Compounds > cfm 2
Page last updated: 2024-12-10

cfm 2

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Description

CFM 2: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4377504
CHEMBL ID279218
CHEBI ID107638
SCHEMBL ID1056361
MeSH IDM0304868

Synonyms (37)

Synonym
HMS3267G18
BRD-K42859542-001-01-7
BPBIO1_001170
NCGC00024988-01 ,
tocris-1082
BIOMOL-NT_000179
NCGC00024988-02
CHEBI:107638
CHEMBL279218
1-(4-aminophenyl)-7,8-dimethoxy-3,5-dihydro-2,3-benzodiazepin-4-one
cfm-2
cfm 2
1-(4'-aminophenyl)-3,5-dihydro-7,8-dimethoxy-4h-2,3-benzodiazepin-4-one
178616-26-7
SCHEMBL1056361
CS-3625
1-(4-amino-phenyl)-7,8-dimethoxy-3,5-dihydro-benzo[d][1,2]diazepin-4-one
HB0179
HY-12503
AKOS024456374
DTXSID10402591
Q27185961
sr-01000597376
SR-01000597376-1
J-011389
(z)-1-(4-aminophenyl)-7,8-dimethoxy-3h-benzo[d][1,2]diazepin-4(5h)-one
cfm2;cfm 2
BCP23930
FT-0711883
1-(4-aminophenyl)-7,8-dimethoxy-3h-benzo[d][1,2]diazepin-4(5h)-one
HMS3676G05
HMS3412G05
BRD-K42859542-001-02-5
A911180
MS-24535
E98695
4h-2,3-benzodiazepin-4-one, 1-(4-aminophenyl)-3,5-dihydro-7,8-dimethoxy-

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Both compounds, given intracerebroventricularly at doses which did not show marked anticonvulsant activity, produced a consistent shift to the left of the dose-response curves (i."( Group III mGlu receptor agonists potentiate the anticonvulsant effect of AMPA and NMDA receptor block.
Chimirri, A; De Sarro, G; Meldrum, BS, 2002)		0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzodiazepineA group of heterocyclic compounds with a core structure containing a benzene ring fused to a diazepine ring.
[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 (30)

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
USP1 protein, partialHomo sapiens (human)Potency56.23410.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency19.36230.000811.382244.6684AID686978; AID686979
cytochrome P450 2C19 precursorHomo sapiens (human)Potency15.84890.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency39.81070.00636.904339.8107AID883
mitogen-activated protein kinase 1Homo sapiens (human)Potency25.11890.039816.784239.8107AID995
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency12.58930.031610.279239.8107AID884; AID885
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency39.81070.00638.235039.8107AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
[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)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Molecular Functions (1)

Processvia Protein(s)Taxonomy
protein bindingGlutamate receptor 4Mus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (64)

Assay IDTitleYearJournalArticle
AID129620Compound was evaluated for anticonvulsant activity against AMPA induced seizures in DBA/2 mice( tonic phase)1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists.
AID132757In vivo anticonvulsant activity in mouse determined by maximum electroshock induced seizure (MES) assay1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Synthesis of 7,8-(methylenedioxy)-1-phenyl-3,5-dihydro-4H-2, 3-benzodiazepin-4-ones as novel and potent noncompetitive AMPA receptor antagonists.
AID113630Anticonvulsant activity against tonic phase of the audiogenic seizures in DBA / 2 mice 30 min after ip administration at a dose range 3.3-100 uM/kg1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.
AID53256Anticonvulsant activity against audiogenic seizures in DBA/2 mice 30 min after intraperitoneal administration (tonic phase)2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
Discovery of a novel and highly potent noncompetitive AMPA receptor antagonist.
AID53252Anticonvulsant activity against Audiogenic seizures in DBA/2 mice was observed in tonic phase after intraperitoneal injection2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives.
AID53255Anticonvulsant activity against audiogenic seizures in DBA/2 mice 30 min after intraperitoneal administration (clonic phase)2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
Discovery of a novel and highly potent noncompetitive AMPA receptor antagonist.
AID53431Evaluated for anticonvulsant property in DBA/2 mice against Audiogenic seizures during clonic phase (ip administration); value ranges from 9.01-24.02000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones.
AID223110Anticonvulsant activity was determined when tested at 15 min from intraperitoneal administration2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones.
AID114475Audiogenic seizures after pretreatment with Aniracetam in DBA / 2 mice tonic phase at a dose range of 10-200 uM/kg1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.
AID113023In vivo anticonvulsant activity was measured as median effective dose required to prevent clonic phase of seizure in DBA/2 mice2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
QSAR study of anticonvulsant negative allosteric modulators of the AMPA receptor.
AID113774Anticonvulsant activity against tonic seizures induced by icv injection of AMPA in DBA/2 mice1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists.
AID113623Anticonvulsant activity against tonic phase of the audiogenic seizures after concomitant with flumazenil at 24.72 umol dose in DBA/2 mice1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists.
AID129619Compound was evaluated for anticonvulsant activity against AMPA induced seizures in DBA/2 mice( clonic phase)1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists.
AID129625Compound was evaluated for anticonvulsant activity against audiogenic induced seizures after pretreatment with aniracetam (clonic phase); p <0.011998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists.
AID113625Anticonvulsant activity against tonic phase of the audiogenic seizures after pretreatment with aniracetam in DBA/2 mice1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists.
AID113598Anticonvulsant activity against clonic phase of the audiogenic seizures in DBA / 2 mice 30 min after ip administration at a dose range 3.3-100 uM/kg1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.
AID53253Anticonvulsant activity against Audiogenic seizures in DBA/2 mice was observed in tonic phase after pretreatment with Aniracetam2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives.
AID113459Anticonvulsant activity against clonic phase of the audiogenic seizures after concomitant with flumazenil at 8.24 umol dose in DBA/2 mice1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists.
AID129622Compound was evaluated for anticonvulsant activity against PTZ induced seizures (clonic phase) in swiss mice1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists.
AID20517Relative lipophilicity1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists.
AID113607Anticonvulsant activity against pentylenetetrazole (PTZ)-induced seizures in swiss mice1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists.
AID113603Anticonvulsant activity against clonic seizures induced by icv injection of AMPA in DBA/2 mice1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists.
AID234046Therapeutic index (TD50/ED50) from the clonic phase of the audiogenic seizures1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists.
AID235209Therapeutic index is the ratio between TD50 and ED50 (from the clonic phase of the audiogenic seizures); value ranges from 39.3-82.12000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones.
AID20515Relative Lipophilicity measured by reversed-phase high performance thin-layer chromatography (RP-HPTLC)2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones.
AID113620Anticonvulsant activity against the tonic seizures induced by icv injection of AMPA in DBA / 2 mice at a dose range of 10-100 uM/kg1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.
AID235218Therapeutic index it is the ratio between TD50 and ED50 (from the clonic phase of the audiogenic seizures)1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.
AID212209Compound was evaluated for toxic dose on locomotor assessed by rotarod test in mice1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists.
AID212215Motor toxicity in 50% of mice on locomotion assessed by Rotarod test following 30 min ip administration1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.
AID113460Anticonvulsant activity against clonic phase of the audiogenic seizures after pretreatment with aniracetam in DBA/2 mice1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists.
AID114473Audiogenic seizures after pretreatment with Aniracetam in DBA / 2 mice clonic phase at a dose range of 10-200 uM/kg1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.
AID53444Evaluated for anticonvulsant property in DBA/2 mice against Locomotion assessed by Rotarod test (ip administration)2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones.
AID113624Anticonvulsant activity against tonic phase of the audiogenic seizures after concomitant with flumazenil at 8.24 umol dose in DBA/2 mice1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists.
AID129634Compound was evaluated for anticonvulsant activity against audiogenic seizures in DBA/2 mice( tonic phase)1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists.
AID270294Anticonvulsant activity against tonic phase of audiogenic seizures in ip dosed DBA/2 mouse2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Novel potent anticonvulsant agent containing a tetrahydroisoquinoline skeleton.
AID113024In vivo anticonvulsant activity was measured as median effective dose required to prevent tonic phase of seizure in DBA/2 mice2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
QSAR study of anticonvulsant negative allosteric modulators of the AMPA receptor.
AID53250Anticonvulsant activity against Audiogenic seizures in DBA/2 mice was observed in clonic phase after intraperitoneal injection2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives.
AID113450Anticonvulsant activity against audiogenic seizures in DBA/2 mice (value required to prevent clonic phases of seizures).1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists.
AID209500Anticonvulsant activity against PTZ induced seizures was observed in mice after intraperitoneal injection2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives.
AID113605Anticonvulsant activity against maximal electroshock (MES) seizures in swiss mice1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists.
AID113612Anticonvulsant activity against the clonic seizures induced by icv injection of AMPA in DBA / 2 mice at a dose range of 10-100 uM/kg1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.
AID114471Audiogenic seizures after concomitant treatment with Flumazenil (8.24 uM) in DBA / 2 mice clonic phase1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.
AID231693Ratio between TD50 and ED50 from the clonic phase of the audiogenic seizures was determined1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists.
AID179586In vitro inhibition of AMPA activated current in xenopus oocytes expressing rat cerebral cortex poly(A)+ RNA.1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Synthesis of 7,8-(methylenedioxy)-1-phenyl-3,5-dihydro-4H-2, 3-benzodiazepin-4-ones as novel and potent noncompetitive AMPA receptor antagonists.
AID114072Pentylenetetrazole-induced seizures in Swiss mice after 45 min pretreatment at a dose range 10-150 uM/kg1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.
AID212213Dose which induced 50% of mice to fall from the rotarod1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists.
AID113452Anticonvulsant activity against audiogenic seizures in DBA/2 mice (values required to prevent tonic phases of seizures).1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists.
AID114470Audiogenic seizures after concomitant treatment with Flumazenil (24.72 uM) in DBA / 2 mice tonic phase1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.
AID129633Compound was evaluated for anticonvulsant activity against audiogenic seizures in DBA/2 mice( clonic phase)1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists.
AID20516Relative lipophilicity of compound1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.
AID53126Anticonvulsant activity against AMPA-induced seizures in DBA/2 mice was observed in tonic phase after intraperitoneal injection2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives.
AID129630Compound was evaluated for anticonvulsant activity against audiogenic induced seizures after pretreatment with aniracetam (tonic phase); p <0.011998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists.
AID113458Anticonvulsant activity against clonic phase of the audiogenic seizures after concomitant with flumazenil at 24.72 umol dose in DBA/2 mice1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists.
AID114469Audiogenic seizures after concomitant treatment with Flumazenil (24.72 uM) in DBA / 2 mice clonic phase1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.
AID209504Anticonvulsant activity against in MES was observed in mice after intraperitoneal injection2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives.
AID113617Anticonvulsant activity against the maximal electroshock in Swiss mice after 45 minutes pretreatment at a dose range 10-150 uM/kg1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.
AID53251Anticonvulsant activity against Audiogenic seizures in DBA/2 mice was observed in clonic phase after pretreatment with Aniracetam2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives.
AID270293Anticonvulsant activity against clonic phase of audiogenic seizures in ip dosed DBA/2 mouse2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Novel potent anticonvulsant agent containing a tetrahydroisoquinoline skeleton.
AID114472Audiogenic seizures after concomitant treatment with Flumazenil (8.24 uM) in DBA / 2 mice tonic phase1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.
AID53438Evaluated for anticonvulsant property in DBA/2 mice against Audiogenic seizures during tonic phase (ip administration); value ranges from 8.01-19.02000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones.
AID53125Anticonvulsant activity against AMPA-induced seizures in DBA/2 mice was observed in clonic phase after intraperitoneal injection2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives.
AID129621Compound was evaluated for anticonvulsant activity against MES induced seizures(tonic phase) in swiss mice1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (22)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (22.73)18.2507
2000's14 (63.64)29.6817
2010's1 (4.55)24.3611
2020's2 (9.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 31.96

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index31.96 (24.57)
Research Supply Index3.14 (2.92)
Research Growth Index4.65 (4.65)
Search Engine Demand Index51.21 (26.88)
Search Engine Supply Index2.67 (0.95)

This Compound (31.96)

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%
Other22 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid: An IBOTENIC ACID homolog and glutamate agonist. The compound is the defining agonist for the AMPA subtype of glutamate receptors (RECEPTORS, AMPA). It has been used as a radionuclide imaging agent but is more commonly used as an experimental tool in cell biological studies.		2.0310non-proteinogenic alpha-amino acid
celecoxib
[no description available]		2.0310organofluorine compound;
pyrazoles;
sulfonamide;
toluenes		cyclooxygenase 2 inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
diclofenac
Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position.		2.0310amino acid;
aromatic amine;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
gyki 52466
GYKI 52466: an AMPA (non-NMDA) receptor antagonist; structure given in first source		3.96130benzodiazepine
memantine
[no description available]		2.0310adamantanes;
primary aliphatic amine		antidepressant;
antiparkinson drug;
dopaminergic agent;
neuroprotective agent;
NMDA receptor antagonist
nimesulide
nimesulide: structure. nimesulide : An aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups.		2.0310aromatic ether;
C-nitro compound;
sulfonamide		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
sulfasalazine
Sulfasalazine: A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907). sulfasalazine : An azobenzene consisting of diphenyldiazene having a carboxy substituent at the 4-position, a hydroxy substituent at the 3-position and a 2-pyridylaminosulphonyl substituent at the 4'-position.		2.0310
pentylenetetrazole
Pentylenetetrazole: A pharmaceutical agent that displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GAMMA-AMINOBUTYRIC ACID antagonist. Pentylenetetrazole has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility.. pentetrazol : An organic heterobicyclic compound that is 1H-tetrazole in which the hydrogens at positions 1 and 5 are replaced by a pentane-1,5-diyl group. A central and respiratory stimulant, it was formerly used for the treatment of cough and other respiratory tract disorders, cardiovascular disorders including hypotension, and pruritis.		210organic heterobicyclic compound;
organonitrogen heterocyclic compound
quinoxalines
quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.		2.0310mancude organic heterobicyclic parent;
naphthyridine;
ortho-fused heteroarene
cyclopentane
Cyclopentanes: A group of alicyclic hydrocarbons with the general formula R-C5H9.. cyclopentanes : Cyclopentane and its derivatives formed by substitution.		2.0110cycloalkane;
cyclopentanes;
volatile organic compound		non-polar solvent
kainic acid
Kainic Acid: (2S-(2 alpha,3 beta,4 beta))-2-Carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid. Ascaricide obtained from the red alga Digenea simplex. It is a potent excitatory amino acid agonist at some types of excitatory amino acid receptors and has been used to discriminate among receptor types. Like many excitatory amino acid agonists it can cause neurotoxicity and has been used experimentally for that purpose.		2.0310dicarboxylic acid;
L-proline derivative;
non-proteinogenic L-alpha-amino acid;
pyrrolidinecarboxylic acid		antinematodal drug;
excitatory amino acid agonist
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.		2.0310glutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
methotrexate
[no description available]		2.0310dicarboxylic acid;
monocarboxylic acid amide;
pteridines		abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent
naproxen
Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.. naproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes.		2.0310methoxynaphthalene;
monocarboxylic acid		antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
gout suppressant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
ly 300164
talampanel: AMPA receptor antagonist		2.9340benzodioxoles
2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline
2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline: structure given in first source; neuroprotectant for cerebral ischemia; AMPA receptor antagonist		2.0310naphthalenes;
sulfonic acid derivative
5-nitro-6,7,8,9-tetrahydrobenzo(g)indole-2,3-dione-3-oxime
5-nitro-6,7,8,9-tetrahydrobenzo(G)indole-2,3-dione-3-oxime: a non-NMDA receptor antagonist; shows selective displacement of low-affinity kainate binding; structure given in first source		2.0310
dizocilpine maleate
Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.. dizocilpine maleate : A maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid.		2.0310maleate salt;
tetracyclic antidepressant		anaesthetic;
anticonvulsant;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist
4,5-dihydro-7,8-dimethoxy-1-phenyl-3h-2,3-benzodiazepin-4-one
4,5-Dihydro-7,8-dimethoxy-1-phenyl-3H-2,3-benzodiazepin-4-one: structure in first source		3.150
ConditionIndicatedRelationship StrengthStudiesTrials
Absence Seizure
[description not available]		03.6190
Seizures
Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.		03.6190
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.7530
Aura
[description not available]		02.4120
Epilepsy
A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)		02.4120
Congenital Zika Syndrome
[description not available]		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Innate Inflammatory Response
[description not available]		02.0410
Ache
[description not available]		02.0410
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		02.0410
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		02.0410
Convulsive Generalized Seizure Disorder
[description not available]		02.0310
Absence Seizure Disorder
[description not available]		02.0310
Epilepsy, Absence
A seizure disorder usually occurring in childhood characterized by rhythmic electrical brain discharges of generalized onset. Clinical features include a sudden cessation of ongoing activity usually without loss of postural tone. Rhythmic blinking of the eyelids or lip smacking frequently accompanies the SEIZURES. The usual duration is 5-10 seconds, and multiple episodes may occur daily. Juvenile absence epilepsy is characterized by the juvenile onset of absence seizures and an increased incidence of myoclonus and tonic-clonic seizures. (Menkes, Textbook of Child Neurology, 5th ed, p736)		02.0310
Bladder, Overactive
[description not available]		02.0310
Bladder Neck Obstruction
[description not available]		02.0310
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		02.0310
Urinary Bladder, Overactive
Symptom of overactive detrusor muscle of the URINARY BLADDER that contracts with abnormally high frequency and urgency. Overactive bladder is characterized by the frequent feeling of needing to urinate during the day, during the night, or both. URINARY INCONTINENCE may or may not be present.		02.0310
Adenocarcinoma, Basal Cell
[description not available]		02.0310
Cancer of Lung
[description not available]		02.0310
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		02.0310
Lung Neoplasms
Tumors or cancer of the LUNG.		02.0310