Compounds > a 794282
Page last updated: 2024-11-12

a 794282

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Cross-References

ID SourceID
PubMed CID11530404
CHEMBL ID385336
SCHEMBL ID8241845
MeSH IDM0521819

Synonyms (16)

Synonym
CHEMBL385336 ,
9-dimethylamino-3-(4-ethyl-phenyl)-3h-pyrido[3'',2'':4,5]thieno[3,2-d]pyrimidin-4-one
bdbm50177053
869802-44-8
13-(dimethylamino)-5-(4-ethylphenyl)-8-thia-3,5,10-triazatricyclo[7.4.0.0^{2,7}]trideca-1(13),2(7),3,9,11-pentaen-6-one
a794282
gtpl6211
compound 1n [pmid: 16279797]
a-794282
a 794282
SCHEMBL8241845
13-(dimethylamino)-5-(4-ethylphenyl)-8-thia-3,5,10-triazatricyclo[7.4.0.02,7]trideca-1(13),2(7),3,9,11-pentaen-6-one
DTXSID10468132
VCUKKMIXURRDKL-UHFFFAOYSA-N
Q27074083
AKOS040747711
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Metabotropic glutamate receptor 1Rattus norvegicus (Norway rat)IC50 (µMol)0.00370.00020.58878.9900AID271550; AID362992
Type-1A angiotensin II receptor Rattus norvegicus (Norway rat)IC50 (µMol)1.33000.00040.15553.8000AID271551
Type-1B angiotensin II receptorRattus norvegicus (Norway rat)IC50 (µMol)1.33000.00040.13343.8000AID271551
Metabotropic glutamate receptor 5Rattus norvegicus (Norway rat)IC50 (µMol)1.33000.00000.52627.9700AID271551
Metabotropic glutamate receptor 5Rattus norvegicus (Norway rat)Ki0.19400.00050.19643.7600AID282964
AcetylcholinesteraseRattus norvegicus (Norway rat)IC50 (µMol)0.88600.00020.52597.2000AID271539; AID271551
Metabotropic glutamate receptor 5Homo sapiens (human)IC50 (µMol)0.44200.00050.439410.0000AID271539; AID282966
Metabotropic glutamate receptor 1Homo sapiens (human)IC50 (µMol)0.00300.00052.01408.8000AID271536; AID282965; AID313149
Metabotropic glutamate receptor 2Homo sapiens (human)IC50 (µMol)10.00000.00290.46624.3000AID271537
Metabotropic glutamate receptor 7Homo sapiens (human)IC50 (µMol)10.00000.99000.99000.9900AID271540
Metabotropic glutamate receptor 4Homo sapiens (human)IC50 (µMol)10.00000.00510.00510.0051AID271538
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (44)

Processvia Protein(s)Taxonomy
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 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 1Rattus 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)
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 (45)

Assay IDTitleYearJournalArticle
AID271537Antagonist activity at human mGluR2 expressed in 1321N1 cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID271549Activity in ip dosed rat Rotarod model2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID271550Antagonist activity at rat mGluR1 expressed in 1321N1 cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID282966Antagonist activity at human mGluR5 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
AID271542Efficacy in ip dosed rat CFA model after 30 mins2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID282970Effect on locomotory activity ip dosed Sprague-Dawley rat assessed by rotarod test after 30 mins2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
AID282973Volume of distribution in rat2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
AID282976Bioavailability in orally dosed rat2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
AID271557Bioavailability in ip dosed rat2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID271554Drug level in rat brain at 30 umol/kg, ip2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID313157Effect on CFA-induced hyperalgesia in ip dosed rat2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Prospects for metabotropic glutamate 1 receptor antagonists in the treatment of neuropathic pain.
AID271555Free drug level in rat brain2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID313158Effect on carrageenan model of inflammatory pain in ip dosed rat2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Prospects for metabotropic glutamate 1 receptor antagonists in the treatment of neuropathic pain.
AID282972Half life in rat2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
AID271558Bioavailability in orally dosed rat2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID282968Analgesic effect in ip dosed Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia after 30 mins2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
AID271540Antagonist activity at human mGluR7 expressed in 1321N1 cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID282963Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranes2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
AID271541Selectivity for human mGluR1 over mGluR5 receptor2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID271552Ratio of drug level in plasma against brain in rat after 30 mins at 30 umol/kg, ip2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID282967Analgesic effect in ip dosed Sprague-Dawley rat model of CFA-induced thermal hyperalgesia after 30 mins2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
AID271539Antagonist activity at human mGluR5 expressed in 1321N1 cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID282971Sedative effect in Sprague-Dawley rat2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
AID313149Antagonist activity at mGlu1 receptor2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Prospects for metabotropic glutamate 1 receptor antagonists in the treatment of neuropathic pain.
AID282977Selectivity for rat mGluR1 over rat mGluR52005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
AID313156Effect on pain in ip dosed rat in late phase of formalin assay2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Prospects for metabotropic glutamate 1 receptor antagonists in the treatment of neuropathic pain.
AID271548Activity in ip dosed rat locomotor model2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID271543Efficacy in ip dosed rat Carrageenan model after 30 mins2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID271553Efficacy in rat Chung spinal nerve L5/L6 ligation pain model after 30 mins at 100 umol/kg, ip2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID282964Displacement of [3H]MPEP from rat cortex mGluR52005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
AID271551Antagonist activity at rat mGluR5 expressed in 1321N1 cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID271556Protein binding in rat brain2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID362992Inhibition of rat mGluR12008European journal of medicinal chemistry, May, Volume: 43, Issue:5
3D-QSAR studies of triazafluorenone inhibitors of metabotropic glutamate receptor subtype 1.
AID282965Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
AID282974Cmax in ip dosed rat2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
AID271538Antagonist activity at human mGluR4 expressed in 1321N1 cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID282975Bioavailability in ip dosed rat2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
AID271547Efficacy in ip dosed rat Chung spinal nerve L5/L6 ligation pain model after 30 mins2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID271545Efficacy in ip dosed rat formalin model after 30 mins2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID271546Efficacy in ip dosed rat osteoarthritic pain model after 30 mins2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID271536Antagonist activity at human mGluR1 expressed in 1321N1 cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID271544Efficacy in ip dosed rat skin incision model after 30 mins2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
AID282969Analgesic effect in ip dosed Sprague-Dawley rat model of formalin-induced spontaneous pain after 30 mins2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
AID1346276Rat mGlu1 receptor (Metabotropic glutamate receptors)2008European journal of pharmacology, Feb-12, Volume: 580, Issue:3
Analgesic activity of metabotropic glutamate receptor 1 antagonists on spontaneous post-operative pain in rats.
AID1346268Human mGlu1 receptor (Metabotropic glutamate receptors)2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (100.00)29.6817
2010's0 (0.00)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: 12.56

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 Index12.56 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
alpha-methyl-4-carboxyphenylglycine
alpha-methyl-4-carboxyphenylglycine: glutamate receptor antagonist. (S)-alpha-methyl-4-carboxyphenylglycine : A non-proteinogenic alpha-amino acid that is alanine in which the alpha-hydrogen is replaced by a 4-carboxyphenyl group (the S-enantiomer). It is a non-selective group I/group II metabotropic glutamate receptor (mGluR) antagonist.		3.1310non-proteinogenic alpha-amino acidmetabotropic glutamate receptor antagonist
upf 596
UPF 596: structure in first source		3.1310
4-carboxy-3-hydroxyphenylglycine
[no description available]		3.1310
bay36-7620
BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity. ; structure in first source		3.1310
jnj16259685
[no description available]		3.1310organic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
a-841720
A-841720: structure in first source		2.9540
ConditionIndicatedRelationship StrengthStudiesTrials
Ache
[description not available]		03.3520
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		03.3520
Peripheral Nerve Diseases
[description not available]		02.9510
Peripheral Nervous System Diseases
Diseases of the peripheral nerves external to the brain and spinal cord, which includes diseases of the nerve roots, ganglia, plexi, autonomic nerves, sensory nerves, and motor nerves.		02.9510
Acute Post-operative Pain
[description not available]		02.0410
Pain, Postoperative
Pain during the period after surgery.		02.0410