Compounds > mgs 0028
Page last updated: 2024-12-11

mgs 0028

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Description

MGS 0028: a group II mGluR agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9837317
CHEMBL ID121053
SCHEMBL ID2454643
MeSH IDM0376352

Synonyms (23)

Synonym
mgs0028
(1r,2s,5s,6s)-2-amino-6-fluoro-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acid
mgs 0028
mgs-0028
gtpl1395
(+)-2-amino-6-fluoro-4-oxo-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
bdbm50094843
(-)-2-amino-6-fluoro-4-oxo-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
(+/-)-2-amino-6-fluoro-4-oxo-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
2-amino-6-fluoro-4-oxo-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
CHEMBL121053 ,
260353-67-1
YMS878LR7I ,
bicyclo(3.1.0)hexane-2,6-dicarboxylic acid, 2-amino-6-fluoro-4-oxo-, (1r,2s,5s,6s)-
(+)-mgs-0028
321963-33-1
2-amino-6-fluoro-4-oxobicyclo(3.1.0)hexane-2,6-dicarboxylic acid
unii-yms878lr7i
SCHEMBL2454643
(1r,2s,5s,6s)-2-amino-6-fluoro-4-oxobicyclo[3.1.0]hexane 2,6-dicarboxylic acid
Q27086054
(1r,2s,5s,6s)-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid,2-amino-6-fluoro-4-oxo-
AKOS040748913

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" However, bioavailability was only approximately 20% in monkeys, and MGS0034 was found in relatively high abundance in plasma."( Metabolism and disposition of a potent group II metabotropic glutamate receptor agonist, in rats, dogs, and monkeys.
Brunner, J; Chen, WG; Cook, J; Cramer, M; James, JK; Nakamura, M; Nakazato, A; Zhang, KE, 2005)		0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Metabotropic glutamate receptor 2Rattus norvegicus (Norway rat)Ki0.00330.00310.12650.4760AID108996
Metabotropic glutamate receptor 3Rattus norvegicus (Norway rat)Ki0.00360.00300.13400.4760AID109312
[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 2Rattus norvegicus (Norway rat)EC50 (µMol)25.02410.00061.42627.7000AID108838; AID108843
Metabotropic glutamate receptor 3Rattus norvegicus (Norway rat)EC50 (µMol)50.00100.00211.89099.0000AID109168; AID109169
Metabotropic glutamate receptor 2Homo sapiens (human)EC50 (µMol)0.00060.00061.17848.5000AID705582
Metabotropic glutamate receptor 3Homo sapiens (human)EC50 (µMol)0.00210.00210.93225.1180AID705390
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Metabotropic glutamate receptor 6Homo sapiens (human)Activity0.10000.40001.33333.0000AID107092
Metabotropic glutamate receptor 5Homo sapiens (human)Activity100.00004.00004.55005.1000AID109492
Metabotropic glutamate receptor 1Homo sapiens (human)Activity100.00001.00001.00001.0000AID108354
Metabotropic glutamate receptor 2Homo sapiens (human)Activity0.00060.00060.76864.0000AID108670
Metabotropic glutamate receptor 3Homo sapiens (human)Activity0.00270.00271.63819.0000AID109150
Metabotropic glutamate receptor 4Homo sapiens (human)Activity100.00004.00004.00004.0000AID109324
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (49)

Processvia Protein(s)Taxonomy
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 6Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 6Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 6Homo sapiens (human)
locomotory behaviorMetabotropic glutamate receptor 6Homo sapiens (human)
detection of visible lightMetabotropic glutamate receptor 6Homo sapiens (human)
detection of light stimulus involved in visual perceptionMetabotropic glutamate receptor 6Homo sapiens (human)
retina development in camera-type eyeMetabotropic glutamate receptor 6Homo sapiens (human)
positive regulation of calcium ion import across plasma membraneMetabotropic glutamate receptor 6Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 6Homo 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)
negative regulation of adenylate cyclase activityMetabotropic glutamate receptor 3Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 3Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 3Homo sapiens (human)
gene expressionMetabotropic glutamate receptor 3Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionMetabotropic glutamate receptor 3Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 3Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 3Homo 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 (19)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityMetabotropic glutamate receptor 6Homo sapiens (human)
protein bindingMetabotropic glutamate receptor 6Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 6Homo sapiens (human)
protein homodimerization activityMetabotropic glutamate receptor 6Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activityMetabotropic glutamate receptor 6Homo 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 3Homo sapiens (human)
calcium channel regulator activityMetabotropic glutamate receptor 3Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 3Homo sapiens (human)
scaffold protein bindingMetabotropic glutamate receptor 3Homo sapiens (human)
group II metabotropic glutamate receptor activityMetabotropic glutamate receptor 3Homo 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 (27)

Processvia Protein(s)Taxonomy
Golgi membraneMetabotropic glutamate receptor 6Homo sapiens (human)
endoplasmic reticulum membraneMetabotropic glutamate receptor 6Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 6Homo sapiens (human)
dendriteMetabotropic glutamate receptor 6Homo sapiens (human)
new growing cell tipMetabotropic glutamate receptor 6Homo sapiens (human)
synapseMetabotropic glutamate receptor 6Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 6Homo sapiens (human)
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)
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 3Homo sapiens (human)
postsynaptic densityMetabotropic glutamate receptor 3Homo sapiens (human)
axonMetabotropic glutamate receptor 3Homo sapiens (human)
presynaptic membraneMetabotropic glutamate receptor 3Homo sapiens (human)
dendritic spineMetabotropic glutamate receptor 3Homo sapiens (human)
postsynaptic membraneMetabotropic glutamate receptor 3Homo sapiens (human)
astrocyte projectionMetabotropic glutamate receptor 3Homo sapiens (human)
glutamatergic synapseMetabotropic glutamate receptor 3Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 3Homo 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 (36)

Assay IDTitleYearJournalArticle
AID192827Tested for % inhibition of PCP induced hyperactivity in rats at 1 mg/kg2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID196696Tested for mGluR agonist activity by measuring the PCP induced head weaving behavior in rats at 0.03 ug/kg2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID109312Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID108670Inhibition of c-AMP by human Metabotropic glutamate receptor 2 (mGluR2) expressed in non-neuronal cells2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID109314Agonist potency against cloned Metabotropic glutamate receptor 3; NT is Not Tested.2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID109150Inhibition of c-AMP by human Metabotropic glutamate receptor 3 (mGluR3) expressed in non-neuronal cells2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID108996Tested for binding affinity against Metabotropic glutamate receptor 2 in CHO cells using [3H]-7 as radioligand2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID192821Tested for % inhibition of PCP induced head-weavings in rats at 0.3 ug/kg2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID196705Tested for mGluR agonist activity by measuring the PCP induced hyperactivity in rats at 3 mg/kg2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID108354Phosphoinositide hydrolysis by human Metabotropic glutamate receptor 1 (mGluR1) expressed in non-neuronal cells2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID107257Inhibition of c-AMP by human Metabotropic glutamate receptor 7 (mGluR7) expressed in non-neuronal cells2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID109324Inhibition of c-AMP by human Metabotropic glutamate receptor 4 (mGluR4) expressed in non-neuronal cells2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID192819Tested for % inhibition of PCP induced head-weavings in rats at 0.03 ug/kg2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID109315Antagonist activity against Metabotropic glutamate receptor 3 expressed in CHO cells was evaluated in presence of 30 uM glutamic acid; NT is Not Tested.2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID109168Agonist potency against cloned Metabotropic glutamate receptor 32000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID108838Agonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated by measuring forskolin-induced cyclic AMP formation2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID705390Agonist activity at mGLUR3 expressed in CHO cells2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Radiosynthesis of PET radiotracer as a prodrug for imaging group II metabotropic glutamate receptors in vivo.
AID109492Phosphoinositide hydrolysis by human Metabotropic glutamate receptor 5 (mGluR5) expressed in non neuronal cells2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID192825Tested for % inhibition of PCP induced hyperactivity in rats at 0.1 mg/kg2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID192826Tested for % inhibition of PCP induced hyperactivity in rats at 0.3 mg/kg2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID196698Tested for mGluR agonist activity by measuring the PCP induced head weaving behavior in rats at 0.3 ug/kg2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID108999Antagonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated in presence of 30 uM glutamic acid; NT is Not Tested.2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID705582Agonist activity at mGLUR2 expressed in CHO cells2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Radiosynthesis of PET radiotracer as a prodrug for imaging group II metabotropic glutamate receptors in vivo.
AID228189Effective dose to evaluate PCP induced hyper activity in rats after oral administration2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID107092Inhibition of c-AMP by human Metabotropic glutamate receptor 6 (mGluR6) expressed in non-neuronal cells2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID108843Antagonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated in presence of 30 uM glutamic acid2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID196700Tested for mGluR agonist activity by measuring the PCP induced hyperactivity in rats at 1 mg/kg2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID228376Tested for mGluR agonist activity by measuring the PCP induced hyperactivity in rats at 0.1 mg/kg2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID228188Effective dose to evaluate PCP induced head-weaving behavior in rats after oral administration2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID192829Tested for % inhibition of PCP induced hyperactivity in rats at 3 mg/kg2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID109169Antagonist activity against Metabotropic glutamate receptor 3 expressed in CHO cells was evaluated in presence of 30 uM glutamic acid2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID196697Tested for mGluR agonist activity by measuring the PCP induced head weaving behavior in rats at 0.1 ug/kg2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID107275Inhibition of c-AMP by human Metabotropic glutamate receptor 8 (mGluR8) expressed in non-neuronal cells2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID196699Tested for mGluR agonist activity by measuring the PCP induced hyperactivity in rats at 0.3 mg/kg2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID192820Tested for % inhibition of PCP induced head-weavings in rats at 0.1 ug/kg2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID1346287Rat mGlu2 receptor (Metabotropic glutamate receptors)2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (60.00)29.6817
2010's4 (40.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.60

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 Index12.60 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.99 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.60)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
methamphetamine
Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.. methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent.		2.0610amphetamines;
secondary amine		central nervous system stimulant;
environmental contaminant;
neurotoxin;
psychotropic drug;
xenobiotic
glutamic acid
Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.		2.0110glutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
1-amino-1,3-dicarboxycyclopentane
1-amino-1,3-dicarboxycyclopentane: RN given refers to (cis)-isomer		2.0110
eglumetad
eglumetad: LY-354740 is the active isomer, LY-366563 is the inactive isomer, and LY 314582 is the racemate; structure given in first source		2.730L-alpha-amino acid
opc 28326
OPC 28326: a hindlimb vasodilator; structure in first source		2.0210
inositol 1,4,5-trisphosphate
Inositol 1,4,5-Trisphosphate: Intracellular messenger formed by the action of phospholipase C on phosphatidylinositol 4,5-bisphosphate, which is one of the phospholipids that make up the cell membrane. Inositol 1,4,5-trisphosphate is released into the cytoplasm where it releases calcium ions from internal stores within the cell's endoplasmic reticulum. These calcium ions stimulate the activity of B kinase or calmodulin.		210myo-inositol trisphosphatemouse metabolite
l-2-(carboxypropyl)glycine
[no description available]		2.0110
2-(2,3-dicarboxycyclopropyl)glycine
[no description available]		2.0110
ly 341495
[no description available]		2.0710xanthenes
ly 379268
LY 379268: group II metabotropic glutamate receptor agonist; structure in first source. 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.		2.4420amino dicarboxylic acid;
bridged compound;
organic heterobicyclic compound		antipsychotic agent;
anxiolytic drug;
metabotropic glutamate receptor agonist;
neuroprotective agent
piperidines
Piperidines: A family of hexahydropyridines.		2.0210
ConditionIndicatedRelationship StrengthStudiesTrials
Dementia Praecox
[description not available]		0210
Schizophrenia
A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.		0210
Hyperactivity, Motor
[description not available]		02.0610
ADDH
[description not available]		02.0810
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.0810
Age-Related Memory Disorders
[description not available]		02.0810
Attention Deficit Disorder with Hyperactivity
A behavior disorder originating in childhood in which the essential features are signs of developmentally inappropriate inattention, impulsivity, and hyperactivity. Although most individuals have symptoms of both inattention and hyperactivity-impulsivity, one or the other pattern may be predominant. The disorder is more frequent in males than females. Onset is in childhood. Symptoms often attenuate during late adolescence although a minority experience the full complement of symptoms into mid-adulthood. (From DSM-V)		02.0810
Memory Disorders
Disturbances in registering an impression, in the retention of an acquired impression, or in the recall of an impression. Memory impairments are associated with DEMENTIA; CRANIOCEREBRAL TRAUMA; ENCEPHALITIS; ALCOHOLISM (see also ALCOHOL AMNESTIC DISORDER); SCHIZOPHRENIA; and other conditions.		02.0810
Rheumatoid Arthritis
[description not available]		02.0210
Nearsightedness
[description not available]		02.0210
Arthritis, Rheumatoid
A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.		02.0210
Myopia
A refractive error in which rays of light entering the EYE parallel to the optic axis are brought to a focus in front of the RETINA when accommodation (ACCOMMODATION, OCULAR) is relaxed. This results from an overly curved CORNEA or from the eyeball being too long from front to back. It is also called nearsightedness.		02.0210