Page last updated: 2024-12-07

3,5-dihydroxyphenylglycine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

3,5-Dihydroxyphenylglycine (DOPA) is a naturally occurring amino acid that is a precursor to dopamine, norepinephrine, and epinephrine. It is synthesized in the body from tyrosine. DOPA is used to treat Parkinson's disease, a neurological disorder that affects movement. It is also used to treat restless legs syndrome. DOPA is studied because of its importance in the biosynthesis of dopamine, norepinephrine, and epinephrine. These neurotransmitters play a crucial role in regulating mood, movement, attention, and other important functions.'

3,5-dihydroxyphenylglycine: a potent agonst of metabotropic glutamate receptors [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

(S)-3,5-dihydroxyphenylglycine : A glycine derivative that is L-alpha-phenylglycine substituted at positions 3 and 5 on the phenyl ring by hydroxy groups. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

FloraRankFlora DefinitionFamilyFamily Definition
GlycinegenusA non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.[MeSH]FabaceaeThe large family of plants characterized by pods. Some are edible and some cause LATHYRISM or FAVISM and other forms of poisoning. Other species yield useful materials like gums from ACACIA and various LECTINS like PHYTOHEMAGGLUTININS from PHASEOLUS. Many of them harbor NITROGEN FIXATION bacteria on their roots. Many but not all species of beans belong to this family.[MeSH]

Cross-References

ID SourceID
PubMed CID108001
CHEMBL ID66105
CHEBI ID93822
SCHEMBL ID1512962
MeSH IDM0212102
PubMed CID443586
CHEMBL ID39221
CHEBI ID29474
SCHEMBL ID12648471
MeSH IDM0212102

Synonyms (117)

Synonym
HMS3266G15
gtpl1367
146255-66-5
NCGC00024545-02
alpha-amino-3,5-dihydroxybenzeneacetic acid
3,5-dhpg
3,5-dihydroxyphenylglycine
benzeneacetic acid, alpha-amino-3,5-dihydroxy-
L000068
2-amino-2-(3,5-dihydroxyphenyl)acetic acid
CHEMBL66105
A814242
2-azanyl-2-[3,5-bis(oxidanyl)phenyl]ethanoic acid
AKOS006230321
NCGC00015338-03
5yr2n37e6d ,
unii-5yr2n37e6d
BRD-A20589515-001-01-1
s-3,5-dihydroxyphenylglycine
(+/-)-.alpha.-amino-3,5-dihydroxybenzeneacetic acid
dl-2-(3,5-dihydroxyphenyl)glycine
2-amino-2-(3,5-dihydroxyphenyl)-acetic acid
HOOWCUZPEFNHDT-UHFFFAOYSA-N
SCHEMBL1512962
(+/-)-3,5-dhpg hcl
(rs)-3,5-dihydroxyphenylglycine
(rs)-3,5-dhpg
HB0026
(r,s)-3,5-dhpg
sr-01000597610
SR-01000597610-1
CHEBI:93822
J-012694
dl-3,5-dihydroxyphenylglycine
HMS3675E15
Q27073605
HMS3411E15
HY-12598A
CS-0020572
(rs)-3,5-dhpg(rs)-3,5-dhpg
WFA25566
DTXSID901311536
EN300-298606
E98650
amino(3,5-dihydroxyphenyl)acetic acid
bdbm50079183
amino-(3,5-dihydroxy-phenyl)-acetic acid
amino-(3,5-dihydroxy-phenyl)-acetic acid(s-dhpg)
(s)-3,5-dhpg
(s)-amino-(3,5-dihydroxy-phenyl)-acetic acid
(2s)-amino(3,5-dihydroxyphenyl)ethanoic acid
HMS3266F22
EU-0100328
NCGC00024800-01
tocris-0342
lopac-d-3689
NCGC00015338-01
tocris-0805
NCGC00024545-01
LOPAC0_000328
l-3,5-dihydroxyphenylglycine
3,5-dihydroxy-phenylglycine
(s)-3,5-dihydroxyphenylglycine
dihydroxyphenylglycine
3,5-dihydroxy-l-phenylglycine
s-dhpg
DB04228
NCGC00024800-04
c8h9no4
NCGC00024800-02
NCGC00024800-03
162870-29-3
D 3689
NCGC00024800-05
CHEMBL39221 ,
chebi:29474 ,
(2s)-2-amino-2-(3,5-dihydroxyphenyl)acetic acid
HMS3261A17
AKOS006239507
(2s)-amino(3,5-dihydroxyphenyl)acetic acid
CCG-204423
NCGC00015338-02
(s)-3,5-dihydroxyphenylglycine hydrate
LP00328
NCGC00261013-01
tox21_500328
J516.528H ,
SCHEMBL12648471
(s)-2-amino-2-(3,5-dihydroxyphenyl)acetic acid
dihydroxyphenylglycine, (s)-3,5-
HB0045
benzeneacetic acid, alpha-amino-3,5-dihydroxy-, (alphas)-
benzeneacetic acid, .alpha.-amino-3,5-dihydroxy-, (.alpha.s)-
CF5G2G268A ,
unii-cf5g2g268a
SR-01000597444-1
sr-01000597444
J-009981
sr-01000075813
SR-01000075813-1
(s)-3,5-dihydroxylphenylglycine
(2r)-amino(3,5-dihydroxyphenyl)acetic acid
DTXSID20904031
HMS3675L21
(s)-3,5 dhpg
Q27095051
HMS3411L21
SDCCGSBI-0050316.P002
NCGC00024800-10
3,5-dhpg-(s)
MS-22974
HY-12598
CS-0012064
(alphas)-alpha-amino-3,5-dihydroxybenzeneacetic acid
EN300-3004820
(s)-2-amino-2-(3,5-dihydroxyphenyl)aceticacid
E98655

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" In mixed cultures of cortical cells, the selective mGlu1/5 agonist, 3,5-dihydroxyphenylglycine (DHPG), amplified neurodegeneration induced by a toxic pulse of NMDA."( An activity-dependent switch from facilitation to inhibition in the control of excitotoxicity by group I metabotropic glutamate receptors.
Battaglia, G; Bruno, V; Ceña, V; Cespédes, VM; Copani, A; Flor, PJ; Galindo, MF; Gasparini, F; Kuhn, R; Nicoletti, F; Sánchez-Prieto, J, 2001
)
0.55

Dosage Studied

ExcerptRelevanceReference
" In addition, increasing concentrations of PCCG-13 were able to shift to the right the agonist dose-response curve but had no effect when tested on other receptors coupled to PLD."( Antagonist pharmacology of metabotropic glutamate receptors coupled to phospholipase D activation in adult rat hippocampus: focus on (2R,1'S,2'R,3'S)-2-(2'-carboxy-3'-phenylcyclopropyl)glycine versus 3, 5-dihydroxyphenylglycine.
Albani-Torregrossa, S; Attucci, S; Marinozzi, M; Moroni, F; Pellegrini-Giampietro, DE; Pellicciari, R, 1999
)
0.3
" Ex vivo receptor occupancy with [(3)H]FTIDC revealed that the receptor occupancy level by FTIDC correlated well with FTIDC dosage and plasma concentration."( Correlation of receptor occupancy of metabotropic glutamate receptor subtype 1 (mGluR1) in mouse brain with in vivo activity of allosteric mGluR1 antagonists.
Hata, M; Hikichi, H; Inoue, T; Ito, S; Kawagoe-Takaki, H; Kawamoto, H; Kimura, T; Maehara, S; Murai, T; Ohta, H; Ozaki, S; Satow, A; Suzuki, G, 2009
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (4)

ClassDescription
alpha-amino acidAn amino acid in which the amino group is located on the carbon atom at the position alpha to the carboxy group.
resorcinolsAny benzenediol in which the two hydroxy groups are meta to one another.
non-proteinogenic L-alpha-amino acidAny L-alpha-amino acid which is not a member of the group of 23 proteinogenic amino acids.
amino acid zwitterionThe zwitterionic form of an amino acid having a negatively charged carboxyl group and a positively charged amino group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (46)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency39.81070.003245.467312,589.2998AID2517
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency39.81070.125919.1169125.8920AID2549
phosphopantetheinyl transferaseBacillus subtilisPotency39.81070.141337.9142100.0000AID1490
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency37.65050.011212.4002100.0000AID1030
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency5.01191.000010.475628.1838AID1457
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency39.81070.003245.467312,589.2998AID2517
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency8.71690.177814.390939.8107AID2147
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency39.81070.125919.1169125.8920AID2549
thioredoxin reductaseRattus norvegicus (Norway rat)Potency1.25890.100020.879379.4328AID588453
15-lipoxygenase, partialHomo sapiens (human)Potency39.81070.012610.691788.5700AID887
phosphopantetheinyl transferaseBacillus subtilisPotency44.66840.141337.9142100.0000AID1490
GLS proteinHomo sapiens (human)Potency11.22020.35487.935539.8107AID624146
Microtubule-associated protein tauHomo sapiens (human)Potency17.67160.180013.557439.8107AID1460; AID1468
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
thyroid stimulating hormone receptorHomo sapiens (human)Potency25.11890.001318.074339.8107AID926; AID938
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency3.16230.28189.721235.4813AID2326
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency2.96290.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency15.84890.540617.639296.1227AID2364; AID2528
cytochrome P450 2C19 precursorHomo sapiens (human)Potency12.92440.00255.840031.6228AID899
D(1A) dopamine receptorHomo sapiens (human)Potency18.71370.02245.944922.3872AID488982; AID488983
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency43.92850.010039.53711,122.0200AID1479
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency4.25620.425612.059128.1838AID504536
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency10.26630.031610.279239.8107AID884; AID885
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.81070.251215.843239.8107AID504327
lamin isoform A-delta10Homo sapiens (human)Potency22.38720.891312.067628.1838AID1459
neuropeptide S receptor isoform AHomo sapiens (human)Potency0.39810.015812.3113615.5000AID1461
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency10.26631.000012.224831.6228AID885
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Metabotropic glutamate receptor 8Homo sapiens (human)Ki1,000.00000.06103.68859.5000AID107274
Metabotropic glutamate receptor 1Rattus norvegicus (Norway rat)Ki0.90000.00790.31450.9000AID108493
Metabotropic glutamate receptor 5Homo sapiens (human)Ki1.90000.00050.54638.2000AID107059
Metabotropic glutamate receptor 1Homo sapiens (human)Ki6.60000.00033.536310.0000AID108489
Metabotropic glutamate receptor 2Homo sapiens (human)Ki1,000.00000.00270.71586.4000AID108830; AID108837
Metabotropic glutamate receptor 7Homo sapiens (human)Ki1,000.00000.99000.99000.9900AID107261
Metabotropic glutamate receptor 4Homo sapiens (human)Ki1,000.00000.16001.15672.4000AID109341
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Metabotropic glutamate receptor 4Rattus norvegicus (Norway rat)EC50 (µMol)100.00000.00902.54409.4900AID246705
Metabotropic glutamate receptor 1Homo sapiens (human)EC50 (µMol)6.60000.20004.41009.3000AID108646
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (46)

Processvia Protein(s)Taxonomy
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayMetabotropic glutamate receptor 8Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 8Homo sapiens (human)
visual perceptionMetabotropic glutamate receptor 8Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 8Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 8Homo sapiens (human)
desensitization of G protein-coupled receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of DNA-templated transcriptionMetabotropic glutamate receptor 5Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
phospholipase C-activating G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 5Homo sapiens (human)
learning or memoryMetabotropic glutamate receptor 5Homo sapiens (human)
learningMetabotropic glutamate receptor 5Homo sapiens (human)
locomotory behaviorMetabotropic glutamate receptor 5Homo sapiens (human)
positive regulation of MAPK cascadeMetabotropic glutamate receptor 5Homo sapiens (human)
positive regulation of long-term neuronal synaptic plasticityMetabotropic glutamate receptor 5Homo sapiens (human)
synapse organizationMetabotropic glutamate receptor 5Homo sapiens (human)
positive regulation of calcium-mediated signalingMetabotropic glutamate receptor 5Homo sapiens (human)
cognitionMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of postsynaptic membrane potentialMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of postsynaptic cytosolic calcium ion concentrationMetabotropic glutamate receptor 5Homo sapiens (human)
cellular response to amyloid-betaMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 5Homo sapiens (human)
trans-synaptic signaling by endocannabinoid, modulating synaptic transmissionMetabotropic glutamate receptor 5Homo sapiens (human)
G protein-coupled receptor signaling pathwayMetabotropic glutamate receptor 1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 1Homo sapiens (human)
phospholipase C-activating G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 1Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 1Homo sapiens (human)
locomotory behaviorMetabotropic glutamate receptor 1Homo sapiens (human)
sensory perception of painMetabotropic glutamate receptor 1Homo sapiens (human)
positive regulation of MAPK cascadeMetabotropic glutamate receptor 1Homo sapiens (human)
regulation of sensory perception of painMetabotropic glutamate receptor 1Homo sapiens (human)
regulation of postsynaptic membrane potentialMetabotropic glutamate receptor 1Homo sapiens (human)
cellular response to electrical stimulusMetabotropic glutamate receptor 1Homo sapiens (human)
L-glutamate import across plasma membraneMetabotropic glutamate receptor 1Homo sapiens (human)
regulation of postsynaptic cytosolic calcium ion concentrationMetabotropic glutamate receptor 1Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 1Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 1Homo sapiens (human)
negative regulation of adenylate cyclase activityMetabotropic glutamate receptor 2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 2Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 2Homo sapiens (human)
gene expressionMetabotropic glutamate receptor 2Homo sapiens (human)
glutamate secretionMetabotropic glutamate receptor 2Homo sapiens (human)
regulation of glutamate secretionMetabotropic glutamate receptor 2Homo sapiens (human)
regulation of dopamine secretionMetabotropic glutamate receptor 2Homo sapiens (human)
behavioral response to nicotineMetabotropic glutamate receptor 2Homo sapiens (human)
response to cocaineMetabotropic glutamate receptor 2Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionMetabotropic glutamate receptor 2Homo sapiens (human)
long-term synaptic depressionMetabotropic glutamate receptor 2Homo sapiens (human)
intracellular glutamate homeostasisMetabotropic glutamate receptor 2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMetabotropic glutamate receptor 2Homo sapiens (human)
regulation of response to drugMetabotropic glutamate receptor 2Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 2Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 2Homo sapiens (human)
behavioral fear responseMetabotropic glutamate receptor 7Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 7Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 7Homo sapiens (human)
sensory perception of soundMetabotropic glutamate receptor 7Homo sapiens (human)
negative regulation of glutamate secretionMetabotropic glutamate receptor 7Homo sapiens (human)
axon developmentMetabotropic glutamate receptor 7Homo sapiens (human)
glycosylationMetabotropic glutamate receptor 7Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 7Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 7Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 4Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 4Homo sapiens (human)
neurotransmitter secretionMetabotropic glutamate receptor 4Homo sapiens (human)
positive regulation of MAPK cascadeMetabotropic glutamate receptor 4Homo sapiens (human)
regulation of neuron apoptotic processMetabotropic glutamate receptor 4Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 4Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityMetabotropic glutamate receptor 8Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 8Homo sapiens (human)
group III metabotropic glutamate receptor activityMetabotropic glutamate receptor 8Homo sapiens (human)
G protein-coupled receptor activityMetabotropic glutamate receptor 5Homo sapiens (human)
protein bindingMetabotropic glutamate receptor 5Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 5Homo sapiens (human)
protein tyrosine kinase activator activityMetabotropic glutamate receptor 5Homo sapiens (human)
A2A adenosine receptor bindingMetabotropic glutamate receptor 5Homo sapiens (human)
identical protein bindingMetabotropic glutamate receptor 5Homo sapiens (human)
protein tyrosine kinase bindingMetabotropic glutamate receptor 5Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activityMetabotropic glutamate receptor 5Homo sapiens (human)
neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentrationMetabotropic glutamate receptor 5Homo sapiens (human)
G protein-coupled receptor activity involved in regulation of postsynaptic membrane potentialMetabotropic glutamate receptor 5Homo sapiens (human)
G protein-coupled receptor activityMetabotropic glutamate receptor 1Homo sapiens (human)
protein bindingMetabotropic glutamate receptor 1Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 1Homo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentrationMetabotropic glutamate receptor 1Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activityMetabotropic glutamate receptor 1Homo sapiens (human)
neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentrationMetabotropic glutamate receptor 1Homo sapiens (human)
G protein-coupled receptor activity involved in regulation of postsynaptic membrane potentialMetabotropic glutamate receptor 1Homo sapiens (human)
G protein-coupled receptor activityMetabotropic glutamate receptor 2Homo sapiens (human)
calcium channel regulator activityMetabotropic glutamate receptor 2Homo sapiens (human)
protein bindingMetabotropic glutamate receptor 2Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 2Homo sapiens (human)
scaffold protein bindingMetabotropic glutamate receptor 2Homo sapiens (human)
group II metabotropic glutamate receptor activityMetabotropic glutamate receptor 2Homo sapiens (human)
group III metabotropic glutamate receptor activityMetabotropic glutamate receptor 7Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 7Homo sapiens (human)
adenylate cyclase inhibitor activityMetabotropic glutamate receptor 7Homo sapiens (human)
protein dimerization activityMetabotropic glutamate receptor 7Homo sapiens (human)
serine bindingMetabotropic glutamate receptor 7Homo sapiens (human)
G protein-coupled receptor activityMetabotropic glutamate receptor 4Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 4Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activityMetabotropic glutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
plasma membraneMetabotropic glutamate receptor 8Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 8Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneMetabotropic glutamate receptor 1Rattus norvegicus (Norway rat)
plasma membraneMetabotropic glutamate receptor 4Rattus norvegicus (Norway rat)
dendriteMetabotropic glutamate receptor 5Homo sapiens (human)
cytoplasmMetabotropic glutamate receptor 5Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 5Homo sapiens (human)
dendritic spineMetabotropic glutamate receptor 5Homo sapiens (human)
dendritic shaftMetabotropic glutamate receptor 5Homo sapiens (human)
astrocyte projectionMetabotropic glutamate receptor 5Homo sapiens (human)
Schaffer collateral - CA1 synapseMetabotropic glutamate receptor 5Homo sapiens (human)
glutamatergic synapseMetabotropic glutamate receptor 5Homo sapiens (human)
postsynaptic density membraneMetabotropic glutamate receptor 5Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
nucleusMetabotropic glutamate receptor 1Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 1Homo sapiens (human)
dendriteMetabotropic glutamate receptor 1Homo sapiens (human)
Schaffer collateral - CA1 synapseMetabotropic glutamate receptor 1Homo sapiens (human)
glutamatergic synapseMetabotropic glutamate receptor 1Homo sapiens (human)
G protein-coupled receptor dimeric complexMetabotropic glutamate receptor 1Homo sapiens (human)
G protein-coupled receptor homodimeric complexMetabotropic glutamate receptor 1Homo sapiens (human)
postsynaptic density membraneMetabotropic glutamate receptor 1Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 1Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 2Homo sapiens (human)
axonMetabotropic glutamate receptor 2Homo sapiens (human)
dendriteMetabotropic glutamate receptor 2Homo sapiens (human)
presynaptic membraneMetabotropic glutamate receptor 2Homo sapiens (human)
astrocyte projectionMetabotropic glutamate receptor 2Homo sapiens (human)
glutamatergic synapseMetabotropic glutamate receptor 2Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 2Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 7Homo sapiens (human)
cell cortexMetabotropic glutamate receptor 7Homo sapiens (human)
membraneMetabotropic glutamate receptor 7Homo sapiens (human)
axonMetabotropic glutamate receptor 7Homo sapiens (human)
dendriteMetabotropic glutamate receptor 7Homo sapiens (human)
asymmetric synapseMetabotropic glutamate receptor 7Homo sapiens (human)
dendritic shaftMetabotropic glutamate receptor 7Homo sapiens (human)
postsynaptic membraneMetabotropic glutamate receptor 7Homo sapiens (human)
presynaptic active zoneMetabotropic glutamate receptor 7Homo sapiens (human)
receptor complexMetabotropic glutamate receptor 7Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 7Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 4Homo sapiens (human)
cytoplasmic vesicleMetabotropic glutamate receptor 4Homo sapiens (human)
presynapseMetabotropic glutamate receptor 4Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (46)

Assay IDTitleYearJournalArticle
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346254Rat mGlu5 receptor (Metabotropic glutamate receptors)2000Journal of neurochemistry, Dec, Volume: 75, Issue:6
Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections.
AID1346276Rat mGlu1 receptor (Metabotropic glutamate receptors)2003Molecular pharmacology, May, Volume: 63, Issue:5
[3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID159240Agonistic activity against phospholipase C (PLC) was determined in adult rat hippocampal slices1999Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14
(2R,1'S,2'R,3'S)-2-(2'-Carboxy-3'-phenylcyclopropyl)glycine (PCCG-13), the first potent and selective competitive antagonist of phospholipase D-coupled metabotropic glutamate receptors: asymmetric synthesis and preliminary biological properties.
AID107261Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7).2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID108646Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.1999Journal of medicinal chemistry, Dec-30, Volume: 42, Issue:26
Modeling of amino-terminal domains of group I metabotropic glutamate receptors: structural motifs affecting ligand selectivity.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID108489Agonist potency against cloned human metabotropic glutamate receptor 12000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID109341Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID108830Agonist potency against cloned Metabotropic glutamate receptor 2 (mGluR-2).2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID226293Potency at metabotropic glutamate receptor 2, measured as the ratio of EC50 to IC50; No effect at 1 mM2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.
AID107274Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID1253085Toxic epileptiform activity in C57BL/6 mouse CA3 region of hippocampus assessed as frequency of spike activity at 50 uM by electrophysiolgy method (Rvb = 0.94 +/- 0.06 Hz)2015Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and M
AID246705Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Inactive2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Virtual screening workflow development guided by the "receiver operating characteristic" curve approach. Application to high-throughput docking on metabotropic glutamate receptor subtype 4.
AID231223Potency at metabotropic glutamate receptor 1, measured as the ratio of EC50 to IC502002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.
AID108986Ratio between the measured EC50 and the glutamate EC50 measured against Metabotropic glutamate receptor 2; No effect1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Agonist selectivity of mGluR1 and mGluR2 metabotropic receptors: a different environment but similar recognition of an extended glutamate conformation.
AID107059Agonist potency against cloned metabotropic glutamate receptor 52000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID108506Ratio between EC50 of compound and glutamate measured against metabotropic glutamate receptor 11999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Agonist selectivity of mGluR1 and mGluR2 metabotropic receptors: a different environment but similar recognition of an extended glutamate conformation.
AID108493Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.
AID159245Antagonistic activity against phospholipase D (PLD) was determined in adult rat hippocampal slices1999Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14
(2R,1'S,2'R,3'S)-2-(2'-Carboxy-3'-phenylcyclopropyl)glycine (PCCG-13), the first potent and selective competitive antagonist of phospholipase D-coupled metabotropic glutamate receptors: asymmetric synthesis and preliminary biological properties.
AID226294Potency at metabotropic glutamate receptor 4, measured as the ratio of EC50 to IC50; No effect at 1 mM2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.
AID108837Binding affinity at Metabotropic glutamate receptor 22002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.
AID75015The effective concentration for 50% glutamate response was measured on Group I Metabotropic glutamate receptor1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Pharmacophore models of group I and group II metabotropic glutamate receptor agonists. Analysis of conformational, steric, and topological parameters affecting potency and selectivity.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (312)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's79 (25.32)18.2507
2000's151 (48.40)29.6817
2010's70 (22.44)24.3611
2020's12 (3.85)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 8.74

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index8.74 (24.57)
Research Supply Index5.71 (2.92)
Research Growth Index4.46 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (8.74)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (0.33%)5.53%
Trials0 (0.00%)5.53%
Reviews1 (0.33%)6.00%
Reviews1 (4.55%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other299 (99.34%)84.16%
Other21 (95.45%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]