Page last updated: 2024-12-08

ly 300164

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Description

talampanel: AMPA receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID164509
CHEMBL ID61872
CHEBI ID34992
SCHEMBL ID118011
MeSH IDM0226357

Synonyms (59)

Synonym
gyki-53773
idr-53773
ly-300164
kinampa
ampanel
talampanel (inn)
D02696
ly 300164
7h-1,3-dioxolo(4,5-h)(2,3)benzodiazepine, 7-acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-, (8r)-
7h-1,3-dioxolo(4,5-h)(2,3)benzodiazepine, 7-acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-, (r)-
7h-1,3-dioxolo(4,5-h)(2,3)benzodiazepine, 8,9-dihydro-7-acetyl-5-(4-aminophenyl)-8-methyl-, (r)-
(r)-7-acetyl-5-(p-aminophenyl)-8,9-dihydro-8-methyl-7h-1,3-dioxolo(4,5-h)(2,3)benzodiazepine
(r)-(-)-1-(4-aminophenyl)-3-acetyl-4-methyl-7,8-methylenedioxy-3,4-dihydro-5h-2,3-benzodiazepine
gyki 53773
161832-65-1
talampanel
C14993 ,
ly300164
(8r)-7-acetyl-5-(4-aminophenyl)-8,3-dioxolo[4,5-h][2,3]benzodiazepine
nsc729898
nsc-729898
(r)-7-acetyl-5-(p-aminophenyl)-8,3-dioxolo[4,5-h][2,3]benzodiazepine
(-)-talampanel
CHEMBL61872
chebi:34992 ,
AC1L4UWP ,
7h-1,3-dioxolo[4,5-h][2,3]benzodiazepine,7-acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-, (8r)-
talampanel [inn]
cvs43xg1l5 ,
unii-cvs43xg1l5
DB04982
SCHEMBL118011
talampanel [usan]
7h-1,3-dioxolo[4,5-h][2,3]benzodiazepine, 7-acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-, (8r)-
talampanel [mi]
1-[(8r)-5-(4-aminophenyl)-8-methyl-8,9-dihydro-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-7-yl]ethanone
JACAAXNEHGBPOQ-LLVKDONJSA-N
(r)-7-acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-7h-1,3-dioxolo[4,5-h][2,3]benzodiazepine
(8r)-7-acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-7h-1,3-dioxolo[4,5-h][2,3]benzodiazepine
HY-15079
CS-5225
gtpl8279
gyki 537773
AKOS024458464
DTXSID10167259
(r)-1-(5-(4-aminophenyl)-8-methyl-8,9-dihydro-7h-[1,3]dioxolo[4',5':4,5]benzo[1,2-d][1,2]diazepin-7-yl)ethanone
talampanel(ly300164)
talampanel, >=97% (hplc)
talampanel (gyki 53773)
NCGC00387224-01
talampanel, gyki-53773; ly-300164
EX-A1569
gyki-53773;ly-300164
Q7678869
1-[(8r)-5-(4-aminophenyl)-8-methyl-8,9-dihydro-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-7-yl]ethanone.
T-185
MS-25120
NCGC00387224-02
AC-35959

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" This study examines the single- and multiple-dose pharmacokinetics, safety, and tolerability of talampanel in patients with intractable epilepsy and assesses the potential for pharmacokinetic interaction."( Talampanel, a new antiepileptic drug: single- and multiple-dose pharmacokinetics and initial 1-week experience in patients with chronic intractable epilepsy.
Jewell, H; Langan, YM; Lucas, R; Patsalos, PN; Sander, JW; Schaefer, H; Toublanc, N, 2003
)
0.32
" Fourteen patients were evaluated for safety, 13 patients were used in the single-dose, and 11 patients in the multiple-dose pharmacokinetic analysis."( Talampanel, a new antiepileptic drug: single- and multiple-dose pharmacokinetics and initial 1-week experience in patients with chronic intractable epilepsy.
Jewell, H; Langan, YM; Lucas, R; Patsalos, PN; Sander, JW; Schaefer, H; Toublanc, N, 2003
)
0.32
" Unified parent-metabolite pharmacokinetic (PK) models that allowed three different rates of acetylation were used to simultaneously fit plasma levels for both the parent drug and its metabolite following genotype-based classification as slow, intermediate, or fast acetylator."( Unified pharmacogenetics-based parent-metabolite pharmacokinetic model incorporating acetylation polymorphism for talampanel in humans.
Bell, C; Bodor, N; Buchwald, P; Howes, J; Juhász, A; Pátfalusi, M, 2005
)
0.33

Compound-Compound Interactions

ExcerptReferenceRelevance
"This study was aimed at evaluating the body temperature of mice following the injection of LY 300164, an AMPA/kainate receptor antagonist, alone or in combination with carbamazepine or diphenylhydantoin."( Influence of LY 300164 alone or in combination with carbamazepine or diphenylhydantoin on the body temperature in mice.
Czuczwar, SJ; Luszczki, JJ; Swiader, MJ; Wierzchowska-Cioch, E; Zwolan, A, 2004
)
0.91

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" injections at 1-h intervals, the first dosage was given shortly after the intrastriatal injection of (S)-alpha-amino-3-hydroxy-5,7-methylisoxazole-4-propionic acid (AMPA) (2."( Protective effect of the antiepileptic drug candidate talampanel against AMPA-induced striatal neurotoxicity in neonatal rats.
Banczerowski-Pelyhe, I; Gulyás-Kovács, A; Takács, J; Tarnawa, I; Világi, I, 2002
)
0.31
" dosing regimen was then determined for each patient based on his or her initial pharmacokinetic profile."( Talampanel, a new antiepileptic drug: single- and multiple-dose pharmacokinetics and initial 1-week experience in patients with chronic intractable epilepsy.
Jewell, H; Langan, YM; Lucas, R; Patsalos, PN; Sander, JW; Schaefer, H; Toublanc, N, 2003
)
0.32
"Talampanel dosing strategies may be reliant on concomitant AED medication, as enzyme-inducing AEDs enhance, whereas VPA inhibits its metabolism."( Talampanel, a new antiepileptic drug: single- and multiple-dose pharmacokinetics and initial 1-week experience in patients with chronic intractable epilepsy.
Jewell, H; Langan, YM; Lucas, R; Patsalos, PN; Sander, JW; Schaefer, H; Toublanc, N, 2003
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzodioxoles
[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 (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency37.02590.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency6.74120.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency11.98770.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency30.76640.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (45)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (39)

Assay IDTitleYearJournalArticle
AID1347160Primary screen NINDS Rhodamine 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.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID255729Effective p.o. dose tested for anticonvulsant activity using maximal electroshock seizure model in mouse (value range= 7.0-10.6 mg/kg)2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Potential metabolites of a condensed 2,3-benzodiazepine derivative.
AID129004Anticonvulsant activity of compound, administered perorally in mice was evaluated using maximal electroshock seizure model2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
Structural analogues of some highly active non-competitive AMPA antagonists.
AID223850Compound was tested for inhibition of whole cell current induced by 5 Purkinje cells2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
Structural analogues of some highly active non-competitive AMPA antagonists.
AID496873Toxicity in human assessed as ataxia2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
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.
AID496866Anticonvulsant activity in po dosed mouse assessed as inhibition of MES-induced tonic seizures2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
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.
AID496874Toxicity in human assessed as dizziness2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID256109Activity tested as behavioural change in mouse at an i.p. dose of 100 mg/kg; (loss of righting reflex)2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Potential metabolites of a condensed 2,3-benzodiazepine derivative.
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.
AID110064Ability to abolish the hindlimb tonic extensor components of a maximal electroshock-induced seizure in vivo1999Bioorganic & medicinal chemistry letters, Jul-19, Volume: 9, Issue:14
Synthesis and anticonvulsant activity of 3-aryl-5H-2,3-benzodiazephine AMPA antagonists.
AID255907Evaluated for inhibition of AMPA (5 uM) evoked spreading depression in isolated retina prepared from young chicken2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Potential metabolites of a condensed 2,3-benzodiazepine derivative.
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.
AID256108Activity tested as behavioural change in mouse at a p.o. dose of 200 mg/kg; (loss of righting reflex)2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Potential metabolites of a condensed 2,3-benzodiazepine derivative.
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.
AID51581Compound was examined in vitro for inhibition of kainate (5 uM) evoked spreading depression in isolated retina prepared from young chicken2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
Structural analogues of some highly active non-competitive AMPA antagonists.
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.
AID496867Inhibition of AMPA-induced chicken retinal spreading depression2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID326374Inhibition of kainate-induced C57BL/6N mouse hippocampal neurons excitotoxicity after 48 hrs by MTT assay2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Structure-activity study of 2,3-benzodiazepin-4-ones noncompetitive AMPAR antagonists: identification of the 1-(4-amino-3-methylphenyl)-3,5-dihydro-7,8-ethylenedioxy-4H-2,3-benzodiazepin-4-one as neuroprotective agent.
AID129006Anticonvulsant activity of compound, administered perorally in mice was evaluated using maximal metrazole seizure model2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
Structural analogues of some highly active non-competitive AMPA 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.
AID1194211Anticonvulsant activity in po dosed ICR mouse assessed as protection from maximal electroshock-induced seizure measured after 60 mins post dose2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Synthesis, structure-activity relationships, and anticonvulsant activities of 2-amino-4H-pyrido[3,2-e][1,3]thiazin-4-one derivatives as orally active AMPA receptor antagonists.
AID131234Muscle relaxant activity of compound, administered intraperitoneally in mice was evaluated using inclined screen test2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
Structural analogues of some highly active non-competitive AMPA antagonists.
AID496869Neuroprotective activity against middle cerebral artery occlusion-induced focal cerebral ischemia in Mongolian gerbils assessed as reduction in infarct volume at 6 mg/kg, iv bid2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID130094Loss of righting reflex was observed after the intraperitoneal administration of compound in mice2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
Structural analogues of some highly active non-competitive AMPA antagonists.
AID255718Effective i.p. dose tested for muscle relaxant activity using inclined screen test in mouse (value range= 11.2-16.0 mg/kg) 2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Potential metabolites of a condensed 2,3-benzodiazepine derivative.
AID1194209Inhibition of kainate-induced neurotoxicity in primary rat hippocampal neurons after 24 hrs by LDH assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Synthesis, structure-activity relationships, and anticonvulsant activities of 2-amino-4H-pyrido[3,2-e][1,3]thiazin-4-one derivatives as orally active AMPA receptor antagonists.
AID130095Loss of righting reflex was observed after the peroral administration of compound in mice2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
Structural analogues of some highly active non-competitive AMPA 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.
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.
AID51579Compound was examined in vitro for inhibition of AMPA (5 uM) evoked spreading depression in isolated retina prepared from young chicken2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
Structural analogues of some highly active non-competitive AMPA antagonists.
AID496868Neuroprotective activity against middle cerebral artery occlusion-induced focal cerebral ischemia in Mongolian gerbils assessed survival of hippocampal CA1 neurons2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID1346560Rat GluA2 (Ionotropic glutamate receptors)2013ACS chemical neuroscience, Apr-17, Volume: 4, Issue:4
Mechanism of inhibition of the GluA2 AMPA receptor channel opening by talampanel and its enantiomer: the stereochemistry of the 4-methyl group on the diazepine ring of 2,3-benzodiazepine derivatives.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (71)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's9 (12.68)18.2507
2000's46 (64.79)29.6817
2010's13 (18.31)24.3611
2020's3 (4.23)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.25

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 Index10.25 (24.57)
Research Supply Index4.39 (2.92)
Research Growth Index4.64 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.25)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (9.59%)5.53%
Reviews5 (6.85%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other61 (83.56%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]