus (Norway rat)Ki190.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Estrogen receptorRattus norvegicus (Norway rat)EC5012.043012
Estrogen receptor betaRattus norvegicus (Norway rat)EC5012.043012
Metabotropic glutamate receptor 1Homo sapiens (human)EC50100.000011
Metabotropic glutamate receptor 1Rattus norvegicus (Norway rat)EC50820.000055
Metabotropic glutamate receptor 2Homo sapiens (human)EC50428.575967
Metabotropic glutamate receptor 2Rattus norvegicus (Norway rat)EC50862.000034
Metabotropic glutamate receptor 3Homo sapiens (human)EC500.015434
Metabotropic glutamate receptor 3Rattus norvegicus (Norway rat)EC50100.000011
Metabotropic glutamate receptor 4Homo sapiens (human)EC503.290077
Metabotropic glutamate receptor 4Rattus norvegicus (Norway rat)EC5014.62291516
Metabotropic glutamate receptor 5Rattus norvegicus (Norway rat)EC50640.000045
Metabotropic glutamate receptor 6Homo sapiens (human)EC5020.771255
Metabotropic glutamate receptor 6Rattus norvegicus (Norway rat)EC501.39451010
Metabotropic glutamate receptor 7Homo sapiens (human)EC50180.308477
Metabotropic glutamate receptor 7Rattus norvegicus (Norway rat)EC50316.488989
Metabotropic glutamate receptor 8Homo sapiens (human)EC507.479067
Metabotropic glutamate receptor 8Mus musculus (house mouse)EC500.400011
Metabotropic glutamate receptor 8Rattus norvegicus (Norway rat)EC500.151366
streptokinase A precursorStreptococcus pyogenes M1 GASEC506.546022

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Asparagine synthetase [glutamine-hydrolyzing]Homo sapiens (human)Kis1,450.000011
Metabotropic glutamate receptor 1Homo sapiens (human)Activity100.000011
Metabotropic glutamate receptor 2Homo sapiens (human)Activity0.003011
Metabotropic glutamate receptor 3Homo sapiens (human)Activity0.005011
Metabotropic glutamate receptor 4Homo sapiens (human)Activity21.000011
Metabotropic glutamate receptor 5Homo sapiens (human)Activity100.000011
Metabotropic glutamate receptor 6Homo sapiens (human)Activity0.400011
Metabotropic glutamate receptor 7Homo sapiens (human)Activity100.000011
Metabotropic glutamate receptor 8Homo sapiens (human)Activity2.000011