zk 200775 profile

ZK 200775: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	208953
CHEMBL ID	19892
SCHEMBL ID	353357
MeSH ID	M0295106

Synonym
HMS3268N22
NCGC00159553-01
((3,4-dihydro-7-morpholino-2,3-dioxo-6-(trifluoromethyl)-1(2h)-quinoxalinyl)methyl)phosphonic acid
fanapanel
fanapanel [inn]
ZK1 ,
zk-200775
zk200775
CHEMBL19892
161605-73-8
[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-4h-quinoxalin-1-yl]methylphosphonic acid
mpqx
unii-e3ap71em0o
e3ap71em0o ,
phosphonic acid, ((3,4-dihydro-7-(4-morpholinyl)-2,3-dioxo-6-(trifluoromethyl)-1(2h)-quinoxalinyl)methyl)-
(1,2,3,4-tetrahydro-7-morpholinyl-2,3-dioxo-6-(trifluoromethyl)quinoxalin-1-yl)methylphosphonate
zk 200775
dtxcid5026093
cas-161605-73-8
tox21_111745
dtxsid7046093 ,
gtpl7636
SCHEMBL353357
NCGC00159553-02
tox21_111745_1
{[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2h)-yl]methyl}phosphonic acid
CS-3611
[[3,4-dihydro-7-(4-morpholinyl)-2,3-dioxo-6-(trifluoromethyl)-1(2h)-quinoxalinyl]methyl]phosphonic acid
HY-15069
AKOS024457062
J-009850
DB12393
((7-morpholino-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2h)-yl)methyl)phosphonic acid
HMS3677G20
zk200775 161605-73-8
BCP11020
HMS3413G20
Q19597235
A912211
F85094
wzmqmkncwdccmt-uhfffaoysa-n

Excerpt	Reference	Relevance
"ZK 200775 is an antagonist at the alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor and had earned attention as a possible neuroprotective agent in cerebral ischemia. "	( Effects of the AMPA antagonist ZK 200775 on visual function: a randomized controlled trial. Bergholz, R; Rüther, K; Staks, T, 2010)	2.09
"ZK 200775 is a selective competitive AMPA receptor antagonist. "	( The AMPA antagonist ZK 200775 in patients with acute ischaemic stroke: a double-blind, multicentre, placebo-controlled safety and tolerability study. De Keyser, J; Diener, HC; Hommel, M; Kaste, M; Lees, KR; Steiner, H; Versavel, M; Walters, MR, 2005)	2.09

Excerpt	Reference	Relevance
" Eleven patients received a total dose of 105 mg over a period of 6 hours (dose group 3; reduction of total dose and infusion time because of adverse events in group 2)."	( AMPA antagonist ZK200775 in patients with acute ischemic stroke: possible glial cell toxicity detected by monitoring of S-100B serum levels. De Keyser, J; Diener, HC; Elting, JW; Hommel, M; Kaste, M; Lees, KR; Sulter, GA; Teelken, AW; Versavel, M, 2002)	0.31

Excerpt	Reference	Relevance
"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

Protein Targets (14)

Potency Measurements

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE	Homo sapiens (human)	Potency	0.0050	0.0032	45.4673	12,589.2998	AID2517
GLS protein	Homo sapiens (human)	Potency	28.1838	0.3548	7.9355	39.8107	AID624170
estrogen receptor 2 (ER beta)	Homo sapiens (human)	Potency	3.7578	0.0006	57.9133	22,387.1992	AID1259377
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Glutamate receptor 1	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.1400	0.0001	1.6179	10.0000	AID92370
Glutamate receptor 2	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.1400	0.0001	1.7000	10.0000	AID92370
Glutamate receptor 3	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.1400	0.0001	1.7000	10.0000	AID92370
Glutamate receptor 4	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.1400	0.0001	1.7000	10.0000	AID92370
Glutamate receptor ionotropic, NMDA 1	Rattus norvegicus (Norway rat)	IC50 (µMol)	5.9833	0.0007	1.6003	10.0000	AID496836; AID496837; AID73794
Glutamate receptor ionotropic, NMDA 2A	Rattus norvegicus (Norway rat)	IC50 (µMol)	5.9833	0.0007	1.6306	10.0000	AID496836; AID496837; AID73794
Glutamate receptor ionotropic, NMDA 2B	Rattus norvegicus (Norway rat)	IC50 (µMol)	5.9833	0.0006	1.5257	10.0000	AID496836; AID496837; AID73794
Glutamate receptor ionotropic, NMDA 2C	Rattus norvegicus (Norway rat)	IC50 (µMol)	5.9833	0.0007	1.7472	10.0000	AID496836; AID496837; AID73794
Glutamate receptor ionotropic, NMDA 2D	Rattus norvegicus (Norway rat)	IC50 (µMol)	5.9833	0.0007	1.7411	10.0000	AID496836; AID496837; AID73794
Glutamate receptor ionotropic, NMDA 3B	Rattus norvegicus (Norway rat)	IC50 (µMol)	5.9833	0.0007	1.7411	10.0000	AID496836; AID496837; AID73794
Glutamate receptor ionotropic, NMDA 3A	Rattus norvegicus (Norway rat)	IC50 (µMol)	5.9833	0.0007	1.7411	10.0000	AID496836; AID496837; AID73794
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Glutamate receptor 1	Rattus norvegicus (Norway rat)	Activity	0.1050	0.1050	0.1583	0.2200	AID31451
Glutamate receptor 2	Rattus norvegicus (Norway rat)	Activity	0.1050	0.1050	0.1863	0.2700	AID31451
Glutamate receptor 3	Rattus norvegicus (Norway rat)	Activity	0.1050	0.1050	0.1583	0.2200	AID31451
Glutamate receptor 4	Rattus norvegicus (Norway rat)	Activity	0.1050	0.1050	0.1583	0.2200	AID31451
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (2)

Process	via Protein(s)	Taxonomy
plasma membrane	Glutamate receptor 1	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor 2	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 1	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 1	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2A	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 2A	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2B	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 2B	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2C	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 2C	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2D	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 2D	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 3B	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 3B	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 3A	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 3A	Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (46)

Assay ID	Title	Year	Journal	Article
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings 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.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504749	qHTS profiling for inhibitors of Plasmodium falciparum proliferation	2011	Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043	Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection	2020	ACS 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.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424	RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The Journal of biological chemistry, 11-15, Volume: 294, Issue:46	Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425	Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The Journal of biological chemistry, 11-15, Volume: 294, Issue:46	Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID113366	In vivo effective dose required to protect 6 male CD1 mice against tonic convulsions following ip administration for a pretreatment time of 30 min	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	Synthesis of anticonvulsive AMPA antagonists: 4-oxo-10-substituted-imidaz.
AID496847	Neuroprotective effect against middle cerebral artery occlusion-induced focal cerebral ischemia in iv dosed spontaneously hypertensive rat brain after 1 to 5 hrs of occlusion	2010	Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15	alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID496834	Displacement of [3H]AMPA from AMPA receptor in rat cortical membrane	2010	Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15	alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID92370	Displacement of [3H]AMPA from Ionotropic glutamate receptor AMPA of rat cortical membranes	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	Synthesis of anticonvulsive AMPA antagonists: 4-oxo-10-substituted-imidaz.
AID73794	Displacement of [3H]DCKA from glycine NMDA receptor of rat cortical membranes	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	Synthesis of anticonvulsive AMPA antagonists: 4-oxo-10-substituted-imidaz.
AID31451	Tested for in vitro binding affinity against AMPA receptor using [3H]AMPA binding assay	1998	Bioorganic & medicinal chemistry letters, Jan-06, Volume: 8, Issue:1	5-Aminomethylquinoxaline-2,3-diones. Part I: A novel class of AMPA receptor antagonists.
AID496837	Inhibition of NMDA receptor glycine site from rat cortical membrane	2010	Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15	alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID496848	Anticonvulsant activity in ip dosed rat assessed as inhibition of MES-induced tonic seizures	2010	Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15	alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID113371	In vivo effective dose required to protect 6 male CD1 mice against tonic convulsions following iv administration for a pretreatment time of 5 min	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	Synthesis of anticonvulsive AMPA antagonists: 4-oxo-10-substituted-imidaz.
AID496836	Inhibition of NMDA receptor glutamate site from rat cortical membrane	2010	Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15	alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID496835	Displacement of [3H]kainate from kainate receptor in rat cortical membrane	2010	Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15	alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID219907	Inhibition of currents generated by 50 uM kainate in Xenopus oocytes injected with rat brain mRNA	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	Synthesis of anticonvulsive AMPA antagonists: 4-oxo-10-substituted-imidaz.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	2 (8.70)	18.2507
2000's	6 (26.09)	29.6817
2010's	8 (34.78)	24.3611
2020's	7 (30.43)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	3 (13.04%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	20 (86.96%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
2-amino-5-phosphonovalerate 2-Amino-5-phosphonovalerate: The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.	2.02	1	0	non-proteinogenic alpha-amino acid	NMDA receptor antagonist
8-hydroxy-2-(di-n-propylamino)tetralin 8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.. 8-OH-DPAT : A tetralin substituted at positions 1 and 7 by hydroxy and dipropylamino groups respectively	2.04	1	0	phenols; tertiary amino compound; tetralins	serotonergic antagonist
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.	1.99	1	0	non-proteinogenic alpha-amino acid
4-aminopyridine [no description available]	2.05	1	0	aminopyridine; aromatic amine	avicide; orphan drug; potassium channel blocker
bemegride Bemegride: A CNS stimulant that is used to induce convulsions in experimental animals. It has also been used as a respiratory stimulant and in the treatment of barbiturate overdose.	2.05	1	0	piperidones
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.	2.05	1	0	organic heterobicyclic compound; organonitrogen heterocyclic compound
3-mercaptopropionic acid 3-Mercaptopropionic Acid: An inhibitor of glutamate decarboxylase. It decreases the GAMMA-AMINOBUTYRIC ACID concentration in the brain, thereby causing convulsions.. 3-mercaptopropanoic acid : A mercaptopropanoic acid that is propanoic acid carrying a sulfanyl group at position 3.	2.05	1	0	mercaptopropanoic acid	algal metabolite
quinoxalines quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.	6.96	10	3	mancude organic heterobicyclic parent; naphthyridine; ortho-fused heteroarene
bicuculline Bicuculline: An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.. bicuculline : A benzylisoquinoline alkaloid that is 6-methyl-5,6,7,8-tetrahydro[1,3]dioxolo[4,5-g]isoquinoline which is substituted at the 5-pro-S position by a (6R)-8-oxo-6,8-dihydrofuro[3,4-e][1,3]benzodioxol-6-yl group. A light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from Dicentra cucullaria, Adlumia fungosa, Fumariaceae, and several Corydalis species.	2.05	1	0	benzylisoquinoline alkaloid; isoquinoline alkaloid; isoquinolines	agrochemical; central nervous system stimulant; GABA-gated chloride channel antagonist; GABAA receptor antagonist; neurotoxin
2,3-dihydroxyquinoxaline 2,3-dihydroxyquinoxaline: fluorescent oxalic acid deriv.	2.05	1	0
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.	2.47	2	0	glutamic acid; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid	Escherichia coli metabolite; ferroptosis inducer; micronutrient; mouse metabolite; neurotransmitter; nutraceutical
nicotine (S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum.	2.44	2	0	3-(1-methylpyrrolidin-2-yl)pyridine	anxiolytic drug; biomarker; immunomodulator; mitogen; neurotoxin; nicotinic acetylcholine receptor agonist; peripheral nervous system drug; phytogenic insecticide; plant metabolite; psychotropic drug; teratogenic agent; xenobiotic
gyki 53655 GYKI 53655: an AMPA (alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate) receptor antagonist	2.31	1	0
ly 293558 tezampanel: structure given in first source; an AMPA receptor antagonist	2.43	2	0
ym 872 YM 872: structure in first source	2.05	1	0
ly 300164 talampanel: AMPA receptor antagonist	2.05	1	0	benzodioxoles
organophosphonates hydrogenphosphite : A divalent inorganic anion resulting from the removal of a proton from two of the hydroxy groups of phosphorous acid.	6.96	10	3	divalent inorganic anion; phosphite ion
strychnine Strychnine: An alkaloid found in the seeds of STRYCHNOS NUX-VOMICA. It is a competitive antagonist at glycine receptors and thus a convulsant. It has been used as an analeptic, in the treatment of nonketotic hyperglycinemia and sleep apnea, and as a rat poison.. strychnine : A monoterpenoid indole alkaloid that is strychnidine bearing a keto substituent at the 10-position.	2.05	1	0	monoterpenoid indole alkaloid; organic heteroheptacyclic compound	avicide; cholinergic antagonist; glycine receptor antagonist; neurotransmitter agent; rodenticide
irampanel irampanel: structure in first source	2.05	1	0
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	2.7	3	0	naphthalenes; sulfonic acid derivative
fg 9041 FG 9041: structure given in first source	2.05	1	0	quinoxaline derivative
6-nitro-1,4-dihydroquinoxaline-2,3-dione 6-nitro-1,4-dihydroquinoxaline-2,3-dione: a fluorescent chemosensor; structure in first source	2.05	1	0
myelin basic protein Myelin Basic Protein: An abundant cytosolic protein that plays a critical role in the structure of multilamellar myelin. Myelin basic protein binds to the cytosolic sides of myelin cell membranes and causes a tight adhesion between opposing cell membranes.	2	1	0
cysteine Cysteine: A thiol-containing non-essential amino acid that is oxidized to form CYSTINE.. L-cysteinium : The L-enantiomer of cysteinium.. cysteine : A sulfur-containing amino acid that is propanoic acid with an amino group at position 2 and a sulfanyl group at position 3.	2.1	1	0	cysteinium	fundamental metabolite
lofepramine hydrochloride [no description available]	2.71	3	0
cgp 39551 CGP 39551: N-methyl-D-aspartate receptor antagonist; structure given in first source	2.02	1	0
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.	2.04	1	0	maleate salt; tetracyclic antidepressant	anaesthetic; anticonvulsant; neuroprotective agent; nicotinic antagonist; NMDA receptor antagonist
perampanel perampanel : A member of the class of bipyridines that is 2,3'-bipyridin-6'-one substituted at positions 1' and 5' by phenyl and 2-cyanophenyl groups respectively. Used as an adjunctive therapy for the treatment of partial-onset seizures in patients with epilepsy.	2.05	1	0	bipyridines; nitrile; pyridone	AMPA receptor antagonist; anticonvulsant
pyrimidinones Pyrimidinones: Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O.	2.1	1	0

Condition	Relationship Strength	Studies	Trials
Absence Seizure [description not available]	1.99	1	0
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.	1.99	1	0
Congenital Zika Syndrome [description not available]	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.46	2	0
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.	2.25	1	0
Apoplexy [description not available]	4.37	2	2
Cerebral Ischemia [description not available]	4.37	2	2
Acute Disease Disease having a short and relatively severe course.	4.37	2	2
Brain Ischemia Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION.	4.37	2	2
Stroke A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)	9.37	2	2
Brain Vascular Disorders [description not available]	1.99	1	0
Craniocerebral Injuries [description not available]	1.99	1	0
Cerebrovascular Disorders A spectrum of pathological conditions of impaired blood flow in the brain. They can involve vessels (ARTERIES or VEINS) in the CEREBRUM, the CEREBELLUM, and the BRAIN STEM. Major categories include INTRACRANIAL ARTERIOVENOUS MALFORMATIONS; BRAIN ISCHEMIA; CEREBRAL HEMORRHAGE; and others.	1.99	1	0
Craniocerebral Trauma Traumatic injuries involving the cranium and intracranial structures (i.e., BRAIN; CRANIAL NERVES; MENINGES; and other structures). Injuries may be classified by whether or not the skull is penetrated (i.e., penetrating vs. nonpenetrating) or whether there is an associated hemorrhage.	1.99	1	0
Recrudescence [description not available]	2	1	0
Allergic Encephalomyelitis [description not available]	2	1	0
MS (Multiple Sclerosis) [description not available]	2	1	0
Multiple Sclerosis An autoimmune disorder mainly affecting young adults and characterized by destruction of myelin in the central nervous system. Pathologic findings include multiple sharply demarcated areas of demyelination throughout the white matter of the central nervous system. Clinical manifestations include visual loss, extra-ocular movement disorders, paresthesias, loss of sensation, weakness, dysarthria, spasticity, ataxia, and bladder dysfunction. The usual pattern is one of recurrent attacks followed by partial recovery (see MULTIPLE SCLEROSIS, RELAPSING-REMITTING), but acute fulminating and chronic progressive forms (see MULTIPLE SCLEROSIS, CHRONIC PROGRESSIVE) also occur. (Adams et al., Principles of Neurology, 6th ed, p903)	2	1	0

zk 200775

Description

Cross-References

Synonyms (41)

Research Excerpts

Overview

Toxicity

Bioavailability

Protein Targets (14)

Potency Measurements

Inhibition Measurements

Other Measurements

Ceullar Components (2)

Bioassays (46)

Research

Studies (23)

Market Indicators

Research Demand Index: 11.55

Study Types

zk 200775

Description

Cross-References

Synonyms (41)

Research Excerpts

Overview

Toxicity

Bioavailability

Protein Targets (14)

Potency Measurements

Inhibition Measurements

Other Measurements

Ceullar Components (2)

Bioassays (46)

Research

Studies (23)

Market Indicators

Research Demand Index: 11.55

Study Types

Related Drugs (29)

Related Conditions (18)