Page last updated: 2024-12-05

edaravone

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Edaravone is a free radical scavenger that has been approved for the treatment of amyotrophic lateral sclerosis (ALS) and acute ischemic stroke. It is synthesized through a multi-step process involving the reaction of 3-hydroxy-2-methyl-4H-pyran-4-one with 2-chloro-N-(2-hydroxyethyl)acetamide. Edaravone acts by scavenging reactive oxygen species (ROS), which are known to damage cells and contribute to the progression of neurodegenerative diseases. Its mechanism of action involves the reduction of oxidative stress and the protection of neuronal cells from damage. Edaravone has been shown to slow the progression of ALS in clinical trials and has also been investigated for its potential benefits in other neurodegenerative conditions, such as Alzheimer's disease and Parkinson's disease. The study of edaravone is important due to the lack of effective treatments for neurodegenerative diseases, and its potential to provide a therapeutic option for patients with these conditions. Further research is ongoing to explore its efficacy and safety in different patient populations and to investigate its potential in combination therapies.'

Cross-References

ID SourceID
PubMed CID4021
CHEMBL ID290916
CHEBI ID31530
SCHEMBL ID4704
MeSH IDM0046983

Synonyms (219)

Synonym
AC-4745
MLS001146878
HMS3266F04
BRD-K35458079-001-04-2
nsc-2629
nsc2629
3h-pyrazol-3-one, 2,4-dihydro-5-methyl-2-phenyl-
smr000059020
nsc-26139
nsc26139
DIVK1C_002026
DIVK1C_001018
KBIO1_001018
mci-186
radicut
AE-641/00371017 ,
5-methyl-2-phenyl-2,4-dihydro-3h-pyrazol-3-one
SPECTRUM_000267
CDS1_000986 ,
(mci-186)
tocris-0786
NCGC00022665-02
BIO2_000448
BIO1_001416
BIO1_000927
BIO1_000438
BIO2_000928
SPECTRUM5_001217
BCBCMAP01_000127
BSPBIO_001235
edaravone ,
BSPBIO_002601
IDI1_002203
IDI1_001018
NCGC00022665-04
inchi=1/c10h10n2o/c1-8-7-10(13)12(11-8)9-5-3-2-4-6-9/h2-6h,7h2,1h
brn 0609575
1-phenyl-3-methylpyrazolone-5
ci developer 1
1-fenyl-3-methyl-2-pyrazolin-5-on [czech]
hsdb 4102
norantipyrine
ai3-03557
einecs 201-891-0
ccris 512
norphenazone
methylphenylpyrazolone
developer z
3-methyl-1-phenyl-2-pyrazolin-5-one
3h-pyrazol-3-one,4-dihydro-5-methyl-2-phenyl-
2-pyrazolin-5-one, 3-methyl-1-phenyl-
1-phenyl-3-methyl-5-pyrazolone
nci-c03952
89-25-8
5-pyrazolone, 3-methyl-1-phenyl-
c.i. developer 1
1-phenyl-3-methylpyrazolone
wln: t5nmv dhj br& e1
3-methyl-1-phenyl-2-pyrazoline-5-one, 99%
radicut (tn)
edaravone (usan/jp17/inn)
D01552
radicava (tn)
NCGC00022665-05
NCGC00164015-01
NCGC00022665-06
MLS000069602 ,
KBIO2_003315
KBIOSS_000747
KBIO3_001029
KBIO2_003143
KBIOGR_001502
KBIO3_001030
KBIO2_000747
KBIO3_001821
KBIO2_005711
MAYBRIDGE1_005738
KBIOGR_000575
KBIO2_000575
KBIOSS_000575
KBIO2_005883
SPBIO_001508
NINDS_001018
SPECTRUM4_001091
SPECTRUM3_000971
SPECTRUM2_001574
SPECTRUM1503635
NCGC00018218-01
radicava
2,4-dihydro-5-methyl-2-phenyl-3h-pyrazol-3-one
1-phenyl-3-methyl-5-oxo-2-pyrazoline
3-methyl-1-phenylpyrazol-5-one
phenylmethylpyrazolone
phenyl methyl pyrazolone
CHEBI:31530 ,
STK201315
HMS1990M17
CHEMBL290916
colorex pmp
jarocol pmp
AKOS000313817
HMS557M18
MLS002415675
HMS503K17
HMS1362M17
HMS1792M17
M0687 ,
monopyrazolone
5-methyl-2-phenyl-4h-pyrazol-3-one
A843105
5-methyl-2-phenyl-1,2-dihydropyrazol-3-one;3-methyl-1-phenyl-2-pyrazolin-5-one
NCGC00018218-08
NCGC00018218-05
NCGC00018218-04
NCGC00018218-02
NCGC00018218-03
NCGC00018218-07
NCGC00018218-06
edaravone [usan:inn]
s798v6yjrp ,
unii-s798v6yjrp
1-fenyl-3-methyl-2-pyrazolin-5-on
ec 201-891-0
dtxcid201130
NCGC00256515-01
cas-89-25-8
dtxsid9021130 ,
tox21_302819
tox21_112077
NCGC00259296-01
tox21_201747
BCP9000635
nsc-758622
pharmakon1600-01503635
nsc758622
HMS2234M19
CCG-39352
3-methyl-1-phenyl-2-pyrazoline-5-one
BCPP000246
FT-0608243
AM20060748
S1326
CS-1832
HY-B0099
5-methyl-2-phenyl-2,4-dihydro-3-pyrazolone
1-phenyl-3-methyl-2-pyrazolin-5-one
3-methyl-1-phenyl-1h-pyrazol-5(4h)-one
5-methyl-2-phenyl-2,4-dihydro-pyrazol-3-one
2,4-dihydro-2-phenyl-5-methyl-3h-pyrazol-3-one
SCHEMBL4704
tox21_112077_1
NCGC00018218-10
3-methyl-1-phenyl-4,5-dihydro-1h-pyrazol-5-one
4E-901
norphenazone [mi]
phenazone impurity a [ep impurity]
edaravone [who-dd]
edaravone [hsdb]
phenyl methyl pyrazolone [inci]
edaravone [mart.]
edaravone [usan]
edaravone [inn]
edaravone [orange book]
edaravone [jan]
Z50145861
5-methyl-2-phenyl-2,4-dihydro-3h-pyrazol-3-one #
2 4-dihydro-5-methyl-2-phenyl-3h-pyrazol-3-one
MLS006011753
Q-200386
3-methyl-1-phenyl-2-pyrazolin-5-one (mci-186)
HMS3403M17
AB00375776_15
OPERA_ID_1057
AB00375776_14
mfcd00003138
F0391-0021
3-methyl-1-phenyl-2-pyrazoline-5-one, purum, >=98.0% (nt)
sr-01000000135
SR-01000000135-2
3-methyl-1-phenyl-2-pyrazoline-5-one, saj special grade
HMS3654L15
phenazone impurity a, european pharmacopoeia (ep) reference standard
5-methyl-2-phenyl-2,4-dihydro-3h-pyrazol-3-one (edaravone)
SR-01000000135-3
SR-01000000135-5
SBI-0051836.P002
NCGC00018218-17
bdbm50200541
SW148216-2
DB12243
3-methyl-1-phenyl-2-pyrazolin-5one
Q335099
edaravone (mci-186)
HMS3675L05
BCP26336
HMS3411L05
BRD-K35458079-001-23-2
BRD-K35458079-001-12-5
SB19128
HMS3884A11
3 methyl 1 phenyl 2 pyrazolin 5 one
1 phenyl 3 methyl 5 pyrazolone
mci186
D86209
(edaravone)
3-?methyl-?1-?phenyl-?2-?pyrazolin-?5-?one
mci-186; edaravone
EN300-16234
gtpl11994
edaravone (mart.)
edaravona
1-phenyl-3-methyl-delta3-pyrazol-5-one
phenazone impurity a (ep impurity)
edaravonum
n-desmethylantipyrine
3-methyl-1-phenyl-2h-pyrazolin-5-one
radicava ors
3-pyrazolin-5-one, 3-methyl-1-phenyl-
n07xx14

Research Excerpts

Overview

Edaravone is a free radical scavenger that is approved for motor neuron disease and acute ischemic stroke. It has been shown to inhibit motor neuron death in animal models by reducing oxidative stress & it has shown efficacy in a small subset of people with ALS.

ExcerptReferenceRelevance
"Edaravone (EDR) is a free radical scavenger that is approved for motor neuron disease and acute ischemic stroke."( Preclinical validation of a novel oral Edaravone formulation for treatment of frontotemporal dementia.
Bobrovskaya, L; Kelliny, S; Xiong, J; Zhou, XF, 2021
)
1.61
"Edaravone, is a free-radical scavenger, it has been shown to inhibit motor neuron death in animal models by reducing oxidative stress & it has shown efficacy in a small subset of people with ALS."( Efficacy and Safety of Edaravone in Amyotrophic Lateral Sclerosis Patients in Indian Population.
Gupta, S; Singal, A; Soni, R; Tomar, S, 2022
)
1.75
"Edaravone dexborneol is a novel neuroprotective agent consisting of edaravone and borneol."( Edaravone dexborneol protects cerebral ischemia reperfusion injury through activating Nrf2/HO-1 signaling pathway in mice.
Dong, Y; Gao, Y; Hu, M; Lv, P; Xu, J; Xu, L; Zhang, J, 2022
)
2.89
"Edaravone is a promising treatment for ischemic stroke patients, with a more favorable time window. "( Edaravone for acute ischemic stroke - Systematic review with meta-analysis.
Afreixo, V; Fidalgo, M; Gregório, H; Gregório, T; Magalhães, P; Ricardo Pires, J; Viseu, I, 2022
)
3.61
"Edaravone (ED) is a neuroprotective drug with beneficial effects against several disorders due to its prominent antioxidant activity. "( Edaravone alleviates methotrexate-induced testicular injury in rats: Implications on inflammation, steroidogenesis, and Akt/p53 signaling.
Arafa, EA; Hassanein, EHM; Hussein, RM; Mohamed, WR, 2023
)
3.8
"Edaravone is a mitochondrially targeted drug with a suggested capability to modify the course of diverse neurological diseases. "( Experimental Treatment with Edaravone in a Mouse Model of Spinocerebellar Ataxia 1.
Benediktova, S; Cendelin, J; Jedlicka, J; Jelinkova, D; Kapl, S; Kuncova, J; Purkartova, Z; Sucha, M; Tichanek, F; Tuma, J, 2023
)
2.65
"Edaravone is an anti-stroke medication that may have nitric oxide (NO) modulating properties. "( Acute and Sub-chronic Anticonvulsant Effects of Edaravone on Seizure Induced by Pentylenetetrazole or Electroshock in Mice, Nitric Oxide Involvement.
Dastgheib, M; Moezi, L; Oftadehgan, S; Pirsalami, F; Purkhosrow, A; Sattarinezhad, E, 2023
)
2.61
"Edaravone is a potent free radical scavenger having antioxidant effect."( The protective effect of edaravone on memory impairment induced by chronic sleep deprivation.
Al Mosabih, HS; Alzoubi, KH; Mahasneh, AF, 2019
)
1.54
"The edaravone is a new antioxidant and hydroxyl radical scavenger, which is the novel scavenger for clinical use, mainly for nervous system diseases."( Clinical observation in edaravone treatment for acute cerebral infarction.
Gao, G; Sun, C; Sun, Z; Xu, Q; Zhao, M, 2019
)
1.3
"Edaravone is a potent free radical scavenger that has a promising role in combating many acute lung injuries. "( Edaravone attenuates lung injury in a hind limb ischemia-reperfusion rat model: A histological, immunohistochemical and biochemical study.
Aboregela, AM; Kassab, AA; Shalaby, AM, 2020
)
3.44
"Edaravone Dexborneol is a novel neuroprotective agent that comprised edaravone and (+)-borneol, a food additive with an anti-inflammatory effect in animal ischaemic stroke models. "( Safety and efficacy of Edaravone Dexborneol versus edaravone for patients with acute ischaemic stroke: a phase II, multicentre, randomised, double-blind, multiple-dose, active-controlled clinical trial.
Chen, H; Gao, X; Gao, Z; Wang, A; Wang, Y; Xu, J; Zhao, X; Zhou, J, 2019
)
2.27
"Edaravone is a potent free radical scavenger that has a neuroprotective effect against memory impairment in several experimental models."( Edaravone protects from memory impairment induced by chronic L-methionine administration.
Aburashed, ZO; Alzoubi, KH; Mayyas, F, 2020
)
2.72
"Edaravone is a free-radical scavenger with relatively favorable properties of brain penetration. "( Predicting the Pharmacokinetic Characteristics of Edaravone Intravenous Injection and Sublingual Tablet Through Modeling and Simulation.
Chen, X; Liang, W; Sun, Z; Wang, J; Wang, Y; Zhao, X, 2020
)
2.25
"Edaravone is a synthetic antioxidant that specifically targets oxidative damage interacting with lipid radicals in the cell."( Edaravone May Prevent Ferroptosis in ALS.
Blagojević, D; Miletić, S; Nikolić-Kokić, A; Oreščanin-Dušić, Z; Spasić, MB; Spasić, S; Stević, Z, 2020
)
2.72
"Edaravone (EDA) is an effective free radical scavenger that has been used clinically for the treatment of postischemic neuronal injury."( Edaravone alleviates cell apoptosis and mitochondrial injury in ischemia-reperfusion-induced kidney injury via the JAK/STAT pathway.
Bai, L; Bai, X; Guo, Z; Luo, D; Ren, X; Wang, D; Wang, Q; Yang, J; Zhang, E; Zhao, X, 2020
)
2.72
"Edaravone is a free radical scavenger that has been recently approved for treatment of Amyotrophic lateral sclerosis (ALS) to delay functional decline. "( Evaluation of clinical outcome and safety profile of edaravone in treatment of amyotrophic lateral sclerosis: a 72-week single-center experience.
Al-Hashel, JY; Ismail, II; Kamel, WA; Massoud, F, 2021
)
2.31
"Edaravone is a potent free-radical scavenger that has been in the market for more than 30 years. "( Drug Repurposing: Promises of Edaravone Target Drug in Traumatic Brain Injury.
Ashekyan, O; Habashy, KJ; Hamade, E; Ismail, H; Issa, H; Jourdi, H; Kobeissy, F; Mondello, S; Nasrallah, L; Sabra, M; Shakkour, Z; Zibara, K, 2021
)
2.35
"Edaravone is a potent antioxidant and anti-inflammatory agent that is used in the clinic. "( Anticonvulsive effects of edaravone on penicillin-induced focal onset seizure model in the conscious rats.
Aygun, H; Kurt, S, 2021
)
2.36
"Edaravone is a powerful free radical scavenger used for the treatment of ischemia/reperfusion diseases due to its anti-oxidative stress and anti-inflammatory properties."( Effect of edaravone on pregnant mice and their developing fetuses subjected to placental ischemia.
Abe, K; Atallah, M; Yamashita, T, 2021
)
1.75
"Edaravone is a new antioxidant and hydroxyl radical scavenger. "( Clinical effects and safety of edaravone in treatment of acute ischaemic stroke: A meta-analysis of randomized controlled trials.
Chen, C; Chen, S; Chen, Y; Hong, L; Li, M; Lin, L, 2021
)
2.35
"Edaravone is an antioxidant and oxygen radical scavenger that can inhibit lipid peroxidation during the scavenging of oxygen free radicals."( Safety and efficacy of edaravone for patients with acute stroke: A protocol for randomized clinical trial.
Cheng, X; Dou, Z; Jiao, G; Shan, H, 2021
)
1.65
"Edaravone (EDR) is a well-recognized lipophilic free radical scavenger for diseases including neurodegenerative disease, cardiovascular disease, and cancer. "( Lipid-based nanosystem of edaravone: development, optimization, characterization and in vitro/in vivo evaluation.
Garg, S; Kathawala, K; Parikh, A; Tan, CC; Zhou, XF, 2017
)
2.2
"Edaravone is a strong free radical scavenger most used for treating acute ischemic stroke. "( Edaravone ameliorates compression-induced damage in rat nucleus pulposus cells.
Hu, HZ; Hu, YQ; Lin, H; Liu, JX; Ma, X; Pu, FF; Shao, ZW; Wang, BC; Zhao, L, 2017
)
3.34
"Edaravone is a new type of oxygen free radical scavenger and able to attenuate various brain damage including hypoxic-ischemic brain damage (HIBD). "( Edaravone attenuates neuronal apoptosis in hypoxic-ischemic brain damage rat model via suppression of TRAIL signaling pathway.
Fu, R; Huang, Y; Lei, J; Li, C; Li, H; Luo, S; Mo, Z; Zhang, L, 2018
)
3.37
"Edaravone is an antioxidant free-radical scavenger approved by the FDA in 2017 for the treatment of ALS."( Edaravone in the treatment of amyotrophic lateral sclerosis: efficacy and access to therapy - a roundtable discussion.
Agnese, W; Brooks, BR; Jorgenson, JA; Newhouse, BJ; Shefner, JM, 2018
)
2.64
"Edaravone is a strong antioxidant that prevents oxidative stress from inducing motor neuron death in ALS patients."( Edaravone: a new hope for deadly amyotrophic lateral sclerosis.
Bhandari, R; Kuhad, A, 2018
)
2.64
"Edaravone is an oxygen free radical scavenger that is widely used to treat ischemic injury to the nervous system. "( Edaravone inhibits autophagy after neuronal oxygen-glucose deprivation/recovery injury.
Chen, J; Ding, Q; Fan, J; Gu, J; Tang, P; Wang, Q; Yin, G; Yin, J; Zhou, Z, 2019
)
3.4
"Edaravone is a well-known commercial drug used in the treatment of strokes and amyotrophic lateral sclerosis (ALS)."( Edaravone acts as a potential therapeutic drug against pentylenetetrazole-induced epilepsy in male albino rats by downregulating cyclooxygenase-II.
Liu, LM; Lu, Y; Wang, N; Wang, WP, 2019
)
2.68
"Edaravone is a free radical scavenger, with a neuroprotective effect against cognitive impairment in several animal models."( Edaravone prevents memory impairment in an animal model of post-traumatic distress.
Al-Qudah, MA; Alfaqih, MA; Alzoubi, KH; Shatnawi, A, 2019
)
2.68
"Edaravone is a powerful free radical scavenger used in clinical treatment for cerebral ischemic stroke."( Edaravone prevents neurotoxicity of mutant L166P DJ-1 in Parkinson's disease.
Li, B; Xu, Z; Yu, D, 2013
)
2.55
"Edaravone is a free radical scavenger that protects the adjacent cortex during cerebral infarction. "( Effects of edaravone, a free radical scavenger, on photochemically induced cerebral infarction in a rat hemiplegic model.
Harada, K; Ikeda, S; Kamikawa, Y; Ohwatashi, A, 2013
)
2.22
"Edaravone is a promising treatment for stroke."( Edaravone improves functional and structural outcomes in animal models of focal cerebral ischemia: a systematic review.
Egan, K; Macleod, M; Mead, G; Sena, E; Wu, S, 2014
)
2.57
"Edaravone is a free radical scavenger, and borneol has shown anti-inflammatory effect."( The synergetic effect of edaravone and borneol in the rat model of ischemic stroke.
Gao, LY; Hua, Y; Liao, GY; Luo, CX; Sun, WX; Tang, Y; Wu, HY; Yang, SB; Zhang, ZP; Zhou, QG; Zhu, DY, 2014
)
1.43
"Edaravone is a potent free radical scavenger that exerts antioxidant effects."( Edaravone injection ameliorates cognitive deficits in rat model of Alzheimer's disease.
Li, F; Li, J; Liu, X; Wang, Q; Yang, R, 2015
)
2.58
"Edaravone is a free radical scavenger with brain protection properties and is recommended by "The Japanese Guidelines for the Management of Stroke 2009" for administration to adult patients, in whom it has been shown to improve neurological deficits after cerebral infarction. "( Efficacy, safety, and outcomes in 17 pediatric cases treated with the free radical scavenger edaravone.
Aihara, Y; Kawamata, T; Nakamoto, H; Okada, Y; Yamaguchi, K, 2015
)
2.08
"Edaravone is a neuroprotective agent with a potent free radical scavenging and antioxidant actions. "( Protective role of edaravone against cisplatin-induced ototoxicity in an auditory cell line.
Chang, J; Choi, J; Im, GJ; Jung, HH; Kim, HJ; Kim, JH; Lee, HM; Lee, S; Park, SK; Ryu, SH, 2015
)
2.19
"Edaravone (EDA) is a potent free radical scavenger that has been clinically shown to reduce the neuronal injury after cerebral ischemia."( Protective effect of edaravone against manganese-induced toxicity in cultured rat astrocytes.
Apaydin, M; Erbas, O; Evren, V; Khalilnezhad, A; Taskiran, D, 2015
)
1.46
"Edaravone is a newly developed clinical medicine for the treatment of acute cerebral infarction. "( Protective effect of Edaravone against hypoxia-induced cytotoxicity in osteoblasts MC3T3-E1 cells.
Cao, B; Chai, C; Zhao, S, 2015
)
2.18
"Edaravone is a potent free radical scavenger, which has been clinically used to treat the neuronal damage following acute ischemic stroke."( Edaravone suppresses degradation of type II collagen.
Han, J; Huang, C; Liao, G; Zhang, G; Zou, B, 2016
)
2.6
"Edaravone is a novel free radical scavenger that exerts neuroprotective effects by inhibiting endothelial injury and by ameliorating neuronal damage in brain ischemia. "( Edaravone injection reverses learning and memory deficits in a rat model of vascular dementia.
Ge, X; Li, W; Li, X; Liang, X; Lu, F; Qin, L; Yao, Y; Yu, Q; Zhang, J; Zhao, D, 2017
)
3.34
"Edaravone (Eda) is a potent scavenger of hydroxyl radicals and has been demonstrated to be beneficial for patients with acute ischemic stroke. "( Edaravone protects against MPP+ -induced cytotoxicity in rat primary cultured astrocytes via inhibition of mitochondrial apoptotic pathway.
Chen, H; Ding, JH; Hu, G; Wang, S, 2008
)
3.23
"Edaravone (MCI-186) is a newly developed antioxidative radical scavenger for the treatment of acute cerebral infarction, exerting neuroprotective effects against ischemic insult. "( Neuroprotective effects of edaravone, a free radical scavenger, on the rat hippocampus after pilocarpine-induced status epilepticus.
Abe, T; Anan, M; Fujiki, M; Kamida, T; Kobayashi, H; Ooba, H, 2009
)
2.09
"Edaravone is a free-radical scavenger, an agent being widely used for cerebral ischemia in Japan. "( Treatment with edaravone, initiated at symptom onset, slows motor decline and decreases SOD1 deposition in ALS mice.
Ito, H; Kaneko, S; Kusaka, H; Nakano, S; Ohnishi, S; Wate, R; Zhang, J, 2008
)
2.14
"Edaravone is a lipophilic drug with multiple mechanisms of action. "( The lipophilic multifunctional antioxidant edaravone (radicut) improves behavior following embolic strokes in rabbits: a combination therapy study with tissue plasminogen activator.
Lapchak, PA; Zivin, JA, 2009
)
2.06
"Edaravone is a novel free radical scavenger that is clinically employed in patients with acute cerebral infarction, but has not previously been used to treat traumatic brain injury (TBI). "( The novel free radical scavenger, edaravone, increases neural stem cell number around the area of damage following rat traumatic brain injury.
Hashimoto, S; Ito, H; Itoh, T; Nishida, S; Satou, T; Tsubaki, M, 2009
)
2.07
"Edaravone is a novel free radical scavenger used clinically in patients with acute cerebral infarction; however, it has not been assessed in traumatic brain injury (TBI). "( Edaravone protects against apoptotic neuronal cell death and improves cerebral function after traumatic brain injury in rats.
Hashimoto, S; Imano, M; Ito, H; Itoh, T; Nishida, S; Satou, T; Tsubaki, M, 2010
)
3.25
"Edaravone is a newly developed radical scavenging agent that has been widely used for protection against ischemia/reperfusion (I/R) injury in patients with cerebral infarction. "( Effect of edaravone on ischemia/reperfusion injury in rat urinary bladder--changes in smooth muscle cell phenotype and contractile function.
Hanai, T; Matsumoto, S; Shimizu, N; Sugimoto, K; Uemura, H, 2010
)
2.21
"Edaravone is a free-radical scavenger that has been widely used for acute ischaemic stroke in Japan. "( Does functional outcome in acute ischaemic stroke patients correlate with the amount of free-radical scavenger treatment? A retrospective study of edaravone therapy.
Katayama, M; Shimizu, H; Unno, Y, 2010
)
2
"Edaravone (Radicut) is a free radical scavenger marketed in Japan by Mitsubishi Tanabe Pharma Corp. "( A critical assessment of edaravone acute ischemic stroke efficacy trials: is edaravone an effective neuroprotective therapy?
Lapchak, PA, 2010
)
2.11
"Edaravone (MCI-186) is a potent free radical scavenger used clinically to treat acute brain infarction. "( Edaravone, a novel antidote against lung injury and pulmonary fibrosis induced by paraquat?
Qian, X; Sun, H; Yang, L; Zhi, Q, 2011
)
3.25
"Edaravone is a brain-penetrant free radical scavenger that is known to ameliorate postischemic neuronal dysfunction. "( Edaravone and carnosic acid synergistically enhance the expression of nerve growth factor in human astrocytes under hypoxia/reoxygenation.
Hayakari, R; Imaizumi, T; Ishikawa, A; Itoh, K; Kosaka, K; Matsumiya, T; Metoki, N; Mimura, J; Ota, K; Satoh, K; Tanji, K; Yoshida, H, 2011
)
3.25
"Edaravone is a novel free radical scavenger that is clinically employed in patients with acute cerebral infarction. "( Treatment with edaravone attenuates ischemic brain injury and inhibits neurogenesis in the subventricular zone of adult rats after focal cerebral ischemia and reperfusion injury.
Chen, X; Gao, M; Lei, S; Li, L; Li, W; Li, X; Liu, Y; Lu, H; Wang, N; Zhang, P; Zheng, J, 2012
)
2.17
"Edaravone is a neuroprotective agent that has been widely used in China, and several studies have suggested that it may be beneficial in acute ischaemic stroke."( Edaravone for acute ischaemic stroke.
Feng, S; Li, J; Li, W; Liu, M; Wu, B; Yang, Q; Yuan, W; Zhang, S, 2011
)
2.53
"Edaravone is a scavenger of hydroxyl radicals."( Protective effects of edaravone on experimental spinal cord injury in rats.
Altaş, M; Aras, M; Oran, I; Ozgiray, E; Oztürk, OH; Serarslan, Y; Söğüt, S; Yurtseven, T; Zileli, M, 2011
)
1.41
"Edaravone is a novel free radical scavenger currently used to reduce cerebral damages after acute cerebral infarction."( Effects of edaravone on amyloid-β precursor protein processing in SY5Y-APP695 cells.
Liu, C; Shen, YE; Wang, Y; Yu, GC; Zhang, LM; Zhang, ZY, 2013
)
1.5
"Edaravone is a synthetic radical scavenger that has been used in acute stroke."( A radical scavenger, edaravone, protects canine kidneys from ischemia-reperfusion injury after 72 hours of cold preservation and autotransplantation.
Fujita, M; Furukawa, H; Jin, MB; Nakayama, M; Shimamura, T; Suzuki, T; Tahara, M; Taniguchi, M; Todo, S, 2005
)
1.37
"Edaravone is a newly developed radical scavenging agent that has been used for protection against I/R injury in patients with cerebral infarction."( Edaravone protects against ischemia/reperfusion-induced functional and biochemical changes in rat urinary bladder.
Hanai, T; Levin, RM; Matsumoto, S; Shimizu, N; Sugiyama, T; Uemura, H; Yoshioka, N, 2005
)
2.49
"Edaravone (MCI-186) is a novel synthetic free radical scavenger intended to have neuroprotective effect against ischemic insult. "( Does edaravone (MCI- 186) act as an antioxidant and a neuroprotector in experimental traumatic brain injury?
Aruga, T; Dohi, K; Hiratsuka, K; Nakamachi, T; Nakamura, S; Ohtaki, H; Satoh, K; Shioda, S; Yofu, S; Yoshikawa, T, 2007
)
2.3
"Edaravone is a potent scavenger of hydroxyl radicals and is quite successful in patients with acute cerebral ischemia, and several organ-protective effects have been reported. "( Edaravone mimics sphingosine-1-phosphate-induced endothelial barrier enhancement in human microvascular endothelial cells.
Goda, N; Kataoka, N; Makino, H; Omori, K; Sarai, K; Shikata, K; Shikata, Y; Wada, J; Watanabe, N, 2007
)
3.23
"Edaravone is a potent scavenger of hydroxyl radicals and attenuates oxidative damage-related neurodegenerative diseases. "( The radical scavenger edaravone counteracts diabetes in multiple low-dose streptozotocin-treated mice.
Ago, Y; Fukudome, D; Kawasaki, T; Matsuda, M; Matsuda, T, 2008
)
2.1

Effects

Edaravone has a remarkable protective effect on acute liver injury caused by oxygen radicals through attenuating the membrane lipid peroxidation, but also inhibiting the production of inflammatory cytokines. Edarvone has an inhibitory effect on lipid perOxidation by scavenging free radicals and prevents vascular endothelial cell injury.

Edaravone has been widely used in the treatment of acute ischemic stroke. It has been approved by the US Food and Drug Association (FDA) but not by the European Medicines Agency (EMA)

ExcerptReferenceRelevance
"Edaravone (ED) has a protective effect on IRI."( Effect of Edaravone on MicroRNA Expression in Exosomes after Hepatic Ischemia-reperfusion Injury.
Fei, Y; Huang, G; Shao, J; Sun, H; Wang, L; Yang, J; Zheng, C; Zou, S, 2022
)
1.85
"Edaravone has a remarkable protective effect on acute liver injury caused by oxygen radicals through not only attenuating the membrane lipid peroxidation, but also inhibiting the production of inflammatory cytokines. "( A free radical scavenger, edaravone, attenuates steatosis and cell death via reducing inflammatory cytokine production in rat acute liver injury.
Ishii, H; Kameyama, K; Kitamura, K; Kurita, S; Nakamoto, N; Saito, H; Saito, Y; Tada, S, 2003
)
2.06
"Edaravone has an inhibitory effect on lipid peroxidation by scavenging free radicals and prevents vascular endothelial cell injury. "( Neuroprotection of edaravone on hypoxic-ischemic brain injury in neonatal rats.
Ishida, A; Nakajima, W; Takada, G; Yasuoka, N, 2004
)
2.09
"Edaravone has an anti-inflammatory effect in experimental models of various organ injuries. "( Edaravone prevents iNOS expression by inhibiting its promoter transactivation and mRNA stability in cytokine-stimulated hepatocytes.
Habara, K; Ito, S; Kaibori, M; Kamiyama, Y; Kwon, AH; Nishizawa, M; Okumura, T; Tsuji, K; Yamada, M; Yoshida, H, 2008
)
3.23
"Edaravone (ED) has a protective effect on IRI."( Effect of Edaravone on MicroRNA Expression in Exosomes after Hepatic Ischemia-reperfusion Injury.
Fei, Y; Huang, G; Shao, J; Sun, H; Wang, L; Yang, J; Zheng, C; Zou, S, 2022
)
1.85
"Edaravone has been widely used in the treatment of acute ischemic stroke. "( Neuroprotection of Oral Edaravone on Middle Cerebral Artery Occlusion in Rats.
Luo, HY; Parikh, A; Xiong, YX; Ye, QY; Zhao, LQ; Zhou, XF, 2022
)
2.47
"Edaravone has been demonstrated in previous studies to reduce neurologic deficits in stroke patients."( Edaravone for acute ischemic stroke - Systematic review with meta-analysis.
Afreixo, V; Fidalgo, M; Gregório, H; Gregório, T; Magalhães, P; Ricardo Pires, J; Viseu, I, 2022
)
2.89
"Edaravone has been approved by the US Food and Drug Association (FDA) but not by the European Medicines Agency (EMA), and further studies testing oral formulations are currently conducted."( Clinical studies in amyotrophic lateral sclerosis.
Dorst, J; Genge, A, 2022
)
1.44
"Edaravone has been shown to slow the rate of motor function deterioration experienced by patients with ALS. "( Oral Edaravone - Introducing a Flexible Treatment Option for Amyotrophic Lateral Sclerosis.
Aoki, M; Couratier, P; Genge, A; Jackson, CE; Lunetta, C; Nelson, S; Pattee, GL; Salah, A; Sobue, G; Wymer, J; Yoshino, H,
)
2.09
"Edaravone has showed its neuroprotective effects after ischemia stroke, but its effects and possible mechanisms after ICH are poorly understood."( Edaravone Administration Confers Neuroprotection after Experimental Intracerebral Hemorrhage in Rats via NLRP3 Suppression.
Geng, J; Jiang, Y; Miao, H; Tang, J; Zhang, B; Zhu, G, 2020
)
2.72
"Edaravone has preventive effects on myocardial injury following ischemia and reperfusion in patients with acute myocardial infarction."( The efficacy of edaravone (radicut), a free radical scavenger, for cardiovascular disease.
Kikuchi, K; Morioka, M; Murai, Y; Takeshige, N; Tanaka, E; Tancharoen, S; Yoshitomi, M, 2013
)
1.46
"Edaravone has been used in patients with acute ischemic stroke in Japan for over 10 years but does not have marketing authorization in Europe or America. "( Edaravone improves functional and structural outcomes in animal models of focal cerebral ischemia: a systematic review.
Egan, K; Macleod, M; Mead, G; Sena, E; Wu, S, 2014
)
3.29
"Edaravone has been shown to have a neuroprotective effect."( Edaravone protected PC12 cells against MPP(+)-cytoxicity via inhibiting oxidative stress and up-regulating heme oxygenase-1 expression.
Bai, B; Chen, J; Cheng, B; Guo, Y; Ji, B; Li, C; Pan, Y, 2014
)
2.57
"Edaravone has recently been approved as a new therapeutic option for ALS in Japan."( Novel therapies in development that inhibit motor neuron hyperexcitability in amyotrophic lateral sclerosis.
Kiernan, MC; Noto, Y; Shibuya, K; Vucic, S, 2016
)
1.16
"Edaravone has protective effects on renal ischemia-reperfusion injury in rats."( [Protective effects of edaravone on renal ischemia-reperfusion injury in rats].
Huang, HY; Xu, QP; Zhang, G, 2008
)
2.1
"Edaravone has been shown to reduce oxidative stress, edema, infarct volume, inflammation and apoptosis following ischemic injury of the brain in the adult as well as decrease free radical production in the neonatal brain following hypoxic-ischemic insult."( Antioxidants and neuroprotection in the adult and developing central nervous system.
Kaur, C; Ling, EA, 2008
)
1.07
"Edaravone has been reported to have a radioprotective effect at high concentrations. "( Edaravone, a known free radical scavenger, enhances X-ray-induced apoptosis at low concentrations.
Enomoto, A; Hosoi, Y; Igaki, H; Katsumura, Y; Matsumoto, Y; Miyagawa, K; Morita, A; Nakagawa, K; Sasano, N; Shiraishi, K, 2010
)
3.25
"Edaravone has been recognized as a potential protective agent for cardiovascular diseases. "( A hypothesis: Edaravone exert cardioprotection partly via modulation of adiponectin.
Jia, M; Pei, H; Sun, L; Zheng, X; Zhou, H, 2012
)
2.18
"Edaravone has a remarkable protective effect on acute liver injury caused by oxygen radicals through not only attenuating the membrane lipid peroxidation, but also inhibiting the production of inflammatory cytokines. "( A free radical scavenger, edaravone, attenuates steatosis and cell death via reducing inflammatory cytokine production in rat acute liver injury.
Ishii, H; Kameyama, K; Kitamura, K; Kurita, S; Nakamoto, N; Saito, H; Saito, Y; Tada, S, 2003
)
2.06
"Edaravone has potent free radical quenching and antioxidant actions. "( Free radical scavenger, edaravone, in stroke with internal carotid artery occlusion.
Arihiro, S; Fujii, K; Ibayashi, S; Iida, M; Kamouchi, M; Nakane, H; Okada, Y; Toyoda, K, 2004
)
2.07
"Edaravone has an inhibitory effect on lipid peroxidation by scavenging free radicals and prevents vascular endothelial cell injury. "( Neuroprotection of edaravone on hypoxic-ischemic brain injury in neonatal rats.
Ishida, A; Nakajima, W; Takada, G; Yasuoka, N, 2004
)
2.09
"Edaravone has been used for protection against I/R injury in patients with cerebral infarction."( Edaravone protects against lung injury induced by intestinal ischemia/reperfusion in rat.
Horikawa, S; Ito, K; Ozasa, H, 2005
)
2.49
"Edaravone has been reported to inhibit lipid peroxidation in cerebral ischemia models."( Neuroprotection and enhanced recovery with edaravone after acute spinal cord injury in rats.
Iwashita, Y; Kuno, S; Nakamura, T; Ohta, S; Takada, H, 2005
)
1.31
"Edaravone has an anti-inflammatory effect in experimental models of various organ injuries. "( Edaravone prevents iNOS expression by inhibiting its promoter transactivation and mRNA stability in cytokine-stimulated hepatocytes.
Habara, K; Ito, S; Kaibori, M; Kamiyama, Y; Kwon, AH; Nishizawa, M; Okumura, T; Tsuji, K; Yamada, M; Yoshida, H, 2008
)
3.23
"Edaravone has preventive effects on myocardial injury following ischemia and reperfusion in patients with acute myocardial infarction."( Edaravone (3-methyl-1-phenyl-2-pyrazolin-5-one), a novel free radical scavenger, for treatment of cardiovascular diseases.
Chayama, K; Higashi, Y; Jitsuiki, D; Yoshizumi, M, 2006
)
2.5

Actions

Edaravone (Edv) can inhibit tissue damage, cause cerebral edema, and delay neuronal death caused by acute cerebral infarction. It may inhibit the induction of iNOS gene expression at the steps of its promoter transactivation in a nuclear factor-kappaB-independent manner.

ExcerptReferenceRelevance
"Edaravone (Edv) can inhibit tissue damage, cause cerebral edema, and delay neuronal death caused by acute cerebral infarction. "( Edaravone-Loaded Macrophage-Derived Exosomes Enhance Neuroprotection in the Rat Permanent Middle Cerebral Artery Occlusion Model of Stroke.
Li, F; Liang, J; Shi, Y; Zhao, L, 2020
)
3.44
"Edaravone may inhibit the number of apoptotic neuronal cells and 8-OHdG expression within 48 h after HI insult."( Edaravone inhibits DNA peroxidation and neuronal cell death in neonatal hypoxic-ischemic encephalopathy model rat.
Goto, Y; Itoh, M; Miyazawa, T; Nonoyama, S; Takizawa, Y, 2009
)
2.52
"Edaravone blocked the increase in 3-nitrotyrosine immunoreactivity and the activation of astrocytes, but it did not affect the activation of microglia."( Protective effect of the radical scavenger edaravone against methamphetamine-induced dopaminergic neurotoxicity in mouse striatum.
Ago, Y; Baba, A; Ishihara, K; Itoh, S; Kawasaki, T; Matsuda, T; Nakamura, S, 2006
)
1.32
"Edaravone may inhibit the induction of iNOS gene expression at steps of promoter transactivation and mRNA stabilization in cytokine-stimulated hepatocytes."( Edaravone prevents iNOS expression by inhibiting its promoter transactivation and mRNA stability in cytokine-stimulated hepatocytes.
Habara, K; Ito, S; Kaibori, M; Kamiyama, Y; Kwon, AH; Nishizawa, M; Okumura, T; Tsuji, K; Yamada, M; Yoshida, H, 2008
)
2.51
"Edaravone may inhibit the induction of iNOS gene expression at the steps of its promoter transactivation in a nuclear factor-kappaB-independent manner and mRNA stabilization in RAW264 cells."( Edaravone inhibits the induction of iNOS gene expression at transcriptional and posttranscriptional steps in murine macrophages.
Habara, K; Ito, S; Kaibori, M; Kamiyama, Y; Kwon, AH; Nishizawa, M; Okumura, T; Yamada, M; Yoshida, H, 2008
)
2.51

Treatment

Edaravone treatment was associated with improved chances of 90-day good (OR=1.31, 95% CI 1.06-1.67) and excellent functional outcomes. Treatment could significantly reduce lung permeability, decrease tissue pro-apoptosis protein (cleaved-caspase3) and inflammation (IL-1β)

ExcerptReferenceRelevance
"Edaravone treatment ameliorated EAE severity and attenuated inflammation in the SC of the EAE mice, as verified by histological analysis."( Edaravone attenuates disease severity of experimental auto-immune encephalomyelitis and increases gene expression of Nrf2 and HO-1.
Hrnčíř, T; Hroudová, J; Kübra Öztürk, H; Kučera, T; Kutinová Canová, N; Ľupták, M; Michaličková, D; Šíma, M; Slanař, O, 2022
)
2.89
"With edaravone treatment, subjects in both the FVC24 ≥80%p and the FVC24 <80%p subgroups experienced a reduction in ALS Functional Rating Scale-Revised (ALSFRS-R) score loss vs placebo subjects through week 48. "( Edaravone efficacy in amyotrophic lateral sclerosis with reduced forced vital capacity: Post-hoc analysis of Study 19 (MCI186-19) [clinical trial NCT01492686].
Apple, S; Brooks, BR; Heiman-Patterson, T; Liu, S; Wiedau-Pazos, M; Zhang, J, 2022
)
2.68
"Edaravone treatment was associated with improved chances of 90-day good (OR=1.31, 95% CI 1.06-1.67) and excellent (OR=1.26, 95% CI 1.04-1.54) functional outcomes."( Edaravone for acute ischemic stroke - Systematic review with meta-analysis.
Afreixo, V; Fidalgo, M; Gregório, H; Gregório, T; Magalhães, P; Ricardo Pires, J; Viseu, I, 2022
)
2.89
"Edaravone treatment in ALS patients diagnosed with "definite ALS" or "probable ALS" showed slowing of disease progression, regardless of baseline urate level. "( Associations between the ALSFRS-R score and urate levels during 12 months of edaravone treatment for amyotrophic lateral sclerosis: Post hoc analysis of ALSFRS-R scores in clinical studies MCI186-16, MCI186-17, and MCI186-19.
Kano, O; Nagano, Y; Nelson, S; Takahashi, F; Ushirogawa, Y; Yoneoka, T, 2022
)
2.39
"Edaravone treatment reduced differential VWMD protein expression of the UPR, phagosome regulation, ubiquitination, autophagy, ER stress, senescence, and TCA cycle pathways."( Edaravone and mitochondrial transfer as potential therapeutics for vanishing white matter disease astrocyte dysfunction.
Carroll, L; Chung, J; Maksour, S; Newbery, M; Ng, NS; Ooi, L; Touffu, A; Wu, Y; Zaw, T, 2023
)
3.07
"Edaravone treatment could significantly reduce lung permeability, decrease tissue pro-apoptosis protein (cleaved-caspase3) and inflammation (IL-1β). "( [Edaravone has a protective role in a mouse model of pulmonary oxygen toxicity].
Bao, XC; Fang, YQ; Ma, J; Wang, FF, 2020
)
2.91
"Edaravone pretreatment suppressed epileptiform activity by reducing the mean spike frequency and the behavior scores in ECoG recording."( Anticonvulsive effects of edaravone on penicillin-induced focal onset seizure model in the conscious rats.
Aygun, H; Kurt, S, 2021
)
1.64
"Edaravone pretreatment ameliorated propofol-induced proliferation inhibition, neuroapoptosis, and neural inflammation by activating the mBDNF/TrkB/PI3K pathway."( Edaravone Alleviated Propofol-Induced Neurotoxicity in Developing Hippocampus by mBDNF/TrkB/PI3K Pathway.
Duan, H; Hu, B; Pan, M; Yang, Y; Yi, J, 2021
)
3.51
"Edaravone treatment normalized altered biochemical markers compared with the untreated control."( Edaravone acts as a potential therapeutic drug against pentylenetetrazole-induced epilepsy in male albino rats by downregulating cyclooxygenase-II.
Liu, LM; Lu, Y; Wang, N; Wang, WP, 2019
)
2.68
"Edaravone treatment significantly ameliorated neurological deficits, brain edema, and BBB disruption."( The Role of Oxidative Stress in Microvascular Disturbances after Experimental Subarachnoid Hemorrhage.
Fumoto, T; Katagai, T; Li, Y; Naraoka, M; Ohkuma, H; Shimamura, N, 2019
)
1.24
"Edaravone treatment improved the rats' body weight (p < 0.01) and feed intake levels (p < 0.05), improved the histological scores and alleviated the fibrosis of pancreas samples (p < 0.05), as well as markedly increased superoxide dismutase (SOD) activity and decreased malondialdehyde (MDA) concentrations in pancreatic tissue (p < 0.01 for both). "( Protective effects of edaravone on experimental chronic pancreatitis induced by dibutyltin dichloride in rats.
Dong, Y; Hu, DM; Li, LY; Wang, SF; Zhou, CH; Zhu, XY,
)
1.89
"The edaravone-treated animals also exhibited higher rCBF in the contralateral hemisphere compared with that seen in -vehicle-treated animals."( Edaravone increases regional cerebral blood flow after traumatic brain injury in mice.
Aruga, T; Dohi, K; Kiriyama, K; Miyamoto, K; Nakano, H; Ohtaki, H; Shioda, S; Song, D; Tsumuraya, T, 2013
)
2.31
"In Edaravone-treated group, 500 µmol/L Edaravone was prophylactically added to the medium for 30 minutes before the insult."( [The study of the protective effect and its mechanism of Edaravone to neurons with hydrogen peroxide stimulated].
Cai, WH; Cheng, G; Fan, J; Li, QQ; Li, YM; Long, H; Tang, J; Yin, GY; Zhang, N, 2013
)
1.15
"Edaravone-treated group were 0.90% ± 0.07%, 1.10% ± 0.08%, 3.50% ± 1.90%, 12.60% ± 1.10%, which were lower than H₂O₂-treated group (F = 362.7, P < 0.01)."( [The study of the protective effect and its mechanism of Edaravone to neurons with hydrogen peroxide stimulated].
Cai, WH; Cheng, G; Fan, J; Li, QQ; Li, YM; Long, H; Tang, J; Yin, GY; Zhang, N, 2013
)
1.36
"Edaravone treatment also decreased the postischemic hemorrhage volumes (53.4 mm(3) in edaravone-treated rats vs 176.4 mm(3) in controls)."( Edaravone, a free radical scavenger, attenuates cerebral infarction and hemorrhagic infarction in rats with hyperglycemia.
Johshita, H; Miyazaki, H; Okamura, K; Shiokawa, Y; Tsubokawa, T, 2014
)
2.57
"Edaravone treatment (3mg/kg, i.p."( A radical scavenger edaravone inhibits matrix metalloproteinase-9 upregulation and blood-brain barrier breakdown in a mouse model of prolonged cerebral hypoperfusion.
Arai, K; Liang, AC; Maki, T; Miyamoto, N; Pham, LD, 2014
)
1.45
"Edaravone treatment at 3 mg/kg significantly reduced apomorphine-induced rotational behavior (P < 0.01), improved the spontaneous behavior, prevented the decrease in the levels of TH-positive cells, Nissl bodies and GSH, and inhibited the increase in the levels of MDA (P < 0.05) in SN of rats with 6-OHDA-induced PD."( Edaravone protects neurons in the rat substantia nigra against 6-hydroxydopamine-induced oxidative stress damage.
Li, M; Liu, X; Shao, R; Yang, G, 2014
)
2.57
"The edaravone-treated animals demonstrated an increased number of engrafted donor hepatocytes in the liver. "( Effects of edaravone, a radical scavenger, on hepatocyte transplantation.
Fox, IJ; Hayashi, C; Hiramatsu, N; Horiguchi, A; Ito, M; Ito, R; Murakumo, A; Yamamoto, N, 2014
)
1.35
"Edaravone treatment attenuated neuronal apoptosis as compared with the poisoning group (P < 0.01)."( Edaravone attenuates brain damage in rats after acute CO poisoning through inhibiting apoptosis and oxidative stress.
Bi, MJ; Bi, WK; Guo, YL; Kang, H; Li, Q; Yan, le J, 2016
)
2.6
"Edaravone treatment increased plasma uric acid, suggesting that it is an effective scavenger of peroxynitrite."( Increased oxidative stress in patients with amyotrophic lateral sclerosis and the effect of edaravone administration.
Miyazaki, Y; Nagase, M; Yamamoto, Y; Yoshino, H, 2016
)
1.38
"Edaravone-pretreated BMSCs, control-released edaravone, and BMSCs were respectively transplanted into a rat AMI model."( Edaravone promotes activation of resident cardiac stem cells by transplanted mesenchymal stem cells in a rat myocardial infarction model.
Gu, TX; Li-Ling, J; Qi, X; Sun, XJ; Wang, C; Wang, XB; Zhang, GW, 2016
)
2.6
"Edaravone was treated twice via tail vein; after MCA occlusion and after reperfusion."( A free radical scavenger edaravone suppresses systemic inflammatory responses in a rat transient focal ischemia model.
Arai, K; Fujiwara, N; Lee, BJ; Lo, EH; Mandeville, ET; Pham, LD; Som, AT, 2016
)
1.46
"Edaravone (18 mg/kg) treatment did not prevent hyperlocomotion in the mania model induced with ketamine in rats, but lithium chloride (47.5 mg/kg, i.p., positive control) did prevent hyperlocomotion."( The effects of edaravone in ketamine-induced model of mania in rats.
Altun, İK; Alver, A; Arslan, FC; Gedikli, Ö; İnce, İ; Özkorumak, E; Tiryaki, A; Yıldırım, M, 2016
)
1.51
"Edaravone pretreatment reduced markedly the productions of ROS-HR and MDA and increased the activities of GSH-PX and SOD. "( Pretreatment with edaravone reduces lung mitochondrial damage in an infant rabbit ischemia-reperfusion model.
Chen, D; Chen, Y; Gu, H; Qiu, W; Zheng, L; Zhou, J, 2008
)
2.12
"Edaravone pretreatment reduces the IR-induced lung mitochondrial damage in infant rabbits."( Pretreatment with edaravone reduces lung mitochondrial damage in an infant rabbit ischemia-reperfusion model.
Chen, D; Chen, Y; Gu, H; Qiu, W; Zheng, L; Zhou, J, 2008
)
2.12
"Edaravone treatment significantly reduced the lesion volume and improved the neurological score."( Mechanistic insight into neurotoxicity of tissue plasminogen activator-induced thrombolysis products in a rat intraluminal middle cerebral artery occlusion model.
Fujii, M; Fujisawa, H; Gondo, T; Izuma, H; Kajiwara, K; Kato, S; Nomura, S; Oka, F; Suzuki, M; Uozumi, K, 2009
)
1.07
"Edaravone treatment shifted the %FAC(initial)–%FAC(final) relationship downward (P < 0.0001), indicating that edaravone inhibited progression of LV dilation."( Development of cardiac dysfunction induced by repetitive transient myocardial ischemia is inhibited by edaravone in conscious rats.
Imai, K; Kawamoto, T; Miyamoto, Y; Neishi, Y; Okura, H; Toyota, E; Yoshida, K, 2009
)
1.29
"The edaravone-treated SC group demonstrated less severe apoptosis than the untreated SC group."( [Effects of edaravone on IRE1 mRNA expression and neuronal apoptosis in the hippocampus of rats with status convulsivus].
Deng, XL; Jiao, Y; Li, GQ, 2009
)
1.21
"Edaravone treatment significantly reduced the elevated malondialdehyde levels in rat lungs after acute pancreatitis, suggesting an important role for free radicals in acute pancreatitis-associated lung injury."( Protective effects of the free radical scavenger edaravone on acute pancreatitis-associated lung injury.
Cai, ZY; Deng, XM; Hou, J; Hu, JY; Liu, SQ; Mao, YF; Ni, X; Yang, T; Zhu, XY, 2010
)
1.34
"The edaravone pretreatment group received edaravone by intraperitoneal injection once daily three days before convulsion induction."( [Protection of edaravone on neurons and its effects on the expression of interleukin-lbeta in juvenile rat hippocampus following status convulsion].
Li, GQ; Wang, HP, 2010
)
1.19
"The edaravone pretreatment group showed less severe neuronal changes compared with the SC group under the microscopes."( [Protection of edaravone on neurons and its effects on the expression of interleukin-lbeta in juvenile rat hippocampus following status convulsion].
Li, GQ; Wang, HP, 2010
)
1.19
"Edaravone pretreatment may decrease the IL-1beta expression and neuronal apoptosis in the hippocampus. "( [Protection of edaravone on neurons and its effects on the expression of interleukin-lbeta in juvenile rat hippocampus following status convulsion].
Li, GQ; Wang, HP, 2010
)
2.16
"Edaravone treatment for up to 14 days suppresses the progression of disuse muscle atrophy and improves leg locomotor function to a greater extent than shorter-term treatment in acute stroke patients. "( Effects of edaravone on muscle atrophy and locomotor function in patients with ischemic stroke: a randomized controlled pilot study.
Higashi, Y; Kondo, H; Metoki, N; Moriwaki, H; Naritomi, H; Nishimura, H; Oda, T; Oe, H; Saito, K; Tanahashi, N; Tanaka, K; Terayama, Y; Yamamoto, Y; Yuasa, H, 2010
)
2.19
"Edaravone-treated male rats showed significantly better performance in the landing foot-splay test."( Feasibility study for functional test battery of SOD transgenic rat (H46R) and evaluation of edaravone, a free radical scavenger.
Aoki, M; Itoyama, Y; Mizuno, H; Suzuki, N; Warita, H; Yuki, S, 2011
)
1.31
"Edaravone treatment may aid in preventing photoreceptor cell death after RD by suppressing ROS-induced photoreceptor damage."( Edaravone, an ROS scavenger, ameliorates photoreceptor cell death after experimental retinal detachment.
Miller, JW; Murakami, Y; Roh, MI; Thanos, A; Vavvas, DG, 2011
)
2.53
"Edaravone treatment reduced the volume of the infarct and improved neurological deficits during the subacute period, especially in the small-vessel occlusion strokes."( Free radical scavenger, edaravone, reduces the lesion size of lacunar infarction in human brain ischemic stroke.
Nakase, T; Suzuki, A; Yoshioka, S, 2011
)
2.12
"Edaravone treatment significantly decreased hippocampal CA3 neuron loss, reduced oxidative stress, and decreased neuronal programmed cell death compared to vehicle treatment."( Free-radical scavenger edaravone treatment confers neuroprotection against traumatic brain injury in rats.
Chen, J; Gao, YQ; Jiang, ZL; Li, X; Li, YC; Shi, H; Vosler, PS; Wang, GH, 2011
)
1.4
"Edaravone treatment significantly inhibited both lipid and DNA oxidative damage 72h after ischemia, and decreased neuronal damage."( Edaravone, a free radical scavenger, attenuates behavioral deficits following transient forebrain ischemia by inhibiting oxidative damage in gerbils.
Hirooka, K; Itano, T; Kawai, N; Keep, RF; Liu, Y; Lu, F; Miyamoto, O; Nakamura, T; Okabe, N; Shiraga, F; Tamiya, T; Toyoshima, T, 2012
)
2.54
"Edaravone-treated DCM rats showed better cardiac function compared with those of the vehicle-treated rats."( Beneficial effects of edaravone, a novel antioxidant, in rats with dilated cardiomyopathy.
Arozal, W; Arumugam, S; Giridharan, VV; Harima, M; Kodama, M; Nagata, M; Nakamura, T; Palaniyandi, SS; Sari, FR; Soetikno, V; Suzuki, K; Thandavarayan, RA; Veeraveedu, PT; Watanabe, K, 2012
)
1.41
"Edaravone treatment significantly reduced messenger RNA expressions of cytokines and matrix metalloproteinases (MMPs) in aneurysm walls (MMP-2: 1.1 ± 0.5 in group LD, 0.6 ± 0.1 in group HD, and 2.3 ± 0.4 in group C; P < .001; MMP-9: 1.2 ± 0.1 in group LD, 0.2 ± 0.6 in group HD, and 2.4 ± 0.2 in group C; P < .001)."( Free-radical scavenger edaravone inhibits both formation and development of abdominal aortic aneurysm in rats.
Hasegawa, T; Morimoto, K; Morimoto, N; Okada, K; Okita, Y; Tanaka, A; Wulan, B; Yu, J, 2012
)
1.41
"Edaravone or taurine treatment prevented significantly the decreased body, testicular, and epididymal weight induced by diabetes."( Antioxidant treatment with edaravone or taurine ameliorates diabetes-induced testicular dysfunction in the rat.
Dimitriadis, F; Koukos, S; Saito, M; Satoh, K; Shimizu, S; Sofikitis, N; Takenaka, A; Tsounapi, P, 2012
)
1.4
"Edaravone treatment significantly elevated cell viability, reduced apoptotic rate, attenuated oxidative stress and improved mitochondrial membrane potential in N2a/Swe.Δ9 cells."( Protective effect of edaravone against Alzheimer's disease-relevant insults in neuroblastoma N2a cells.
Gong, K; Gong, Y; Ma, T; Tang, P; Yan, Y; Zhang, L; Zhang, X; Zhao, N, 2012
)
1.42
"Edaravone treatment also reduced mucosal MPO activity, mucosal tissue lipid peroxidate level and serum IL-6 level."( The free radical scavenger edaravone suppresses experimental dextran sulfate sodium-induced colitis in rats.
Andoh, A; Araki, Y; Fujiyama, Y, 2003
)
1.34
"Edaravone treatment improved the response to the level observed in nonirradiated control vessels."( Normalization by edaravone, a free radical scavenger, of irradiation-reduced endothelial nitric oxide synthase expression.
Gando, S; Hattori, Y; Jesmin, S; Kemmotsu, O; Matsuda, N; Sakuraya, F; Zhang, XH, 2003
)
1.38
"Edaravone+tPA-treated group: Edaravone (3 mg/kg, i.v.) was given every 1.5 hours instead of saline and tPA injection as above."( Extension of ischemic therapeutic time window by a free radical scavenger, Edaravone, reperfused with tPA in rat brain.
Abe, K; Hayashi, T; Horiuchi, S; Kato, S; Nagano, I; Omori, N; Sato, K; Zhang, W, 2004
)
1.28
"Edaravone treatment decreased the neutrophil infiltration, the lipid membrane peroxidation, and the expression of proinflammatory cytokine interleukin-6 mRNA in the lungs after intestinal I/R compared to the I/R-treated rat lungs without edaravone treatment."( Edaravone protects against lung injury induced by intestinal ischemia/reperfusion in rat.
Horikawa, S; Ito, K; Ozasa, H, 2005
)
2.49
"Edaravone-treated animals showed significantly improved neurological outcome."( Anti-apoptotic and neuroprotective effects of edaravone following transient focal ischemia in rats.
Amemiya, S; Inaba, T; Kamiya, T; Katayama, Y; Kato, K; Nito, C; Shimazaki, K; Ueda, M, 2005
)
1.31
"Edaravone treatment (10mg/kg i.p.) for 3 days suppressed endothelial apoptosis, as evaluated by chromatin staining of en face specimens at 24h, by approximately 40%."( Potent free radical scavenger, edaravone, suppresses oxidative stress-induced endothelial damage and early atherosclerosis.
Akishita, M; Eto, M; Hasegawa, H; Kozaki, K; Nagai, K; Toba, K; Xi, H; Yu, W, 2007
)
1.35
"Edaravone treatment induces significant reduction of free radical precursors and their metabolites compared with controls in burn rats. "( The therapeutic efficacy of edaravone in extensively burned rats.
Koizumi, T; Sakaki, S; Shimazaki, S; Tanaka, H, 2006
)
2.07
"Edaravone treatment immediately or 2 hours after ICH also ameliorated neurologic deficits (P<0.05)."( Edaravone attenuates brain edema and neurologic deficits in a rat model of acute intracerebral hemorrhage.
Itano, T; Keep, RF; Kuroda, Y; Miyamoto, O; Nagao, S; Nakamura, T; Tamiya, T; Xi, G; Yamashita, S; Zhang, X, 2008
)
2.51
"Pretreatment with edaravone may reduce the level of autophagy in neurons subjected to OGD/R injury."( Edaravone inhibits autophagy after neuronal oxygen-glucose deprivation/recovery injury.
Chen, J; Ding, Q; Fan, J; Gu, J; Tang, P; Wang, Q; Yin, G; Yin, J; Zhou, Z, 2019
)
2.29
"Treatment with edaravone significantly improved STZ-induced cognitive damage as evaluated in Morris water maze and step-down tests and markedly restored changes in malondialdehyde (MDA), 4-hydroxy-2-nonenal (4-HNE) adducts, hydroxyl radical (OH), hydrogen peroxide (H2O2), total superoxide dismutase (T-SOD), reduced glutathione (GSH), glutathione peroxidase (GPx) and protein carbonyl (PC) levels."( Neuroprotective effects of edaravone on cognitive deficit, oxidative stress and tau hyperphosphorylation induced by intracerebroventricular streptozotocin in rats.
Chi, L; Yu, G; Zhang, L; Zhang, W; Zhang, Y; Zhou, S; Zhu, J, 2013
)
1.03
"Pretreatment with edaravone significantly inhibited hypoxia-induced oxidative stress formation and sFlt-1 expression in trophoblasts."( Edaravone inhibits hypoxia-induced trophoblast-soluble Fms-like tyrosine kinase 1 expression: a possible therapeutic approach to preeclampsia.
Han, L; Liu, XX; Luo, QQ; Yan, T; Zhao, Y; Zheng, YF; Zou, L, 2014
)
2.17
"Treatment with edaravone significantly increased the number of NSPCs and newly generated neurons in the subgranular zone (p < .05)."( Pre- and posttreatment with edaravone protects CA1 hippocampus and enhances neurogenesis in the subgranular zone of dentate gyrus after transient global cerebral ischemia in rats.
Chen, X; Gao, M; He, X; Lei, S; Li, W; Li, X; Liu, Y; Lu, H; Qi, C; Wang, N; Wang, X; Zhang, J; Zhang, P; Zheng, J, 2014
)
1.04
"Pretreatment with edaravone, dexamethasone, or L-NMMA attenuated the hyperpermeability and inhibited the cytokine-induced reduction of VE-cadherin expression on immunofluorescence staining."( Inhibitory Effects of Edaravone, a Free Radical Scavenger, on Cytokine-induced Hyperpermeability of Human Pulmonary Microvascular Endothelial Cells:A Comparison with Dexamethasone and Nitric Oxide Synthase Inhibitor.
Fujii, Y; Morishima, T; Nosaka, N; Saito, Y; Tsuge, M; Tsukahara, H; Yamada, M; Yamashita, N; Yashiro, M, 2015
)
1.06
"Treatment with edaravone significantly ameliorated the clinical severity of EAE, and a reduced infiltration of lymphocytes was observed based on a histological analysis."( Edaravone, a free radical scavenger, ameliorates experimental autoimmune encephalomyelitis.
Kinoshita, M; Kumanogoh, A; Kusunoki, S; Miyamoto, K; Moriya, M; Nakatsuji, Y; Okuno, T; Sakoda, S, 2008
)
2.13
"Pretreatment with edaravone significantly improved motor dysfunction and reduced the lesion volume to about 63% of the control (p < 0.05)."( Edaravone (MCI-186) scavenges reactive oxygen species and ameliorates tissue damage in the murine spinal cord injury model.
Aoyama, T; Hida, K; Iwasaki, Y; Kuroda, S; Seki, T; Shichinohe, H; Yano, S, 2008
)
2.11
"Treatment with edaravone prevented partially but significantly the decreased body and penile weight induced by diabetes. "( Edaravone ameliorates diabetes-induced dysfunction of NO-induced relaxation in corpus cavernosum smooth muscle in the rat.
Dimitriadis, F; Inoue, S; Kinoshita, Y; Ohmasa, F; Saito, M; Satoh, K; Shimizu, S; Shomori, K; Tsounapi, P, 2011
)
2.16
"Treatment with edaravone reduced fibrosis in mice with bleomycin-induced SSc and in TSK/+ mice. "( The specific free radical scavenger edaravone suppresses fibrosis in the bleomycin-induced and tight skin mouse models of systemic sclerosis.
Asano, Y; Iwata, Y; Kadono, T; Ogawa, A; Ogawa, F; Sato, S; Shimizu, K; Takenaka, M; Yanaba, K; Yoshizaki, A, 2011
)
1
"Treatment with edaravone (3 and 10 mg/kg) significantly diminished the cerebral infarct, oedema volume and improved functional recovery of neurological deficits."( Edaravone offers neuroprotection in a diabetic stroke model via inhibition of endoplasmic reticulum stress.
Sharma, SS; Srinivasan, K, 2012
)
2.16
"Treatment with edaravone not only mitigated cerebral infarct size (P<0.05) and neurological defects (P<0.05), but also decreased cell proliferation and neural progenitor cells in the ischemic ipsilateral SVZ (P<0.05)."( Treatment with edaravone attenuates ischemic brain injury and inhibits neurogenesis in the subventricular zone of adult rats after focal cerebral ischemia and reperfusion injury.
Chen, X; Gao, M; Lei, S; Li, L; Li, W; Li, X; Liu, Y; Lu, H; Wang, N; Zhang, P; Zheng, J, 2012
)
1.07
"For treatment with edaravone, edaravone was given daily to the animals from the day before irradiation at an intrapenetreal dose of 10 mg/kg twice a day."( Normalization by edaravone, a free radical scavenger, of irradiation-reduced endothelial nitric oxide synthase expression.
Gando, S; Hattori, Y; Jesmin, S; Kemmotsu, O; Matsuda, N; Sakuraya, F; Zhang, XH, 2003
)
0.98
"Pretreatment with edaravone can prevent occurrence of cerebral hyperperfusion after CEA."( Pretreatment with the free radical scavenger edaravone prevents cerebral hyperperfusion after carotid endarterectomy.
Endo, H; Fukuda, T; Inoue, T; Kobayashi, M; Ogasawara, K; Ogawa, A, 2004
)
0.92
"Pretreatment with edaravone scavenged the SN38-produced reactive oxygen species, and inhibited the SN38-induced activation of NF-kB."( The radical scavenger edaravone enhances the anti-tumor effects of CPT-11 in murine colon cancer by increasing apoptosis via inhibition of NF-kappaB.
Handa, O; Higashihara, H; Ishikawa, T; Kokura, S; Naito, Y; Nakabe, N; Sakamoto, N; Takagi, T; Yoshida, N; Yoshikawa, T, 2005
)
0.97
"Pretreatment with edaravone can prevent development of cognitive impairment after CEA."( Effects of the free radical scavenger, edaravone, on the development of postoperative cognitive impairment in patients undergoing carotid endarterectomy.
Endo, H; Fukuda, T; Inoue, T; Kobayashi, M; Ogasawara, K; Ogawa, A; Terasaki, K; Yamadate, K; Yoshida, K, 2005
)
0.93
"Pretreatment with edaravone (1 and 3 mg/kg i.p.) significantly reduced the neurotoxicity in the SNc but not striatum."( Edaravone (3-methyl-1-phenyl-2-pyrazolin-5-one), a radical scavenger, prevents 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced neurotoxicity in the substantia nigra but not the striatum.
Ago, Y; Baba, A; Ishihara, K; Kawasaki, T; Matsuda, T, 2007
)
2.11
"Pretreatment with edaravone but not post-treatment dose-dependently improved the response to high K+ but not the massive dopamine increase during ischemia."( Improvement of postischemic dopaminergic dysfunction by edaravone, a free radical scavenger.
Akiyama, Y; Miwa, S, 2007
)
0.91

Toxicity

Edaravone Dexborneol was safe and well tolerated at all doses, although no significant improvement in functional outcomes was observed at 90 days. Edarav one combined with alteplase seems to be safe and effective for AIS patients' short term outcomes.

ExcerptReferenceRelevance
" No adverse events were observed."( Stroke in a child safely treated with intravenous tissue plasminogen activator and edaravone, a free radical scavenger.
Baba, H; Hashizume, M; Kuwashiro, T; Lee, S; Nagata, H; Nanishi, E; Sugimori, H, 2012
)
0.6
"Edaravone was safe and well tolerated in the volunteers and displayed linear increases in the C(max) and AUC(τ) values."( Phase I clinical study of edaravone in healthy Chinese volunteers: safety and pharmacokinetics of single or multiple intravenous infusions.
Gong, X; Li, H; Li, T; Meng, L; Ou, N; Ruan, J; Wang, Y; Xu, K; Zhang, H, 2012
)
2.12
" Edaravone effectively protected against CNS-OT and the adverse effects of PFC."( Perfluorocarbon-facilitated CNS oxygen toxicity in rats: reversal by edaravone.
Cai, Z; Li, R; Liu, S; Ni, X; Quock, RM; Sun, X; Xu, W; Zhang, R, 2012
)
1.52
" Safety parameters included adverse events, severe adverse events, physical examinations, local reactions at infusion site, ECG, clinical chemistry and hematology, modified Total Neuropathy Score and CT scans."( Safety, tolerability and pharmacokinetics of MCI-186 in patients with acute ischemic stroke: new formulation and dosing regimen.
Dippel, DW; Ford, GA; Kaste, M; Murayama, S; Tatlisumak, T; Walters, MR, 2013
)
0.39
" The number of treatment emergent adverse events that occurred was 109, most of which were transient, mild or moderate."( Safety, tolerability and pharmacokinetics of MCI-186 in patients with acute ischemic stroke: new formulation and dosing regimen.
Dippel, DW; Ford, GA; Kaste, M; Murayama, S; Tatlisumak, T; Walters, MR, 2013
)
0.39
" Adverse events amounted to 88."( Confirmatory double-blind, parallel-group, placebo-controlled study of efficacy and safety of edaravone (MCI-186) in amyotrophic lateral sclerosis patients.
Abe, K; Akimoto, M; Aoki, M; Doyu, M; Hamada, C; Itoyama, Y; Kondo, K; Sobue, G; Tsuji, S; Yoneoka, T; Yoshino, H, 2014
)
0.62
" Previous studies have reported an increased generation of reactive oxygen species and oxidative stress in the toxic mechanism of VPA."( Edaravone ameliorates the adverse effects of valproic acid toxicity in small intestine.
Alev, B; Emekli-Alturfan, E; Koc-Ozturk, L; Oktay, S; Tunali, S; Tunali-Akbay, T; Yanardag, R; Yarat, A, 2015
)
1.86
" The aim of the present study was to assess the toxic effects of subacute exposure of Mn by measuring weight gain, motor performance, and biochemical parameters (complex I activity, lipid peroxides, and protein carbonyls) in brain mitochondria in rats."( Protection by Edaravone, a Radical Scavenger, against Manganese-Induced Neurotoxicity in Rats.
Apaydin, M; Erbas, O; Taskiran, D, 2016
)
0.79
" Treatment-emergent adverse events were reported in 58 (84%) patients receiving edaravone and 57 (84%) patients receiving placebo."( Safety and efficacy of edaravone in well defined patients with amyotrophic lateral sclerosis: a randomised, double-blind, placebo-controlled trial.
, 2017
)
0.99
" Endpoints included treatment-emergent adverse events (TEAEs), including AEs leading to discontinuation, serious adverse events (SAEs), and deaths."( A safety analysis of edaravone (MCI-186) during the first six cycles (24 weeks) of amyotrophic lateral sclerosis (ALS) therapy from the double-blind period in three randomized, placebo-controlled studies.
Ishizaki, K; Kalin, A; Kim, A; Medina-Paraiso, E; Saita, T; Wasaki, M; Zhang, Y, 2017
)
0.77
"Our results indicate that oral delivery of NEF holds a promise as a safe and effective therapeutic agent for AD."( Self-nanomicellizing solid dispersion of edaravone: part II: in vivo assessment of efficacy against behavior deficits and safety in Alzheimer's disease model.
Cao, X; Chen, C; Garg, S; Kathawala, K; Li, J; Parikh, A; Shan, Z; Wang, YJ; Zhou, XF, 2018
)
0.75
" Measure of safety was the frequency of investigated adverse events and serious adverse events."( Efficacy and safety of edaravone in treatment of amyotrophic lateral sclerosis-a systematic review and meta-analysis.
He, J; Li, X; Luo, L; Song, Z; Zeng, Y, 2019
)
0.82
" No differences in the frequency of adverse events (odds ratio [OR] = 1."( Efficacy and safety of edaravone in treatment of amyotrophic lateral sclerosis-a systematic review and meta-analysis.
He, J; Li, X; Luo, L; Song, Z; Zeng, Y, 2019
)
0.82
"Intravenous edaravone is efficacious in amyotrophic lateral sclerosis patients, with no severe adverse effects."( Efficacy and safety of edaravone in treatment of amyotrophic lateral sclerosis-a systematic review and meta-analysis.
He, J; Li, X; Luo, L; Song, Z; Zeng, Y, 2019
)
1.2
" Moreover, using C+P did not lead to any serious adverse effects when compared to the treatment group."( Low dose concomitant treatment with chlorpromazine and promethazine is safe in acute ischemic stroke.
Chandra, A; Cheng, Z; Ding, Y; Du, H; Geng, X; Tong, Y; Zhu, H, 2019
)
0.51
"While the addition of low dose chlorpromazine and promethazine to standard of care for acute ischemic stroke did not have any significant improvement in functional outcomes, there were no serious adverse effects."( Low dose concomitant treatment with chlorpromazine and promethazine is safe in acute ischemic stroke.
Chandra, A; Cheng, Z; Ding, Y; Du, H; Geng, X; Tong, Y; Zhu, H, 2019
)
0.51
" EDA was found to ameliorate autoimmune thyroiditis (Hashimoto thyroiditis), which is a frequent side effect observed after treatment of cancer patients with monoclonal antibodies targeting the immune checkpoint PD-1."( Potential use of edaravone to reduce specific side effects of chemo-, radio- and immuno-therapy of cancers.
Bailly, C, 2019
)
0.85
" The safety outcome included any adverse event during 90 days after treatment."( Safety and efficacy of Edaravone Dexborneol versus edaravone for patients with acute ischaemic stroke: a phase II, multicentre, randomised, double-blind, multiple-dose, active-controlled clinical trial.
Chen, H; Gao, X; Gao, Z; Wang, A; Wang, Y; Xu, J; Zhao, X; Zhou, J, 2019
)
0.82
" No significant difference in severe adverse events was found among the four groups (p=0."( Safety and efficacy of Edaravone Dexborneol versus edaravone for patients with acute ischaemic stroke: a phase II, multicentre, randomised, double-blind, multiple-dose, active-controlled clinical trial.
Chen, H; Gao, X; Gao, Z; Wang, A; Wang, Y; Xu, J; Zhao, X; Zhou, J, 2019
)
0.82
"Compared with edaravone alone, Edaravone Dexborneol was safe and well tolerated at all doses, although no significant improvement in functional outcomes was observed at 90days."( Safety and efficacy of Edaravone Dexborneol versus edaravone for patients with acute ischaemic stroke: a phase II, multicentre, randomised, double-blind, multiple-dose, active-controlled clinical trial.
Chen, H; Gao, X; Gao, Z; Wang, A; Wang, Y; Xu, J; Zhao, X; Zhou, J, 2019
)
1.19
" Adverse effects and the need of a special catheter for infusion were rare."( Logistics and safety of edaravone treatment for amyotrophic lateral sclerosis: experience in Argentina.
Bendersky, M; Quarracino, C; Rey, R; Rodríguez, GE, 2021
)
0.93
" While several trials in the last 8 years have reported the favourable long-term functional outcomes, a few reports indicated edaravone to be associated with an increase in adverse events."( Efficacy and safety of edaravone for acute intracerebral haemorrhage: protocol for a systematic review and meta-analysis.
Feng, L; Gao, Y; Guo, S; Jiang, P; Li, T; Liang, N; Yang, Q; Zhang, C, 2020
)
1.07
" The incidence of adverse events will be assessed for safety evaluation."( Efficacy and safety of edaravone for acute intracerebral haemorrhage: protocol for a systematic review and meta-analysis.
Feng, L; Gao, Y; Guo, S; Jiang, P; Li, T; Liang, N; Yang, Q; Zhang, C, 2020
)
0.87
" Safety evaluation was conducted according to the incidence of adverse events."( Clinical effects and safety of edaravone in treatment of acute ischaemic stroke: A meta-analysis of randomized controlled trials.
Chen, C; Chen, S; Chen, Y; Hong, L; Li, M; Lin, L, 2021
)
0.91
" The oral edaravone formulations were safe and tolerable under the assessed conditions."( Evaluation of Pharmacokinetics, Safety, and Drug-Drug Interactions of an Oral Suspension of Edaravone in Healthy Adults.
Akimoto, M; Kato, Y; Kondo, K; Matsuda, H; Matsuda, M; Nakamaru, Y; Nishimura, Y; Shiide, Y; Shimizu, H, 2021
)
1.24
" Conclusions: Edaravone combined with alteplase seems to be safe and effective for AIS patients' short term outcomes."( Safety and efficacy of edaravone combined with alteplase for patients with acute ischemic stroke: A systematic review and meta-analysis.
Guo, Y; Hu, R; Lin, Y; Tang, Q; Tang, Y; Wang, X; Yang, J, 2021
)
1.29
" Potential adverse effects were observed in 30 cases (16%), most notably infections at infusion sites and allergic reactions."( Safety and Effectiveness of Long-term Intravenous Administration of Edaravone for Treatment of Patients With Amyotrophic Lateral Sclerosis.
Cordts, I; Dorst, J; Grosskreutz, J; Günther, K; Günther, R; Hagenacker, T; Hermann, A; Koch, B; Koch, JC; Kohl, Z; Lingor, P; Löscher, WN; Ludolph, AC; Maier, A; Meyer, T; Michels, S; Petri, S; Prudlo, J; Ruckes, C; Sarikidi, A; Spittel, S; Steinbach, R; Witzel, S; Wolf, J, 2022
)
0.96
" Safety endpoints was include the incidence of adverse drug reactions."( Efficacy and Safety of Edaravone in Amyotrophic Lateral Sclerosis Patients in Indian Population.
Gupta, S; Singal, A; Soni, R; Tomar, S, 2022
)
1.03
"6%) of subjects receiving Edaravone therapy reported with adverse side-effects."( Efficacy and Safety of Edaravone in Amyotrophic Lateral Sclerosis Patients in Indian Population.
Gupta, S; Singal, A; Soni, R; Tomar, S, 2022
)
1.33
"Edaravone usage data were collected, and adverse events (AEs) were identified from a postmarketing safety database from August 8, 2017 through August 7, 2020 (cutoff date)."( Analysis of the US Safety Data for Edaravone (Radicava
Apple, S; Bower, L; Brooks, BR; Genge, A; Ji, M; Kalin, A; Oskarsson, B, 2022
)
2.44
" The most common treatment-emergent adverse events (TEAEs) at week 48 were fall (22."( Oral edaravone demonstrated a favorable safety profile in patients with amyotrophic lateral sclerosis after 48 weeks of treatment.
Aoki, M; Apple, S; Bidani, S; Couratier, P; Genge, A; Hirai, M; Jackson, CE; Kalin, A; Lunetta, C; Pattee, GL; Petri, S; Sakata, T; Salah, A; Selness, D; Sobue, G; Wamil, A; Yoshino, H, 2023
)
1.42
"Edaravone improves survival rates of ALS patients at 18, 24, and 30 months with no adverse effects."( Safety and efficacy of edaravone in patients with amyotrophic lateral sclerosis: a systematic review and meta-analysis.
Elhady, MM; Eshag, MME; Fathallah, AH; Hagrass, AI; Kamal, I; Nourelden, AZ; Tawfik, AG; Zaazouee, MS, 2023
)
2.66

Pharmacokinetics

Data from 3 Phase I clinical studies were used to evaluate the effect of food on the pharmacokinetic profiles of a single dose of edaravone oral suspension. Two methods were successfully applied to a drug-drug interaction study and a pharmacokinetics study of edravone and taurine in healthy Chinese volunteers.

ExcerptReferenceRelevance
"01) by verapamil (80 mg three times daily for 2 days prior to antipyrine administration and 2 days following) while half-life was increased from 13."( The effect of verapamil on antipyrine pharmacokinetics and metabolism in man.
Bach, D; Blevins, R; Edwards, DJ; Kerner, N; Rubenfire, M, 1986
)
0.27
" The first three months of life were characterised by a steady decrease in the apparent volume of distribution (aVd) and half-life (t0."( Effect of age on the pharmacokinetics of antipyrine in calves.
Janus, K; Suszycka, J, 1996
)
0.29
" The plasma elimination half-life of antipyrine was significantly elevated by 23% at 11 weeks postinfection (p."( Effect of experimental fasciolosis on antipyrine metabolism and clearance in water buffaloes.
Bayón, JE; Ferre, I; González-Gallego, J; Jiang, SX; Mao, XZ, 2000
)
0.31
"The aim was to investigate the pharmacokinetic interaction between puerarin and edaravone, and the effect of borneol on the brain distribution kinetics of puerarin in rats."( Pharmacokinetic interaction between puerarin and edaravone, and effect of borneol on the brain distribution kinetics of puerarin in rats.
Gao, C; Li, X; Li, Y; Wang, L; Xue, M, 2010
)
0.84
" The detection method was successfully applied to compare the pharmacokinetic interaction and brain distribution kinetics of puerarin and edaravone using in-situ microdialysis sampling in rats after intravenous administration and co-administration with a single dose."( Pharmacokinetic interaction between puerarin and edaravone, and effect of borneol on the brain distribution kinetics of puerarin in rats.
Gao, C; Li, X; Li, Y; Wang, L; Xue, M, 2010
)
0.82
" The validated methods were successfully applied to study the pharmacokinetic interaction of taurine and edaravone in rats after independent intravenous administration and co-administration with a single dose."( LC-MS/MS methods for the determination of edaravone and/or taurine in rat plasma and its application to a pharmacokinetic study.
Bian, TT; Du, Q; Jiang, SS; Li, Y; Li, YJ; Tang, DQ; Wu, XW; Zheng, XX, 2014
)
0.88
" The present work was primarily undertaken to provide a comprehensive clinical pharmacokinetic summary of the two approved ALS therapeutics."( Two Decades-Long Journey from Riluzole to Edaravone: Revisiting the Clinical Pharmacokinetics of the Only Two Amyotrophic Lateral Sclerosis Therapeutics.
Babu, RJ; Dash, RP; Srinivas, NR, 2018
)
0.75
" This study aimed to establish a pharmacokinetic (PK) model to fit the PK profile of edaravone after a single sublingual (SL) dose of a novel edaravone tablet and single IV infusion of injectable edaravone in healthy Chinese volunteers participating in a bioavailability study."( Predicting the Pharmacokinetic Characteristics of Edaravone Intravenous Injection and Sublingual Tablet Through Modeling and Simulation.
Chen, X; Liang, W; Sun, Z; Wang, J; Wang, Y; Zhao, X, 2020
)
1.04
" Two methods were successfully applied to a drug-drug interaction study and a pharmacokinetic study of edaravone and taurine in healthy Chinese volunteers after intravenous infusion of single or compound injection."( Two high-performance liquid chromatography-tandem mass spectrometry methods for determination of edaravone and taurine in human plasma: Application to drug-drug interaction and pharmacokinetic studies.
Ding, L; Li, L; Su, Y; Xu, L; Zhao, S, 2020
)
0.99
"Two studies were conducted to assess the pharmacokinetic (PK) properties and tolerability of edaravone in Japanese subjects with mild to moderate hepatic impairment or normal hepatic functioning (study 1), and in white subjects with severe hepatic impairment compared to subjects with normal hepatic functioning (study 2)."( Open-label, Single-dose Studies of the Pharmacokinetics of Edaravone in Subjects with Mild, Moderate, or Severe Hepatic Impairment Compared to Subjects with Normal Hepatic Functioning.
Akimoto, M; Greis, T; Kakubari, M; Kondo, K; Nakamaru, Y; Todorovic, V; Yoshida, K, 2020
)
1.02
" An oral suspension of edaravone has been developed, but the food effect on its pharmacokinetic profile has not been evaluated."( Food Effect Study to Assess the Impact on Edaravone Pharmacokinetic Profiles in Healthy Participants.
Akimoto, M; Hirai, M; Kato, Y; Matsuda, H; Nishimura, Y; Shiide, Y; Shimizu, H, 2022
)
1.3
"Data from 3 Phase I clinical studies were used to evaluate the effect of food on the pharmacokinetic profiles of a single dose of edaravone oral suspension."( Food Effect Study to Assess the Impact on Edaravone Pharmacokinetic Profiles in Healthy Participants.
Akimoto, M; Hirai, M; Kato, Y; Matsuda, H; Nishimura, Y; Shiide, Y; Shimizu, H, 2022
)
1.19
"The pharmacokinetic interactions between XNJ and EDA were studied by GC-MS in rats, and the inhibition of XNJ and (-)-borneol on UDP-glucuronosyltransferase (UGTs) were assayed by LC-MS/MS in vitro."( Herb-drug interaction of Xingnaojing injection and Edaravone via pharmacokinetics, mixed inhibition of UGTs, and molecular docking.
Gao, Y; Li, H; Li, Z; Liang, C; Liu, Z; Peng, P; Qi, D; Yang, Z; Zhang, Q, 2023
)
1.16
"(-)-Borneol modulates the pharmacokinetic behavior of edaravone via mixed inhibition of UGT2B7 and UGT1A6."( Herb-drug interaction of Xingnaojing injection and Edaravone via pharmacokinetics, mixed inhibition of UGTs, and molecular docking.
Gao, Y; Li, H; Li, Z; Liang, C; Liu, Z; Peng, P; Qi, D; Yang, Z; Zhang, Q, 2023
)
1.41

Compound-Compound Interactions

The addition of Shenxiong glucose injection combined with edaravone injection can improve platelet aggregation and reduce inflammation by affecting P-selectin, D-dimer, and FIB.

ExcerptReferenceRelevance
"The efficacy of hyperbaric oxygen (HBO) therapy combined with intravenous edaravone (free radical scavenger) administration was prospectively investigated in patients with acute embolic stroke involving the anterior cerebral circulation."( Hyperbaric oxygen combined with intravenous edaravone for treatment of acute embolic stroke: a pilot clinical trial.
Imai, K; Izumoto, H; Kunieda, T; Mori, T; Takabatake, N; Watanabe, M, 2006
)
0.83
"To investigate the effects of penehyclidine combined with edaravone on acute cerebral infarction (ACI) in rats."( Curative efficacy of penehyclidine combined with edaravone on acute cerebral infarction and their effects on serum TNF-α and NDS score in rats.
Chen, Y; Zhao, Y, 2018
)
0.98
" After grouping, rats in the treatment groups were treated with edaravone combined with phenecyclidine."( Curative efficacy of penehyclidine combined with edaravone on acute cerebral infarction and their effects on serum TNF-α and NDS score in rats.
Chen, Y; Zhao, Y, 2018
)
0.97
"Penehyclidine combined with edaravone has a better clinical treatment effect on ACI rats, which can significantly reduce the levels of serum TNF-α, IL-6 and HMGB1 and the NDS score, so it is worthy of popularization in clinical application."( Curative efficacy of penehyclidine combined with edaravone on acute cerebral infarction and their effects on serum TNF-α and NDS score in rats.
Chen, Y; Zhao, Y, 2018
)
1.03
" Here we analyzed the clinical outcomes of acute ischemic stroke (AIS) patients treated with human urinary kallidinogenase (HUK) or edaravone (Eda) combined with butylphthalide (NBP)."( Human urinary kallidinogenase or edaravone combined with butylphthalide in the treatment of acute ischemic stroke.
Jiang, M; Lu, S; Lyu, Y; Nie, T; Qian, Y; Tang, B, 2019
)
1
"Human urinary kallidinogenase combined with NBP can enhance AIS patients' long-term independency rate, and the effectiveness of HUK combined therapy is better than Eda."( Human urinary kallidinogenase or edaravone combined with butylphthalide in the treatment of acute ischemic stroke.
Jiang, M; Lu, S; Lyu, Y; Nie, T; Qian, Y; Tang, B, 2019
)
0.8
" Two methods were successfully applied to a drug-drug interaction study and a pharmacokinetic study of edaravone and taurine in healthy Chinese volunteers after intravenous infusion of single or compound injection."( Two high-performance liquid chromatography-tandem mass spectrometry methods for determination of edaravone and taurine in human plasma: Application to drug-drug interaction and pharmacokinetic studies.
Ding, L; Li, L; Su, Y; Xu, L; Zhao, S, 2020
)
0.99
"There involved a total of 118 patients with acute cerebral infarction from November 2017 to May 2019 in our hospital were randomly divided into 2 groups: the observation group (59 patients were treated with intravenous thrombolysis with alteplase combined with edaravone) and the control group (59 patients were treated with intravenous thrombolysis of alteplase)."( Effects of intravenous thrombolysis with alteplase combined with edaravone on cerebral hemodynamics and T lymphocyte level in patients with acute cerebral infarction.
Guo, SF; Li, XX; Liu, SH; Pang, SL; Zhuang, SJ, 2020
)
0.98
" Therefore, 2 phase 1 studies of oral formulations of edaravone in healthy subjects examined the pharmacokinetics (PK), safety, racial differences, and drug-drug interactions (DDIs) and investigated the dose of the oral formulation considered to be bioequivalent to the approved dose of the IV formulation."( Evaluation of Pharmacokinetics, Safety, and Drug-Drug Interactions of an Oral Suspension of Edaravone in Healthy Adults.
Akimoto, M; Kato, Y; Kondo, K; Matsuda, H; Matsuda, M; Nakamaru, Y; Nishimura, Y; Shiide, Y; Shimizu, H, 2021
)
1.09
"03%) patients received edaravone combined with alteplase treatment."( Safety and efficacy of edaravone combined with alteplase for patients with acute ischemic stroke: A systematic review and meta-analysis.
Guo, Y; Hu, R; Lin, Y; Tang, Q; Tang, Y; Wang, X; Yang, J, 2021
)
1.24
" In this study, we aimed to evaluate the protective effects of edaravone combined with dexamethasone on smoke-induced inhalational lung injury."( Edaravone combined with dexamethasone exhibits synergic effects on attenuating smoke-induced inhalation lung injury in rats.
Chen, K; Guo, H; He, J; Li, H; Liu, J; Xiao, K; Yang, R; Yang, W, 2021
)
2.3
"To investigate the clinical efficacy and safety of Shenxiong glucose injection combined with edaravone in the treatment of acute large-area cerebral infarction."( A Single-Center Clinical Study to Evaluate Shenxiong Glucose Injection Combined with Edaravone in the Treatment of Acute Large-Area Cerebral Infarction.
Huang, P; Li, Z; Luo, J; Rong, X; Xu, X; Zeng, T, 2021
)
1.06
"In addition to the routine basic treatment of acute large-area cerebral infarction, the addition of Shenxiong glucose injection combined with edaravone injection can improve platelet aggregation and reduce inflammation by affecting P-selectin, D-dimer, and FIB."( A Single-Center Clinical Study to Evaluate Shenxiong Glucose Injection Combined with Edaravone in the Treatment of Acute Large-Area Cerebral Infarction.
Huang, P; Li, Z; Luo, J; Rong, X; Xu, X; Zeng, T, 2021
)
1.05
"Several studies have investigated the efficacy of human urinary kallidinogenase (HUK) combined with edaravone (Eda) in acute ischemic stroke (AIS) patients."( Human urinary kallidinogenase combined with edaravone in treating acute ischemic stroke patients: A meta-analysis.
Chen, LQ; Guan, B; Li, Y; Ming, Q; Yang, DX; Yu, D, 2021
)
1.1
"HUK combined with Eda provides potential clinical benefits as a treatment for AIS."( Human urinary kallidinogenase combined with edaravone in treating acute ischemic stroke patients: A meta-analysis.
Chen, LQ; Guan, B; Li, Y; Ming, Q; Yang, DX; Yu, D, 2021
)
0.88
"This paper aimed to study the application value of Internet of Things (IoT) edge computing algorithm-based ultrasound-guided erector spinae plane block combined with edaravone anesthesia in thoracoscopic lobectomy."( Internet of Things-Based Ultrasound-Guided Erector Spinae Plane Block Combined with Edaravone Anesthesia in Thoracoscopic Lobectomy.
Li, L; Liu, C; Wang, X; Zhou, X, 2021
)
1.04
"The objective of this study was to investigate the effects of edaravone combined with oxiracetam on neuronal apoptosis in rats with cerebral infarction (CI) and to explore the potential molecular mechanism."( Effects of edaravone combined with Oxiracetam on neuronal apoptosis in rats with cerebral infarction through targeting SIRT1/NF-κB inflammatory pathway.
Cui, XP; Lin, H; Mu, JS; Ye, JX; Ye, S; Zhou, H, 2022
)
1.35
" After modeling, the rats in sham-operation group and model group were intraperitoneally injected with normal saline, and those in treatment group were administered with edaravone and oxiracetam solutions via intraperitoneal injection."( Effects of edaravone combined with Oxiracetam on neuronal apoptosis in rats with cerebral infarction through targeting SIRT1/NF-κB inflammatory pathway.
Cui, XP; Lin, H; Mu, JS; Ye, JX; Ye, S; Zhou, H, 2022
)
1.31
"Edaravone combined with oxiracetam can inhibit the neuronal apoptosis in CI rats by regulating the SIRT1/NF-κB signaling pathway, thereby exerting a neuroprotective effect."( Effects of edaravone combined with Oxiracetam on neuronal apoptosis in rats with cerebral infarction through targeting SIRT1/NF-κB inflammatory pathway.
Cui, XP; Lin, H; Mu, JS; Ye, JX; Ye, S; Zhou, H, 2022
)
2.55
"Edaravone combined with anticoagulant therapy is a reliable method to enhance ADL and reduce the inflammatory response of ACI patients."( Effect of Edaravone Combined with Anticoagulant Therapy on the Serum hs-CRP, IL-6, and TNF-
Ma, C; Ma, L; Sun, C; Sun, Y, 2022
)
2.57
"For investigating an influence on butylphthalide sodium chloride injection combined with edaravone dexborneol on neurological function and serum inflammatory factor levels in sufferers having acute ischemic stroke, 120 sufferers having acute ischemic stroke from September 2020 to September 2021 are chosen for the study subjects."( Effects of Butylphthalide Sodium Chloride Injection Combined with Edaravone Dexborneol on Neurological Function and Serum Inflammatory Factor Levels in Sufferers Having Acute Ischemic Stroke.
Li, K; Lu, X; Yao, S; Zhang, Q, 2022
)
1.18
"Eighty-one patients with T2DM combined with CS who attended our hospital and received rehabilitation treatment from March 2020 to May 2021 were enrolled to a prospective nonrandomized controlled analysis."( Significance of Edaravone Combined with Emotion Management Model in Promoting the Recovery Process and Improving Negative Psychology in Patients with Type 2 Diabetes Mellitus Combined with Stroke.
Lu, X; Lv, X, 2022
)
1.07
"The EDA combined with emotion management model can effectively promote the recovery process of patients with type II T2DM combined with CS, while improving their negative psychology and enhancing their self-management ability, which has high potential for clinical application."( Significance of Edaravone Combined with Emotion Management Model in Promoting the Recovery Process and Improving Negative Psychology in Patients with Type 2 Diabetes Mellitus Combined with Stroke.
Lu, X; Lv, X, 2022
)
1.07
"This study observed the effects of edaravone combined with Dl-3-N-butylphthalide (NBP) on the serum levels of tumor necrosis factor-alpha (TNF-α), interleukin-10 (IL-10), and neuron-specific enolase (NSE), and its therapeutic effect in patients with acute cerebral infarction (ACI)."( The effect of edaravone combined with DL-3-N-butylphthalide on the levels of tumor necrosis factor-alpha, interleukin-10, neuron-specific enolase and effect in patients with acute cerebral infarction.
Shen, QQ; Tong, XW; Wang, W; Wu, H, 2022
)
1.36
"This study will provide a comprehensive analysis of the current clinical evidence on the application of blood-activating herbs combined with EDA in the treatment of AIS."( Efficacy and safety of blood-activating herbs combined with edaravone in the treatment of acute ischemic stroke: A protocol for systematic review and meta-analysis.
Jin, H; Su, Z; Sun, W; Yang, Z; Yu, Z; Zhang, S; Zhao, D, 2022
)
0.96
" At present, little is known about the pharmacokinetics and potential mechanism of XNJ combined with EDA."( Herb-drug interaction of Xingnaojing injection and Edaravone via pharmacokinetics, mixed inhibition of UGTs, and molecular docking.
Gao, Y; Li, H; Li, Z; Liang, C; Liu, Z; Peng, P; Qi, D; Yang, Z; Zhang, Q, 2023
)
1.16
"The study aimed to explore the roles of alprostadil combined with edaravone in inflammation, oxidative stress and Pulmonary function in patients with traumatic hemorrhagic shock (HS)."( Effects of Alprostadil Combined with Edaravone on Inflammation, Oxidative Stress and Pulmonary Function in Patients with Traumatic Hemorrhagic Shock.
Bao, W; Luo, D; Pan, Q; Wang, L; Zhao, W, 2022
)
1.23
" Whether it can provide better outcomes when combined with edaravone injection (ERI) for the treatment of acute cerebral infarction is not well determined."( Edaravone combined with Shuxuening versus edaravone alone in the treatment of acute cerebral infarction: A systematic review and meta-analysis.
Li, LD; Shi, SF; Zhou, Y, 2023
)
2.6
"To investigate the efficacy of butylphthalide combined with edaravone in the treatment of acute ischemic stroke and the effect on serum inflammatory factors."( Efficacy of Butylphthalide in Combination with Edaravone in the Treatment of Acute Ischemic Stroke and the Effect on Serum Inflammatory Factors.
Hong, Z; Li, S; Li, Y; Liu, Y; Wang, J; Xie, S, 2023
)
1.41
" The control group was treated with edaravone injection, while the experimental group was treated with butylphthalide combined with edaravone."( Efficacy of Butylphthalide in Combination with Edaravone in the Treatment of Acute Ischemic Stroke and the Effect on Serum Inflammatory Factors.
Hong, Z; Li, S; Li, Y; Liu, Y; Wang, J; Xie, S, 2023
)
1.44
"The treatment of acute ischemic stroke with butylphthalide combined with edaravone has positive significance in improving blood circulation regulation and serum inflammatory factor levels and is reliable and worthy of clinical promotion."( Efficacy of Butylphthalide in Combination with Edaravone in the Treatment of Acute Ischemic Stroke and the Effect on Serum Inflammatory Factors.
Hong, Z; Li, S; Li, Y; Liu, Y; Wang, J; Xie, S, 2023
)
1.4

Bioavailability

The PK profiles after a single SL dose or IV infusion of edaravone 30 mg can be well described by a 3-compartment linear disposition model. The objective of the study was to evaluate the effect of hydroxypropyl-sulfobutyl-β-cyclodextrin (HP-SBE-βCD) on the bioavailability and intestinal absorption of edravone. Mathematical modeling determined that equivalent exposures in plasma with the approved dose of the IV edarvone formulation, as reported previously, could be achieved when the oral edarivone formulation w.

ExcerptReferenceRelevance
" On the other hand, bioavailability of oral mucosal, rectal and oral administration was about 100, 63."( A novel administration route of edaravone--II: mucosal absorption of edaravone from edaravone/hydroxypropyl-beta-cyclodextrin complex solution including L-cysteine and sodium hydrogen sulfite.
Ishii, F; Mizuno, K; Sato, T, 2010
)
0.64
" We have probably wasted too much time on agents like antioxidant vitamins instead of focusing on more disease specific, target-directed, highly bioavailable antioxidants."( Antioxidant therapy: current status and future prospects.
Firuzi, O; Miri, R; Saso, L; Tavakkoli, M, 2011
)
0.37
"These results support the critical role of NO in the microcirculation and suggest that free-radical scavenging increases the bioavailability of NO in the microcirculation via eNOS upregulation."( Effect of a free radical scavenger on nitric oxide release in microvessels.
Sakamoto, K; Totani, N; Yamamoto, J; Yamanishi, H; Yamashita, T, 2013
)
0.39
"The objective of the study was to evaluate the effect of hydroxypropyl-sulfobutyl-β-cyclodextrin (HP-SBE-βCD) on the bioavailability and intestinal absorption of edaravone, and identify its mechanism of action."( Hydroxypropyl-sulfobutyl-β-cyclodextrin improves the oral bioavailability of edaravone by modulating drug efflux pump of enterocytes.
Guo, M; Lu, Y; Lu, YP; Ren, Y; Rong, WT; Tao, Q; Yu, SQ, 2014
)
0.83
" Most importantly, 3d possessed a very high absolute bioavailability and was rapidly distributed in brain tissue to keep high plasma drug concentration for the treatment of ischemic strokes."( Discovery of 3-n-butyl-2,3-dihydro-1H-isoindol-1-one as a potential anti-ischemic stroke agent.
Lan, Z; Lei, M; Li, J; Liang, Z; Xu, W; Xu, X; Zhang, X; Zhao, C, 2015
)
0.42
"Edaravone (EDR), a strong free radical scavenger, is known for its promising therapeutic potential in oxidative stress (OS) associated diseases, however poor oral bioavailability is the major obstacle in its potential use."( Development of a novel oral delivery system of edaravone for enhancing bioavailability.
Garg, S; Kathawala, K; Parikh, A; Tan, CC; Zhou, XF, 2016
)
2.13
" However, its oral use is restricted due to poor oral bioavailability (BA)."( Lipid-based nanosystem of edaravone: development, optimization, characterization and in vitro/in vivo evaluation.
Garg, S; Kathawala, K; Parikh, A; Tan, CC; Zhou, XF, 2017
)
0.76
" Pharmacokinetic experiments performed with rats and beagles showed that the absolute bioavailability of EDR solution and enteric-coated pellets following oral administration were 33."( Gastric retention pellets of edaravone with enhanced oral bioavailability: Absorption mechanism, development, and in vitro/in vivo evaluation.
Cheng, Y; Guan, S; Hu, M; Huang, W; Li, Q; Mo, J; Ou, Z; Wang, J; Yang, J; Zhang, ZJ, 2018
)
0.77
"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
" This study aimed to establish a pharmacokinetic (PK) model to fit the PK profile of edaravone after a single sublingual (SL) dose of a novel edaravone tablet and single IV infusion of injectable edaravone in healthy Chinese volunteers participating in a bioavailability study."( Predicting the Pharmacokinetic Characteristics of Edaravone Intravenous Injection and Sublingual Tablet Through Modeling and Simulation.
Chen, X; Liang, W; Sun, Z; Wang, J; Wang, Y; Zhao, X, 2020
)
1.04
"The PK profiles after a single SL dose or IV infusion of edaravone 30 mg can be well described by a 3-compartment linear disposition model, on which a first-order absorption model with a lag time and a parameter for bioavailability was incorporated to fit the absorption phase of the SL dose."( Predicting the Pharmacokinetic Characteristics of Edaravone Intravenous Injection and Sublingual Tablet Through Modeling and Simulation.
Chen, X; Liang, W; Sun, Z; Wang, J; Wang, Y; Zhao, X, 2020
)
1.06
" Here, we developed macrophage-derived exosomes (Exo) containing Edv (Exo + Edv) to improve the bioavailability of Edv and enhance the neuroprotective effects in a rat model of permanent middle cerebral artery occlusion (PMCAO)."( Edaravone-Loaded Macrophage-Derived Exosomes Enhance Neuroprotection in the Rat Permanent Middle Cerebral Artery Occlusion Model of Stroke.
Li, F; Liang, J; Shi, Y; Zhao, L, 2020
)
2
" Mathematical modeling determined that equivalent exposures in plasma with the approved dose of the IV edaravone formulation, as reported previously, could be achieved when the oral edaravone formulation was administered at a dose of  ≈100 mg, with an absolute bioavailability of ≈60%."( Evaluation of Pharmacokinetics, Safety, and Drug-Drug Interactions of an Oral Suspension of Edaravone in Healthy Adults.
Akimoto, M; Kato, Y; Kondo, K; Matsuda, H; Matsuda, M; Nakamaru, Y; Nishimura, Y; Shiide, Y; Shimizu, H, 2021
)
1.06
" Although EDV promotes ischemic recovery by inhibiting the generation of ROS, its poor safety and bioavailability limit its clinical applications."( A novel brain targeted plasma exosomes enhance the neuroprotective efficacy of edaravone in ischemic stroke.
Guo, L; Li, F; Pan, J; Shi, Y; Zhao, L, 2021
)
0.85
" Highly bioavailable form of novel edaravone formulation developed using self-nanomicellizing solid dispersion strategy which showed up to 16."( Neuroprotection of Oral Edaravone on Middle Cerebral Artery Occlusion in Rats.
Luo, HY; Parikh, A; Xiong, YX; Ye, QY; Zhao, LQ; Zhou, XF, 2022
)
1.31
" This randomized, open-label, two-way crossover, single-dose phase 1 study compared the relative bioavailability of a newly developed edaravone oral suspension when administered orally and via a nasogastric tube (NGT) as a model of percutaneous endoscopic gastrostomy tube administration in healthy adult subjects."( Edaravone Administered Orally and Via Nasogastric Tube in Healthy Adults: A Comparative Bioavailability Phase 1 Study.
Hirai, M; Kato, Y; Nishimura, Y; Shiide, Y; Shimizu, H; Ueda, M; Yokota, S, 2023
)
2.56
" However, poor water solubility, low stability, and bioavailability in aqueous media are major EDV drawbacks."( Enhancing the Neuroprotection Potential of Edaravone in Transient Global Ischemia Treatment with Glutathione- (GSH-) Conjugated Poly(methacrylic acid) Nanogel as a Promising Carrier for Targeted Brain Drug Delivery.
Bijani, S; Danafar, H; Hosseini, MJ; Islambulchilar, Z; Kalantari-Hesari, A; Mozafari, F; Ramazani, A; Rashidzadeh, H; Zare-Molaei, F, 2023
)
1.17

Dosage Studied

The protective effect of edaravone showed the dose-response was at the same level as that of dimethylthiourea. Edarvone and Scutellarin effectively suppressed the inflammatory responses in activated microglia. The model is expected to be useful for predicting the concentration-time profiles of edravone following different dosing regimens.

ExcerptRelevanceReference
" Unknown additional peaks were detected in urine after NORA dosing but not after HMA or OHA administration."( The pharmacokinetics of antipyrine and three of its metabolites in the rabbit: intravenous administration of pure metabolites.
Abul-Hajj, Y; Awni, WM; St Peter, JV, 1991
)
0.28
" Mefloquine (750 mg) had no significant effect on salivary kinetics of antipyrine or on the metabolic clearance of antipyrine to its three main metabolites, 3-hydroxymethylantipyrine, 4-hydroxyantipyrine and norantipyrine, when antipyrine was administered either 2 h or 2 weeks after dosing with mefloquine."( The pharmacokinetics of mefloquine in man: lack of effect of mefloquine on antipyrine metabolism.
Back, DJ; Breckenridge, AM; Howells, RE; Rivière, JH, 1985
)
0.27
" Seven-day-old rat pups were subjected to a modified Levine procedure, then given either vehicle or MCI-186 (at one of three dosage levels: 3, 6, or 9 mg/kg), and the extent of brain damage was evaluated either 24 h or 7 days later."( Effect of the free radical scavenger, 3-methyl-1-phenyl-2-pyrazolin-5-one (MCI-186), on hypoxia-ischemia-induced brain injury in neonatal rats.
Ikeda, T; Ikenoue, T; Kaneko, M; Sameshima, H; Xia, YX, 2002
)
0.31
" In this study, we evaluated the efficacy of edaravone, a newly synthesized free radical scavenger, in its clinical dosage on an experimental model of acute liver injury in rats."( A free radical scavenger, edaravone, attenuates steatosis and cell death via reducing inflammatory cytokine production in rat acute liver injury.
Ishii, H; Kameyama, K; Kitamura, K; Kurita, S; Nakamoto, N; Saito, H; Saito, Y; Tada, S, 2003
)
0.88
" The protective effect of edaravone showed the dose-response was at the same level as that of dimethylthiourea."( Radical scavenger edaravone developed for clinical use ameliorates ischemia/reperfusion injury in rat kidney.
Doi, K; Fujita, T; Nakao, A; Noiri, E; Suzuki, Y, 2004
)
0.96
" Data from the permanent MCAO model and an embolic stroke model suggested a bell shaped dose-response curve."( Free radical trapping as a therapeutic approach to neuroprotection in stroke: experimental and clinical studies with NXY-059 and free radical scavengers.
Ashwood, T; Green, AR, 2005
)
0.33
" Edaravone might be a hopeful therapeutic option for PD, although the high therapeutic dosage remains to be solved for the clinical application."( Neuroprotective effects of edaravone-administration on 6-OHDA-treated dopaminergic neurons.
Agari, T; Baba, T; Date, I; Jing, M; Kameda, M; Leung, H; Matsui, T; Miyoshi, Y; Morimoto, T; Muraoka, K; Shingo, T; Tajiri, N; Uozumi, T; Wang, F; Yasuhara, T; Yuan, WJ, 2008
)
1.55
" However, the optimal total dosage of edaravone has not been established."( Does functional outcome in acute ischaemic stroke patients correlate with the amount of free-radical scavenger treatment? A retrospective study of edaravone therapy.
Katayama, M; Shimizu, H; Unno, Y, 2010
)
0.83
"In a double-blind, placebo-controlled randomized clinical trial we studied two dosing regimens, each in a cohort of 18 patients."( Safety, tolerability and pharmacokinetics of MCI-186 in patients with acute ischemic stroke: new formulation and dosing regimen.
Dippel, DW; Ford, GA; Kaste, M; Murayama, S; Tatlisumak, T; Walters, MR, 2013
)
0.39
" Both doses of the new formulation and dosing regimen were well tolerated."( Safety, tolerability and pharmacokinetics of MCI-186 in patients with acute ischemic stroke: new formulation and dosing regimen.
Dippel, DW; Ford, GA; Kaste, M; Murayama, S; Tatlisumak, T; Walters, MR, 2013
)
0.39
"The primary objective of the present study, safety and tolerability of the new formulation and dosing regimen, was achieved."( Safety, tolerability and pharmacokinetics of MCI-186 in patients with acute ischemic stroke: new formulation and dosing regimen.
Dippel, DW; Ford, GA; Kaste, M; Murayama, S; Tatlisumak, T; Walters, MR, 2013
)
0.39
" The effect of higher dosage of Edaravone on circulating MMP-9 concentration and subsequent hemorrhagic transformation should be investigated."( Effects of edaravone, a free radical scavenger, on circulating levels of MMP-9 and hemorrhagic transformation in patients with intravenous thrombolysis using low-dose alteplase.
Atsumi, C; Hagiwara, Y; Hasegawa, Y; Imai, T; Mizukami, H; Tsuruoka, A,
)
0.8
"In vivo, both Edaravone and Scutellarin markedly reduced the infarct cerebral tissue area with the latter drug being more effective with the dosage used; furthermore, when used in combination the reduction was more substantial."( Anti-inflammatory effects of Edaravone and Scutellarin in activated microglia in experimentally induced ischemia injury in rats and in BV-2 microglia.
Ling, EA; Rangarajan, P; Wu, C; Yuan, Y; Zha, H, 2014
)
1.05
"The results suggest that Edaravone and Scutellarin effectively suppressed the inflammatory responses in activated microglia, with Scutellarin being more efficacious within the dosage range used."( Anti-inflammatory effects of Edaravone and Scutellarin in activated microglia in experimentally induced ischemia injury in rats and in BV-2 microglia.
Ling, EA; Rangarajan, P; Wu, C; Yuan, Y; Zha, H, 2014
)
1
" We investigated the protective effects of an antioxidant substance, edaravone, and its slow-release dosage form, edaravone solid lipid nanoparticles (SLNs), in steady noise-exposed guinea pigs."( Solid lipid nanoparticles loaded with edaravone for inner ear protection after noise exposure.
Gao, G; Jiang, P; Liu, Y; Sun, JJ; Zhou, CH, 2015
)
0.92
" However, its dosage and effects have not yet been established in children."( Efficacy, safety, and outcomes in 17 pediatric cases treated with the free radical scavenger edaravone.
Aihara, Y; Kawamata, T; Nakamoto, H; Okada, Y; Yamaguchi, K, 2015
)
0.64
" Oral liquid dosage form is the most preferred delivery method in paediatric, geriatric and specialised therapies."( Development of a novel oral delivery system of edaravone for enhancing bioavailability.
Garg, S; Kathawala, K; Parikh, A; Tan, CC; Zhou, XF, 2016
)
0.69
" Questions regarding whether the dosing regimen could be simplified or improved, the duration of the effects, and the timing of the potential treatment to different stages of disease remain to be answered."( What can we learn from the edaravone development program for ALS?
Maragakis, NJ, 2017
)
0.75
" Based on this review, the following key highlights were deduced: (i) as a result of both presystemic metabolism and polymorphic hepatic cytochrome P450 (CYP) metabolism, the oral drug riluzole exhibited more inter-subject variability than that of intravenous edaravone; (ii) using various parameters for comparison, including the published intravenous data for riluzole, it was apparent that edaravone was achieving the desired systemic concentrations to possibly drive the local brain concentrations for its efficacy in ALS patients with lesser variability than riluzole; (iii) using scientific conjectures, it was deduced that the availability of intravenous riluzole may not be beneficial in therapy due to its fast systemic clearance; (iv) on the contrary, however, there appeared to be an opportunity for the development of an oral dosage form of edaravone, which may potentially benefit the therapy option for ALS patients by avoiding hospitalization costs; and (v) because of the existence of pharmaco-resistance for the brain entry in ALS patients, it appeared prudent to consider combination strategies of edaravone and/or riluzole with suitable P-glycoprotein efflux-blocking drugs to gain more favorable outcomes in ALS patients."( Two Decades-Long Journey from Riluzole to Edaravone: Revisiting the Clinical Pharmacokinetics of the Only Two Amyotrophic Lateral Sclerosis Therapeutics.
Babu, RJ; Dash, RP; Srinivas, NR, 2018
)
0.92
" This short report provides an overview of the two drugs that have been approved for ALS treatment and highlights an update on the timeline of drug development, how clinical trials were done, the outcome of these trials, primary endpoint, mechanism of actions, dosing information, administration, side effects, and storage procedures."( Riluzole and edaravone: A tale of two amyotrophic lateral sclerosis drugs.
Jaiswal, MK, 2019
)
0.88
" The model is expected to be useful for predicting the concentration-time profiles of edaravone following different dosing regimens in a healthy Chinese population."( Predicting the Pharmacokinetic Characteristics of Edaravone Intravenous Injection and Sublingual Tablet Through Modeling and Simulation.
Chen, X; Liang, W; Sun, Z; Wang, J; Wang, Y; Zhao, X, 2020
)
1.03
"The resultant estimates support the possibility and feasibility of demonstrating bioequivalence between an SL administration of edaravone 60 mg and the currently approved dosing regimen for ALS (ie, 60 mg IV over 60 min) once per day."( Predicting the Pharmacokinetic Characteristics of Edaravone Intravenous Injection and Sublingual Tablet Through Modeling and Simulation.
Chen, X; Liang, W; Sun, Z; Wang, J; Wang, Y; Zhao, X, 2020
)
1.02
"The models can be further applied to simulate favorable concentration-time profiles in diseases with different underlying courses of oxidative stress, and hence facilitate the optimization of current dosing regimens."( Predicting the Pharmacokinetic Characteristics of Edaravone Intravenous Injection and Sublingual Tablet Through Modeling and Simulation.
Chen, X; Liang, W; Sun, Z; Wang, J; Wang, Y; Zhao, X, 2020
)
0.81
"1-Phenyl-3-methyl-5-pyrazolone is a reagent, known as PMP, used to derivatize monosaccharides for the study of polysaccharides composition and structure, and for the dosage of carbohydrates in complex media."( Chemical reactivity and uses of 1-phenyl-3-methyl-5-pyrazolone (PMP), also known as edaravone.
Bailly, C; Goossens, JF; Hecquet, PE; Kouach, M; Thuru, X, 2020
)
0.78
" Thus, edaravone dosage adjustments are unlikely to be needed in edaravone-treated patients with mild to moderate and severe hepatic impairment."( Open-label, Single-dose Studies of the Pharmacokinetics of Edaravone in Subjects with Mild, Moderate, or Severe Hepatic Impairment Compared to Subjects with Normal Hepatic Functioning.
Akimoto, M; Greis, T; Kakubari, M; Kondo, K; Nakamaru, Y; Todorovic, V; Yoshida, K, 2020
)
1.26
"Findings will provide timely information on the safety, efficacy, and optimal dosing of t-PA to treat moderate/severe COVID-19-induced ARDS, which can be rapidly adapted to a phase III trial (NCT04357730; FDA IND 149634)."(
Abbasi, S; Abd El-Wahab, A; Abdallah, M; Abebe, G; Aca-Aca, G; Adama, S; Adefegha, SA; Adidigue-Ndiome, R; Adiseshaiah, P; Adrario, E; Aghajanian, C; Agnese, W; Ahmad, A; Ahmad, I; Ahmed, MFE; Akcay, OF; Akinmoladun, AC; Akutagawa, T; Alakavuklar, MA; Álava-Rabasa, S; Albaladejo-Florín, MJ; Alexandra, AJE; Alfawares, R; Alferiev, IS; Alghamdi, HS; Ali, I; Allard, B; Allen, JD; Almada, E; Alobaid, A; Alonso, GL; Alqahtani, YS; Alqarawi, W; Alsaleh, H; Alyami, BA; Amaral, BPD; Amaro, JT; Amin, SAW; Amodio, E; Amoo, ZA; Andia Biraro, I; Angiolella, L; Anheyer, D; Anlay, DZ; Annex, BH; Antonio-Aguirre, B; Apple, S; Arbuznikov, AV; Arinsoy, T; Armstrong, DK; Ash, S; Aslam, M; Asrie, F; Astur, DC; Atzrodt, J; Au, DW; Aucoin, M; Auerbach, EJ; Azarian, S; Ba, D; Bai, Z; Baisch, PRM; Balkissou, AD; Baltzopoulos, V; Banaszewski, M; Banerjee, S; Bao, Y; Baradwan, A; Barandika, JF; Barger, PM; Barion, MRL; Barrett, CD; Basudan, AM; Baur, LE; Baz-Rodríguez, SA; Beamer, P; Beaulant, A; Becker, DF; Beckers, C; Bedel, J; Bedlack, R; Bermúdez de Castro, JM; Berry, JD; Berthier, C; Bhattacharya, D; Biadgo, B; Bianco, G; Bianco, M; Bibi, S; Bigliardi, AP; Billheimer, D; Birnie, DH; Biswas, K; Blair, HC; Bognetti, P; Bolan, PJ; Bolla, JR; Bolze, A; Bonnaillie, P; Borlimi, R; Bórquez, J; Bottari, NB; Boulleys-Nana, JR; Brighetti, G; Brodeur, GM; Budnyak, T; Budnyk, S; Bukirwa, VD; Bulman, DM; Burm, R; Busman-Sahay, K; Butcher, TW; Cai, C; Cai, H; Cai, L; Cairati, M; Calvano, CD; Camacho-Ordóñez, A; Camela, E; Cameron, T; Campbell, BS; Cansian, RL; Cao, Y; Caporale, AS; Carciofi, AC; Cardozo, V; Carè, J; Carlos, AF; Carozza, R; Carroll, CJW; Carsetti, A; Carubelli, V; Casarotta, E; Casas, M; Caselli, G; Castillo-Lora, J; Cataldi, TRI; Cavalcante, ELB; Cavaleiro, A; Cayci, Z; Cebrián-Tarancón, C; Cedrone, E; Cella, D; Cereda, C; Ceretti, A; Ceroni, M; Cha, YH; Chai, X; Chang, EF; Chang, TS; Chanteux, H; Chao, M; Chaplin, BP; Chaturvedi, S; Chaturvedi, V; Chaudhary, DK; Chen, A; Chen, C; Chen, HY; Chen, J; Chen, JJ; Chen, K; Chen, L; Chen, Q; Chen, R; Chen, SY; Chen, TY; Chen, WM; Chen, X; Chen, Y; Cheng, G; Cheng, GJ; Cheng, J; Cheng, YH; Cheon, HG; Chew, KW; Chhoker, S; Chiu, WN; Choi, ES; Choi, MJ; Choi, SD; Chokshi, S; Chorny, M; Chu, KI; Chu, WJ; Church, AL; Cirrincione, A; Clamp, AR; Cleff, MB; Cohen, M; Coleman, RL; Collins, SL; Colombo, N; Conduit, N; Cong, WL; Connelly, MA; Connor, J; Cooley, K; Correa Ramos Leal, I; Cose, S; Costantino, C; Cottrell, M; Cui, L; Cundall, J; Cutaia, C; Cutler, CW; Cuypers, ML; da Silva Júnior, FMR; Dahal, RH; Damiani, E; Damtie, D; Dan-Li, W; Dang, Z; Dasa, SSK; Davin, A; Davis, DR; de Andrade, CM; de Jong, PL; de Oliveira, D; de Paula Dorigam, JC; Dean, A; Deepa, M; Delatour, C; Dell'Aiera, S; Delley, MF; den Boer, RB; Deng, L; Deng, Q; Depner, RM; Derdau, V; Derici, U; DeSantis, AJ; Desmarini, D; Diffo-Sonkoue, L; Divizia, M; Djenabou, A; Djordjevic, JT; Dobrovolskaia, MA; Domizi, R; Donati, A; Dong, Y; Dos Santos, M; Dos Santos, MP; Douglas, RG; Duarte, PF; Dullaart, RPF; Duscha, BD; Edwards, LA; Edwards, TE; Eichenwald, EC; El-Baba, TJ; Elashiry, M; Elashiry, MM; Elashry, SH; Elliott, A; Elsayed, R; Emerson, MS; Emmanuel, YO; Emory, TH; Endale-Mangamba, LM; Enten, GA; Estefanía-Fernández, K; Estes, JD; Estrada-Mena, FJ; Evans, S; Ezra, L; Faria de, RO; Farraj, AK; Favre, C; Feng, B; Feng, J; Feng, L; Feng, W; Feng, X; Feng, Z; Fernandes, CLF; Fernández-Cuadros, ME; Fernie, AR; Ferrari, D; Florindo, PR; Fong, PC; Fontes, EPB; Fontinha, D; Fornari, VJ; Fox, NP; Fu, Q; Fujitaka, Y; Fukuhara, K; Fumeaux, T; Fuqua, C; Fustinoni, S; Gabbanelli, V; Gaikwad, S; Gall, ET; Galli, A; Gancedo, MA; Gandhi, MM; Gao, D; Gao, K; Gao, M; Gao, Q; Gao, X; Gao, Y; Gaponenko, V; Garber, A; Garcia, EM; García-Campos, C; García-Donas, J; García-Pérez, AL; Gasparri, F; Ge, C; Ge, D; Ge, JB; Ge, X; George, I; George, LA; Germani, G; Ghassemi Tabrizi, S; Gibon, Y; Gillent, E; Gillies, RS; Gilmour, MI; Goble, S; Goh, JC; Goiri, F; Goldfinger, LE; Golian, M; Gómez, MA; Gonçalves, J; Góngora-García, OR; Gonul, I; González, MA; Govers, TM; Grant, PC; Gray, EH; Gray, JE; Green, MS; Greenwald, I; Gregory, MJ; Gretzke, D; Griffin-Nolan, RJ; Griffith, DC; Gruppen, EG; Guaita, A; Guan, P; Guan, X; Guerci, P; Guerrero, DT; Guo, M; Guo, P; Guo, R; Guo, X; Gupta, J; Guz, G; Hajizadeh, N; Hamada, H; Haman-Wabi, AB; Han, TT; Hannan, N; Hao, S; Harjola, VP; Harmon, M; Hartmann, MSM; Hartwig, JF; Hasani, M; Hawthorne, WJ; Haykal-Coates, N; Hazari, MS; He, DL; He, P; He, SG; Héau, C; Hebbar Kannur, K; Helvaci, O; Heuberger, DM; Hidalgo, F; Hilty, MP; Hirata, K; Hirsch, A; Hoffman, AM; Hoffmann, JF; Holloway, RW; Holmes, RK; Hong, S; Hongisto, M; Hopf, NB; Hörlein, R; Hoshino, N; Hou, Y; Hoven, NF; Hsieh, YY; Hsu, CT; Hu, CW; Hu, JH; Hu, MY; Hu, Y; Hu, Z; Huang, C; Huang, D; Huang, DQ; Huang, L; Huang, Q; Huang, R; Huang, S; Huang, SC; Huang, W; Huang, Y; Huffman, KM; Hung, CH; Hung, CT; Huurman, R; Hwang, SM; Hyun, S; Ibrahim, AM; Iddi-Faical, A; Immordino, P; Isla, MI; Jacquemond, V; Jacques, T; Jankowska, E; Jansen, JA; Jäntti, T; Jaque-Fernandez, F; Jarvis, GA; Jatt, LP; Jeon, JW; Jeong, SH; Jhunjhunwala, R; Ji, F; Jia, X; Jia, Y; Jian-Bo, Z; Jiang, GD; Jiang, L; Jiang, W; Jiang, WD; Jiang, Z; Jiménez-Hoyos, CA; Jin, S; Jobling, MG; John, CM; John, T; Johnson, CB; Jones, KI; Jones, WS; Joseph, OO; Ju, C; Judeinstein, P; Junges, A; Junnarkar, M; Jurkko, R; Kaleka, CC; Kamath, AV; Kang, X; Kantsadi, AL; Kapoor, M; Karim, Z; Kashuba, ADM; Kassa, E; Kasztura, M; Kataja, A; Katoh, T; Kaufman, JS; Kaupp, M; Kehinde, O; Kehrenberg, C; Kemper, N; Kerr, CW; Khan, AU; Khan, MF; Khan, ZUH; Khojasteh, SC; Kilburn, S; Kim, CG; Kim, DU; Kim, DY; Kim, HJ; Kim, J; Kim, OH; Kim, YH; King, C; Klein, A; Klingler, L; Knapp, AK; Ko, TK; Kodavanti, UP; Kolla, V; Kong, L; Kong, RY; Kong, X; Kore, S; Kortz, U; Korucu, B; Kovacs, A; Krahnert, I; Kraus, WE; Kuang, SY; Kuehn-Hajder, JE; Kurz, M; Kuśtrowski, P; Kwak, YD; Kyttaris, VC; Laga, SM; Laguerre, A; Laloo, A; Langaro, MC; Langham, MC; Lao, X; Larocca, MC; Lassus, J; Lattimer, TA; Lazar, S; Le, MH; Leal, DB; Leal, M; Leary, A; Ledermann, JA; Lee, JF; Lee, MV; Lee, NH; Leeds, CM; Leeds, JS; Lefrandt, JD; Leicht, AS; Leonard, M; Lev, S; Levy, K; Li, B; Li, C; Li, CM; Li, DH; Li, H; Li, J; Li, L; Li, LJ; Li, N; Li, P; Li, T; Li, X; Li, XH; Li, XQ; Li, XX; Li, Y; Li, Z; Li, ZY; Liao, YF; Lin, CC; Lin, MH; Lin, Y; Ling, Y; Links, TP; Lira-Romero, E; Liu, C; Liu, D; Liu, H; Liu, J; Liu, L; Liu, LP; Liu, M; Liu, T; Liu, W; Liu, X; Liu, XH; Liu, Y; Liuwantara, D; Ljumanovic, N; Lobo, L; Lokhande, K; Lopes, A; Lopes, RMRM; López-Gutiérrez, JC; López-Muñoz, MJ; López-Santamaría, M; Lorenzo, C; Lorusso, D; Losito, I; Lu, C; Lu, H; Lu, HZ; Lu, SH; Lu, SN; Lu, Y; Lu, ZY; Luboga, F; Luo, JJ; Luo, KL; Luo, Y; Lutomski, CA; Lv, W; M Piedade, MF; Ma, J; Ma, JQ; Ma, JX; Ma, N; Ma, P; Ma, S; Maciel, M; Madureira, M; Maganaris, C; Maginn, EJ; Mahnashi, MH; Maierhofer, M; Majetschak, M; Malla, TR; Maloney, L; Mann, DL; Mansuri, A; Marelli, E; Margulis, CJ; Marrella, A; Martin, BL; Martín-Francés, L; Martínez de Pinillos, M; Martínez-Navarro, EM; Martinez-Quintanilla Jimenez, D; Martínez-Velasco, A; Martínez-Villaseñor, L; Martinón-Torres, M; Martins, BA; Massongo, M; Mathew, AP; Mathews, D; Matsui, J; Matsumoto, KI; Mau, T; Maves, RC; Mayclin, SJ; Mayer, JM; Maynard, ND; Mayr, T; Mboowa, MG; McEvoy, MP; McIntyre, RC; McKay, JA; McPhail, MJW; McVeigh, AL; Mebazaa, A; Medici, V; Medina, DN; Mehmood, T; Mei-Li, C; Melku, M; Meloncelli, S; Mendes, GC; Mendoza-Velásquez, C; Mercadante, R; Mercado, MI; Merenda, MEZ; Meunier, J; Mi, SL; Michels, M; Mijatovic, V; Mikhailov, V; Milheiro, SA; Miller, DC; Ming, F; Mitsuishi, M; Miyashita, T; Mo, J; Mo, S; Modesto-Mata, M; Moeller, S; Monte, A; Monteiro, L; Montomoli, J; Moore, EE; Moore, HB; Moore, PK; Mor, MK; Moratalla-López, N; Moratilla Lapeña, L; Moreira, R; Moreno, MA; Mörk, AC; Morton, M; Mosier, JM; Mou, LH; Mougharbel, AS; Muccillo-Baisch, AL; Muñoz-Serrano, AJ; Mustafa, B; Nair, GM; Nakanishi, I; Nakanjako, D; Naraparaju, K; Nawani, N; Neffati, R; Neil, EC; Neilipovitz, D; Neira-Borrajo, I; Nelson, MT; Nery, PB; Nese, M; Nguyen, F; Nguyen, MH; Niazy, AA; Nicolaï, J; Nogueira, F; Norbäck, D; Novaretti, JV; O'Donnell, T; O'Dowd, A; O'Malley, DM; Oaknin, A; Ogata, K; Ohkubo, K; Ojha, M; Olaleye, MT; Olawande, B; Olomo, EJ; Ong, EWY; Ono, A; Onwumere, J; Ortiz Bibriesca, DM; Ou, X; Oza, AM; Ozturk, K; Özütemiz, C; Palacio-Pastrana, C; Palaparthi, A; Palevsky, PM; Pan, K; Pantanetti, S; Papachristou, DJ; Pariani, A; Parikh, CR; Parissis, J; Paroul, N; Parry, S; Patel, N; Patel, SM; Patel, VC; Pawar, S; Pefura-Yone, EW; Peixoto Andrade, BCO; Pelepenko, LE; Peña-Lora, D; Peng, S; Pérez-Moro, OS; Perez-Ortiz, AC; Perry, LM; Peter, CM; Phillips, NJ; Phillips, P; Pia Tek, J; Piner, LW; Pinto, EA; Pinto, SN; Piyachaturawat, P; Poka-Mayap, V; Polledri, E; Poloni, TE; Ponessa, G; Poole, ST; Post, AK; Potter, TM; Pressly, BB; Prouty, MG; Prudêncio, M; Pulkki, K; Pupier, C; Qian, H; Qian, ZP; Qiu, Y; Qu, G; Rahimi, S; Rahman, AU; Ramadan, H; Ramanna, S; Ramirez, I; Randolph, GJ; Rasheed, A; Rault, J; Raviprakash, V; Reale, E; Redpath, C; Rema, V; Remucal, CK; Remy, D; Ren, T; Ribeiro, LB; Riboli, G; Richards, J; Rieger, V; Rieusset, J; Riva, A; Rivabella Maknis, T; Robbins, JL; Robinson, CV; Roche-Campo, F; Rodriguez, R; Rodríguez-de-Cía, J; Rollenhagen, JE; Rosen, EP; Rub, D; Rubin, N; Rubin, NT; Ruurda, JP; Saad, O; Sabell, T; Saber, SE; Sabet, M; Sadek, MM; Saejio, A; Salinas, RM; Saliu, IO; Sande, D; Sang, D; Sangenito, LS; Santos, ALSD; Sarmiento Caldas, MC; Sassaroli, S; Sassi, V; Sato, J; Sauaia, A; Saunders, K; Saunders, PR; Savarino, SJ; Scambia, G; Scanlon, N; Schetinger, MR; Schinkel, AFL; Schladweiler, MC; Schofield, CJ; Schuepbach, RA; Schulz, J; Schwartz, N; Scorcella, C; Seeley, J; Seemann, F; Seinige, D; Sengoku, T; Seravalli, J; Sgromo, B; Shaheen, MY; Shan, L; Shanmugam, S; Shao, H; Sharma, S; Shaw, KJ; Shen, BQ; Shen, CH; Shen, P; Shen, S; Shen, Y; Shen, Z; Shi, J; Shi-Li, L; Shimoda, K; Shoji, Y; Shun, C; Silva, MA; Silva-Cardoso, J; Simas, NK; Simirgiotis, MJ; Sincock, SA; Singh, MP; Sionis, A; Siu, J; Sivieri, EM; Sjerps, MJ; Skoczen, SL; Slabon, A; Slette, IJ; Smith, MD; Smith, S; Smith, TG; Snapp, KS; Snow, SJ; Soares, MCF; Soberman, D; Solares, MD; Soliman, I; Song, J; Sorooshian, A; Sorrell, TC; Spinar, J; Staudt, A; Steinhart, C; Stern, ST; Stevens, DM; Stiers, KM; Stimming, U; Su, YG; Subbian, V; Suga, H; Sukhija-Cohen, A; Suksamrarn, A; Suksen, K; Sun, J; Sun, M; Sun, P; Sun, W; Sun, XF; Sun, Y; Sundell, J; Susan, LF; Sutjarit, N; Swamy, KV; Swisher, EM; Sykes, C; Takahashi, JA; Talmor, DS; Tan, B; Tan, ZK; Tang, L; Tang, S; Tanner, JJ; Tanwar, M; Tarazi, Z; Tarvasmäki, T; Tay, FR; Teketel, A; Temitayo, GI; Thersleff, T; Thiessen Philbrook, H; Thompson, LC; Thongon, N; Tian, B; Tian, F; Tian, Q; Timothy, AT; Tingle, MD; Titze, IR; Tolppanen, H; Tong, W; Toyoda, H; Tronconi, L; Tseng, CH; Tu, H; Tu, YJ; Tung, SY; Turpault, S; Tuynman, JB; Uemoto, AT; Ugurlu, M; Ullah, S; Underwood, RS; Ungell, AL; Usandizaga-Elio, I; Vakonakis, I; van Boxel, GI; van den Beucken, JJJP; van der Boom, T; van Slegtenhorst, MA; Vanni, JR; Vaquera, A; Vasconcellos, RS; Velayos, M; Vena, R; Ventura, G; Verso, MG; Vincent, RP; Vitale, F; Vitali, S; Vlek, SL; Vleugels, MPH; Volkmann, N; Vukelic, M; Wagner Mackenzie, B; Wairagala, P; Waller, SB; Wan, J; Wan, MT; Wan, Y; Wang, CC; Wang, H; Wang, J; Wang, JF; Wang, K; Wang, L; Wang, M; Wang, S; Wang, WM; Wang, X; Wang, Y; Wang, YD; Wang, YF; Wang, Z; Wang, ZG; Warriner, K; Weberpals, JI; Weerachayaphorn, J; Wehrli, FW; Wei, J; Wei, KL; Weinheimer, CJ; Weisbord, SD; Wen, S; Wendel Garcia, PD; Williams, JW; Williams, R; Winkler, C; Wirman, AP; Wong, S; Woods, CM; Wu, B; Wu, C; Wu, F; Wu, P; Wu, S; Wu, Y; Wu, YN; Wu, ZH; Wurtzel, JGT; Xia, L; Xia, Z; Xia, ZZ; Xiao, H; Xie, C; Xin, ZM; Xing, Y; Xing, Z; Xu, S; Xu, SB; Xu, T; Xu, X; Xu, Y; Xue, L; Xun, J; Yaffe, MB; Yalew, A; Yamamoto, S; Yan, D; Yan, H; Yan, S; Yan, X; Yang, AD; Yang, E; Yang, H; Yang, J; Yang, JL; Yang, K; Yang, M; Yang, P; Yang, Q; Yang, S; Yang, W; Yang, X; Yang, Y; Yao, JC; Yao, WL; Yao, Y; Yaqub, TB; Ye, J; Ye, W; Yen, CW; Yeter, HH; Yin, C; Yip, V; Yong-Yi, J; Yu, HJ; Yu, MF; Yu, S; Yu, W; Yu, WW; Yu, X; Yuan, P; Yuan, Q; Yue, XY; Zaia, AA; Zakhary, SY; Zalwango, F; Zamalloa, A; Zamparo, P; Zampini, IC; Zani, JL; Zeitoun, R; Zeng, N; Zenteno, JC; Zepeda-Palacio, C; Zhai, C; Zhang, B; Zhang, G; Zhang, J; Zhang, K; Zhang, Q; Zhang, R; Zhang, T; Zhang, X; Zhang, Y; Zhang, YY; Zhao, B; Zhao, D; Zhao, G; Zhao, H; Zhao, Q; Zhao, R; Zhao, S; Zhao, T; Zhao, X; Zhao, XA; Zhao, Y; Zhao, Z; Zheng, Z; Zhi-Min, G; Zhou, CL; Zhou, HD; Zhou, J; Zhou, W; Zhou, XQ; Zhou, Z; Zhu, C; Zhu, H; Zhu, L; Zhu, Y; Zitzmann, N; Zou, L; Zou, Y, 2022
)
0.72
" This study aimed to assess the food effect on the pharmacokinetic profile of edaravone after oral administration and to investigate dosing regimens and administration instructions with different meal intake and timing."( Food Effect Study to Assess the Impact on Edaravone Pharmacokinetic Profiles in Healthy Participants.
Akimoto, M; Hirai, M; Kato, Y; Matsuda, H; Nishimura, Y; Shiide, Y; Shimizu, H, 2022
)
1.21
" Patients received a 105-mg dose of oral edaravone in treatment cycles replicating the dosing of IV edaravone."( Oral edaravone demonstrated a favorable safety profile in patients with amyotrophic lateral sclerosis after 48 weeks of treatment.
Aoki, M; Apple, S; Bidani, S; Couratier, P; Genge, A; Hirai, M; Jackson, CE; Kalin, A; Lunetta, C; Pattee, GL; Petri, S; Sakata, T; Salah, A; Selness, D; Sobue, G; Wamil, A; Yoshino, H, 2023
)
1.69
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
radical scavengerA role played by a substance that can react readily with, and thereby eliminate, radicals.
antioxidantA substance that opposes oxidation or inhibits reactions brought about by dioxygen or peroxides.
[role 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]

Drug Classes (1)

ClassDescription
pyrazoloneA member of the class of pyrazoles in which one of the carbons of the pyrazole ring is substituted by an oxo group.
[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 (71)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency21.89590.003245.467312,589.2998AID2517
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency35.39770.004023.8416100.0000AID485290
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency2.33500.177814.390939.8107AID2147
acetylcholinesteraseHomo sapiens (human)Potency43.60200.002541.796015,848.9004AID1347397; AID1347398; AID1347399
thioredoxin reductaseRattus norvegicus (Norway rat)Potency79.43280.100020.879379.4328AID588453
RAR-related orphan receptor gammaMus musculus (house mouse)Potency30.82490.006038.004119,952.5996AID1159521
SMAD family member 2Homo sapiens (human)Potency49.27790.173734.304761.8120AID1346924
SMAD family member 3Homo sapiens (human)Potency49.27790.173734.304761.8120AID1346924
GLI family zinc finger 3Homo sapiens (human)Potency71.05280.000714.592883.7951AID1259369; AID1259392
Microtubule-associated protein tauHomo sapiens (human)Potency3.64260.180013.557439.8107AID1460
AR proteinHomo sapiens (human)Potency31.09230.000221.22318,912.5098AID743035
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency69.00830.013326.981070.7614AID1346978
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency6.88090.011212.4002100.0000AID1030
thyroid stimulating hormone receptorHomo sapiens (human)Potency39.81070.001318.074339.8107AID926; AID938
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency22.24410.001022.650876.6163AID1224838; AID1224839
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency21.24790.01237.983543.2770AID1346984; AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency0.01290.000214.376460.0339AID588532
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency20.10210.003041.611522,387.1992AID1159552; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency30.25860.000817.505159.3239AID588544
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency32.97230.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
pregnane X nuclear receptorHomo sapiens (human)Potency58.25730.005428.02631,258.9301AID1346982; AID720659
estrogen nuclear receptor alphaHomo sapiens (human)Potency48.38180.000229.305416,493.5996AID743069; AID743075; AID743079
GVesicular stomatitis virusPotency34.67130.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency24.54540.00108.379861.1304AID1645840
glucocerebrosidaseHomo sapiens (human)Potency31.62280.01268.156944.6684AID2101
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency62.03720.001024.504861.6448AID743215
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency47.55070.001019.414170.9645AID588537; AID743191
caspase-3Homo sapiens (human)Potency69.00830.013326.981070.7614AID1346978
IDH1Homo sapiens (human)Potency32.64270.005210.865235.4813AID686970
aryl hydrocarbon receptorHomo sapiens (human)Potency21.84050.000723.06741,258.9301AID743085; AID743122
Histone H2A.xCricetulus griseus (Chinese hamster)Potency113.00400.039147.5451146.8240AID1224845
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency39.50680.036619.637650.1187AID2100
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency3.98110.354828.065989.1251AID504847
flap endonuclease 1Homo sapiens (human)Potency8.91250.133725.412989.1251AID588795
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency89.12510.010323.856763.0957AID2662
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency61.76780.000627.21521,122.0200AID651741; AID743202
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency0.70790.050127.073689.1251AID588590
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency21.95110.00798.23321,122.0200AID2551
gemininHomo sapiens (human)Potency2.81840.004611.374133.4983AID624297
survival motor neuron protein isoform dHomo sapiens (human)Potency0.70790.125912.234435.4813AID1458
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency22.53580.031610.279239.8107AID884; AID885
lethal factor (plasmid)Bacillus anthracis str. A2012Potency0.00160.020010.786931.6228AID912
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
Interferon betaHomo sapiens (human)Potency34.67130.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency34.67130.01238.964839.8107AID1645842
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency34.67130.01238.964839.8107AID1645842
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency22.53581.000012.224831.6228AID885
cytochrome P450 2C9, partialHomo sapiens (human)Potency34.67130.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Amyloid-beta precursor proteinHomo sapiens (human)IC50 (µMol)50.00000.00053.889510.0000AID1265941
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
recombinase AMycobacterium tuberculosis H37RvEC50 (µMol)3.02450.018023.2882287.6000AID434968; AID435010
[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)
replicative DNA helicaseMycobacterium tuberculosis H37RvAC502.99800.057030.7482325.3000AID449749; AID449750
UDP-glucuronosyltransferase 1A9Homo sapiens (human)KmH6.00006.00006.00006.0000AID1210129
UDP-glucuronosyltransferase 1A7Homo sapiens (human)Km432.30005.00007.20009.4000AID1210126
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (145)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processUDP-glucuronosyltransferase 1A9Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A9Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A9Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A9Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A9Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A9Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A9Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 2B17Homo sapiens (human)
steroid metabolic processUDP-glucuronosyltransferase 2B17Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 2B17Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 2B17Homo sapiens (human)
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)
regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
cognitionAmyloid-beta precursor proteinHomo sapiens (human)
G2/M transition of mitotic cell cycleAmyloid-beta precursor proteinHomo sapiens (human)
microglial cell activationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of protein phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
suckling behaviorAmyloid-beta precursor proteinHomo sapiens (human)
astrocyte activation involved in immune responseAmyloid-beta precursor proteinHomo sapiens (human)
regulation of translationAmyloid-beta precursor proteinHomo sapiens (human)
protein phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
intracellular copper ion homeostasisAmyloid-beta precursor proteinHomo sapiens (human)
endocytosisAmyloid-beta precursor proteinHomo sapiens (human)
response to oxidative stressAmyloid-beta precursor proteinHomo sapiens (human)
cell adhesionAmyloid-beta precursor proteinHomo sapiens (human)
regulation of epidermal growth factor-activated receptor activityAmyloid-beta precursor proteinHomo sapiens (human)
Notch signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
axonogenesisAmyloid-beta precursor proteinHomo sapiens (human)
learning or memoryAmyloid-beta precursor proteinHomo sapiens (human)
learningAmyloid-beta precursor proteinHomo sapiens (human)
mating behaviorAmyloid-beta precursor proteinHomo sapiens (human)
locomotory behaviorAmyloid-beta precursor proteinHomo sapiens (human)
axo-dendritic transportAmyloid-beta precursor proteinHomo sapiens (human)
cholesterol metabolic processAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of cell population proliferationAmyloid-beta precursor proteinHomo sapiens (human)
adult locomotory behaviorAmyloid-beta precursor proteinHomo sapiens (human)
visual learningAmyloid-beta precursor proteinHomo sapiens (human)
regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of peptidyl-threonine phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleAmyloid-beta precursor proteinHomo sapiens (human)
microglia developmentAmyloid-beta precursor proteinHomo sapiens (human)
axon midline choice point recognitionAmyloid-beta precursor proteinHomo sapiens (human)
neuron remodelingAmyloid-beta precursor proteinHomo sapiens (human)
dendrite developmentAmyloid-beta precursor proteinHomo sapiens (human)
regulation of Wnt signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
extracellular matrix organizationAmyloid-beta precursor proteinHomo sapiens (human)
forebrain developmentAmyloid-beta precursor proteinHomo sapiens (human)
neuron projection developmentAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of chemokine productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of interleukin-1 beta productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of interleukin-6 productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of tumor necrosis factor productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
regulation of multicellular organism growthAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of neuron differentiationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of glycolytic processAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of mitotic cell cycleAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of JNK cascadeAmyloid-beta precursor proteinHomo sapiens (human)
astrocyte activationAmyloid-beta precursor proteinHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityAmyloid-beta precursor proteinHomo sapiens (human)
collateral sprouting in absence of injuryAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of inflammatory responseAmyloid-beta precursor proteinHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
regulation of synapse structure or activityAmyloid-beta precursor proteinHomo sapiens (human)
synapse organizationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of calcium-mediated signalingAmyloid-beta precursor proteinHomo sapiens (human)
neuromuscular process controlling balanceAmyloid-beta precursor proteinHomo sapiens (human)
synaptic assembly at neuromuscular junctionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of protein metabolic processAmyloid-beta precursor proteinHomo sapiens (human)
neuron apoptotic processAmyloid-beta precursor proteinHomo sapiens (human)
smooth endoplasmic reticulum calcium ion homeostasisAmyloid-beta precursor proteinHomo sapiens (human)
neuron cellular homeostasisAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAmyloid-beta precursor proteinHomo sapiens (human)
response to interleukin-1Amyloid-beta precursor proteinHomo sapiens (human)
modulation of excitatory postsynaptic potentialAmyloid-beta precursor proteinHomo sapiens (human)
NMDA selective glutamate receptor signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
regulation of spontaneous synaptic transmissionAmyloid-beta precursor proteinHomo sapiens (human)
cytosolic mRNA polyadenylationAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of long-term synaptic potentiationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of long-term synaptic potentiationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionAmyloid-beta precursor proteinHomo sapiens (human)
cellular response to amyloid-betaAmyloid-beta precursor proteinHomo sapiens (human)
regulation of presynapse assemblyAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of amyloid fibril formationAmyloid-beta precursor proteinHomo sapiens (human)
amyloid fibril formationAmyloid-beta precursor proteinHomo sapiens (human)
neuron projection maintenanceAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of T cell migrationAmyloid-beta precursor proteinHomo sapiens (human)
central nervous system developmentAmyloid-beta precursor proteinHomo sapiens (human)
lipid metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
androgen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 2B7Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1-6Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1-6Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
bilirubin conjugationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
acute-phase responseUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to nutrientUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
animal organ regenerationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to lipopolysaccharideUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to starvationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
negative regulation of steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
biphenyl catabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to ethanolUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to glucocorticoid stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to estradiol stimulusUDP-glucuronosyltransferase 1A1 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)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A7Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 1A7Homo sapiens (human)
coumarin metabolic processUDP-glucuronosyltransferase 1A7Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A7Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A7Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A7Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A7Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A7Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A7Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (36)

Processvia Protein(s)Taxonomy
retinoic acid bindingUDP-glucuronosyltransferase 1A9Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A9Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A9Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A9Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A9Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 2B17Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 2B17Homo sapiens (human)
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)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingAmyloid-beta precursor proteinHomo sapiens (human)
DNA bindingAmyloid-beta precursor proteinHomo sapiens (human)
serine-type endopeptidase inhibitor activityAmyloid-beta precursor proteinHomo sapiens (human)
signaling receptor bindingAmyloid-beta precursor proteinHomo sapiens (human)
protein bindingAmyloid-beta precursor proteinHomo sapiens (human)
heparin bindingAmyloid-beta precursor proteinHomo sapiens (human)
enzyme bindingAmyloid-beta precursor proteinHomo sapiens (human)
identical protein bindingAmyloid-beta precursor proteinHomo sapiens (human)
transition metal ion bindingAmyloid-beta precursor proteinHomo sapiens (human)
receptor ligand activityAmyloid-beta precursor proteinHomo sapiens (human)
PTB domain bindingAmyloid-beta precursor proteinHomo sapiens (human)
protein serine/threonine kinase bindingAmyloid-beta precursor proteinHomo sapiens (human)
signaling receptor activator activityAmyloid-beta precursor proteinHomo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 2B7Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 2B7Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1-6Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1-6Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1-6Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1-6Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1-6Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme inhibitor activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A1 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)
retinoic acid bindingUDP-glucuronosyltransferase 1A7Homo sapiens (human)
enzyme inhibitor activityUDP-glucuronosyltransferase 1A7Homo sapiens (human)
protein kinase C bindingUDP-glucuronosyltransferase 1A7Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A7Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A7Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A7Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A7Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (57)

Processvia Protein(s)Taxonomy
endoplasmic reticulumUDP-glucuronosyltransferase 1A9Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A9Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A9Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 2B17Homo sapiens (human)
membraneUDP-glucuronosyltransferase 2B17Homo sapiens (human)
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)
extracellular spaceAmyloid-beta precursor proteinHomo sapiens (human)
dendriteAmyloid-beta precursor proteinHomo sapiens (human)
extracellular regionAmyloid-beta precursor proteinHomo sapiens (human)
extracellular spaceAmyloid-beta precursor proteinHomo sapiens (human)
nuclear envelope lumenAmyloid-beta precursor proteinHomo sapiens (human)
cytoplasmAmyloid-beta precursor proteinHomo sapiens (human)
mitochondrial inner membraneAmyloid-beta precursor proteinHomo sapiens (human)
endosomeAmyloid-beta precursor proteinHomo sapiens (human)
early endosomeAmyloid-beta precursor proteinHomo sapiens (human)
endoplasmic reticulumAmyloid-beta precursor proteinHomo sapiens (human)
endoplasmic reticulum lumenAmyloid-beta precursor proteinHomo sapiens (human)
smooth endoplasmic reticulumAmyloid-beta precursor proteinHomo sapiens (human)
Golgi apparatusAmyloid-beta precursor proteinHomo sapiens (human)
Golgi lumenAmyloid-beta precursor proteinHomo sapiens (human)
Golgi-associated vesicleAmyloid-beta precursor proteinHomo sapiens (human)
cytosolAmyloid-beta precursor proteinHomo sapiens (human)
plasma membraneAmyloid-beta precursor proteinHomo sapiens (human)
clathrin-coated pitAmyloid-beta precursor proteinHomo sapiens (human)
cell-cell junctionAmyloid-beta precursor proteinHomo sapiens (human)
synaptic vesicleAmyloid-beta precursor proteinHomo sapiens (human)
cell surfaceAmyloid-beta precursor proteinHomo sapiens (human)
membraneAmyloid-beta precursor proteinHomo sapiens (human)
COPII-coated ER to Golgi transport vesicleAmyloid-beta precursor proteinHomo sapiens (human)
axonAmyloid-beta precursor proteinHomo sapiens (human)
growth coneAmyloid-beta precursor proteinHomo sapiens (human)
platelet alpha granule lumenAmyloid-beta precursor proteinHomo sapiens (human)
neuromuscular junctionAmyloid-beta precursor proteinHomo sapiens (human)
endosome lumenAmyloid-beta precursor proteinHomo sapiens (human)
trans-Golgi network membraneAmyloid-beta precursor proteinHomo sapiens (human)
ciliary rootletAmyloid-beta precursor proteinHomo sapiens (human)
dendritic spineAmyloid-beta precursor proteinHomo sapiens (human)
dendritic shaftAmyloid-beta precursor proteinHomo sapiens (human)
perikaryonAmyloid-beta precursor proteinHomo sapiens (human)
membrane raftAmyloid-beta precursor proteinHomo sapiens (human)
apical part of cellAmyloid-beta precursor proteinHomo sapiens (human)
synapseAmyloid-beta precursor proteinHomo sapiens (human)
perinuclear region of cytoplasmAmyloid-beta precursor proteinHomo sapiens (human)
presynaptic active zoneAmyloid-beta precursor proteinHomo sapiens (human)
spindle midzoneAmyloid-beta precursor proteinHomo sapiens (human)
recycling endosomeAmyloid-beta precursor proteinHomo sapiens (human)
extracellular exosomeAmyloid-beta precursor proteinHomo sapiens (human)
receptor complexAmyloid-beta precursor proteinHomo sapiens (human)
early endosomeAmyloid-beta precursor proteinHomo sapiens (human)
membrane raftAmyloid-beta precursor proteinHomo sapiens (human)
cell surfaceAmyloid-beta precursor proteinHomo sapiens (human)
Golgi apparatusAmyloid-beta precursor proteinHomo sapiens (human)
plasma membraneAmyloid-beta precursor proteinHomo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
endoplasmic reticulumUDP-glucuronosyltransferase 1-6Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1-6Homo sapiens (human)
intracellular membrane-bounded organelleUDP-glucuronosyltransferase 1-6Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1-6Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
plasma membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
perinuclear region of cytoplasmUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum chaperone complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cytochrome complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
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)
endoplasmic reticulumUDP-glucuronosyltransferase 1A7Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A7Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A7Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (289)

Assay IDTitleYearJournalArticle
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1210105Activity of human recombinant UGT1A3 expressed in insect cells assessed as enzyme mediated glucuronidation at 500 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1264240Neuroprotective activity against oxygen-glucose deprivation-induced neuronal cell death in Sprague-Dawley rat CGN cells at 50 uM preincubated for 24 hrs followed by induction of oxygen-glucose deprivation measured after 24 hrs relative to control2015European journal of medicinal chemistry, Oct-20, Volume: 103Design, synthesis and biological evaluation of tricyclic diterpene derivatives as novel neuroprotective agents against ischemic brain injury.
AID412356Antioxidant activity against Fe2SO4/ascorbate-induced lipid peroxidation in Wistar rat liver microsomal membrane by TBARS assay2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Edaravone derivatives containing NO-donor functions.
AID1210149Drug metabolism in human kidney microsomes assessed as intrinsic clearance for drug glucuronidation per mg tissue in absence of BSA by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1240307Antioxidant activity in rat PC12 cells assessed as reduction of H2O2/Fe2+-mediated hydroxyl radical formation at 10 uM preincubated for 1 hr followed by H2O2/Fe2+ addition by Griess assay2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Novel hybrids of 3-n-butylphthalide and edaravone: Design, synthesis and evaluations as potential anti-ischemic stroke agents.
AID1264253Anti-ischemic activity in Sprague-Dawley rat transient middle cerebral artery occlusion model assessed as reduction in infarct volume at 3 mg/kg, iv administered for 2 to 6 hrs post middle cerebral artery occlusion measured at 24 hrs by TTC staining-based2015European journal of medicinal chemistry, Oct-20, Volume: 103Design, synthesis and biological evaluation of tricyclic diterpene derivatives as novel neuroprotective agents against ischemic brain injury.
AID226891Scavenging activity against DPPH2003Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
A theoretical investigation on DPPH radical-scavenging mechanism of edaravone.
AID1294583Neuroprotective activity against glutamate-induced cell death in rat PC12 cells assessed as cell viability at 90 uM after 24 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Synthesis and biological evaluation of aryloxyacetamide derivatives as neuroprotective agents.
AID1401199Antiischemic stroke activity in Sprague-Dawley rat middle cerebral artery occlusion-induced ischemia-reperfusion injury model assessed as decrease in infarct size at 0.2 mg/kg, icv as nanoparticle measured after 72 hrs by TTC staining-based assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis, and evaluation of NDGA analogues as potential anti-ischemic stroke agents.
AID1210132Activity of human recombinant UGT2B7 expressed in insect cells assessed as enzyme mediated glucuronidation by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1210160Drug metabolism in human liver microsomes assessed as drug glucuronidation per mg tissue in presence of BSA by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1264233Neuroprotective activity against glutamate-induced neuronal cell death in Sprague-Dawley rat CGN cells assessed as cell viability at 50 uM preincubated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay (Rvb = 40.4%)2015European journal of medicinal chemistry, Oct-20, Volume: 103Design, synthesis and biological evaluation of tricyclic diterpene derivatives as novel neuroprotective agents against ischemic brain injury.
AID1210107Activity of human recombinant UGT1A7 expressed in insect cells assessed as enzyme mediated glucuronidation at 500 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1325481Antioxidant activity in 10% C57BL/6J mouse plasma assessed as inhibition of SIN-1-derived peroxynitrite-induced lipid oxidation by DPPP-based fluorescence assay2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID1325484Inhibition of 15-LOX-mediated lipid oxidation in 10% C57BL/6J mouse plasma2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID1683015Glutathione peroxidase-like catalytic antioxidant activity in pH 7 phosphate buffer assessed as catalytic reduction of H2O2 by measuring initial velocity at 0.2 mM and 25 degreeC using reduced DTT as di-thiol co-substrate in presence of NADPH by UV absorb
AID276888Hydroxyl radical scavenging activity by ESR spin-trapping method2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Hydroxyl radical scavenging by edaravone derivatives: Efficient scavenging by 3-methyl-1-(pyridin-2-yl)-5-pyrazolone with an intramolecular base.
AID1210161Drug metabolism in human liver microsomes assessed as intrinsic clearance for drug glucuronidation per mg tissue in presence of BSA by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1775905Neuroprotective activity in mouse model of transient middle cerebral artery occlusion-induced cerebral ischemia-reperfusion injury assessed as reduction in infarct volume at 1 mg/kg, iv treated for 3 hrs after onset of reperfusion by TTC staining based as2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.
AID412359Lipophilicity, neutral log P of the compound2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Edaravone derivatives containing NO-donor functions.
AID1210145Drug metabolism in human kidney microsomes assessed as drug glucuronidation in presence of 5 to 35 uM androsterone by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID283749Antioxidant effect against hydrogen peroxide-induced impairment in PC12 cells assessed as cell viability at 10 uM by MTT assay relative to control2007Journal of natural products, Apr, Volume: 70, Issue:4
Mixed lignan-neolignans from Tarenna attenuata.
AID1071848Antioxidant activity assessed as t-butylhyroperoxide-induced alkylperoxyl radical scavenging activity by ESR spin trapping method relative to CYPMPO2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID768377In vivo neuroprotective activity in Sprague-Dawley rat transient middle cerebral artery occlusion model assessed as reduction of brain-water content at 6 mg/kg, iv measured 24 hrs post reperfusion2013European journal of medicinal chemistry, Sep, Volume: 67Coumarin derivatives protect against ischemic brain injury in rats.
AID600288Vasorelaxant activity in rat aortic ring assessed as inhibition of phenylephrine-induced contraction2009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Synthesis, biological evaluation of prenylflavonoids as vasorelaxant and neuroprotective agents.
AID1240303Neuroprotective activity against H2O2-induce cell damage in rat PC12 cells assessed as cell viability at 10 uM preincubated for 1 hr followed by H2O2 induction measured after 3 hrs by MTT assay in presence of NBP (Rvb = 50.85%)2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Novel hybrids of 3-n-butylphthalide and edaravone: Design, synthesis and evaluations as potential anti-ischemic stroke agents.
AID1055904Cytotoxicity against human NCI-H157 cells at 10 uM after 24 hrs by sulforhodamine B assay2013European journal of medicinal chemistry, , Volume: 70Identification of sulfonic acids as efficient ecto-5'-nucleotidase inhibitors.
AID499980Neuroprotective activity in rat PC12 cells assessed as protection against H2O2-induced cell damage at 25 ug/ml after 1 hr by MTT assay relative to control2010Journal of natural products, Aug-27, Volume: 73, Issue:8
Neuroprotective xanthone glycosides from Swertia punicea.
AID1210157Drug metabolism in human liver microsomes assessed as drug glucuronidation per mg tissue in absence of BSA by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1071851Antioxidant activity assessed as H2O2-induced hydroxyl radical scavenging activity by ESR spin trapping method relative to CYPMPO2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID768379In vivo neuroprotective activity in Sprague-Dawley rat transient middle cerebral artery occlusion model assessed as reduction of infarct size at 6 mg/kg, iv measured 24 hrs post reperfusion by TTC staining assay relative to vehicle-treated control2013European journal of medicinal chemistry, Sep, Volume: 67Coumarin derivatives protect against ischemic brain injury in rats.
AID1264255Anti-ischemic activity in Sprague-Dawley rat transient middle cerebral artery occlusion model assessed as reduction in neurological deficit at 3 mg/kg, iv administered for 2 to 6 hrs post middle cerebral artery occlusion measured at 24 hrs2015European journal of medicinal chemistry, Oct-20, Volume: 103Design, synthesis and biological evaluation of tricyclic diterpene derivatives as novel neuroprotective agents against ischemic brain injury.
AID1210125Activity of human recombinant UGT1A6 expressed in insect cells assessed as intrinsic clearance for enzyme mediated glucuronidation per mg protein by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1210129Activity of human recombinant UGT1A9 expressed in insect cells assessed as enzyme mediated glucuronidation by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1210144Drug metabolism in human liver microsomes assessed as drug glucuronidation in presence of 5 to 35 uM androsterone by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1437170Inhibition of recombinant human MAO-B at 10 uM using kynuramine as substrate after 30 mins by fluorescence assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's therapy.
AID85745The concentration producing 50% protection against L-HCA-mediated neurotoxicity in HT-22 hippocampal cell line.2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
New quinolinic derivatives as centrally active antioxidants.
AID1325482Antioxidant activity in 10% C57BL/6J mouse plasma assessed as inhibition of NaOCl-induced lipid oxidation by DPPP-based fluorescence assay2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID1775909Neuroprotective activity in mouse model of transient middle cerebral artery occlusion-induced cerebral ischemia-reperfusion injury assessed as reduction neurological score at 0.3 mg/kg, iv treated for 3 hrs after onset of reperfusion by TTC staining based2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.
AID698743Inhibition of adenosine diphosphate-induced platelet aggregation in rabbit platelet rich plasma at 0.1 mM by Born's turbidimetric method2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of a potential anti-ischemic stroke agent: 3-pentylbenzo[c]thiophen-1(3H)-one.
AID698770Antithrombotic activity in Sprague-Dawley rat arteriovenous shunt model assessed as reduction of thrombus wet weight at 3 mg/kg, po qd for 5 consecutive days2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of a potential anti-ischemic stroke agent: 3-pentylbenzo[c]thiophen-1(3H)-one.
AID1891101Neuroprotective activity against SNP induced rat PC-12 cells assessed as increase in cell viability at 10 uM preincubated for 2 hrs followed by SNP stimulation for 24 hrs by MTT assay relative to control2022European journal of medicinal chemistry, Jun-05, Volume: 236Synthesis and biological evaluation of 1,2,4-triazole derivatives as potential Nrf2 activators for the treatment of cerebral ischemic injury.
AID1071845Antioxidant activity assessed as H2O2-induced hydroxyl radical scavenging activity by ESR spin trapping method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1775908Neuroprotective activity in mouse model of transient middle cerebral artery occlusion-induced cerebral ischemia-reperfusion injury assessed as reduction neurological score at 1 mg/kg, iv treated for 3 hrs after onset of reperfusion by TTC staining based a2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.
AID349363Neuroprotective effect against H202-induced Sprague-Dawley rat cortical neuron injury assessed as cell viability at 1 mM treated 30 mins before H202 challenge measured after 24 hrs by MTT assay relative to control2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Antioxidative and thrombolytic TMP nitrone for treatment of ischemic stroke.
AID1240300Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of arachidonic acid-induced platelet aggregation at 0.1 mM preincubated for 5 mins followed by arachidonic acid addition measured after 5 mins by Born's turbidimetric method in pr2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Novel hybrids of 3-n-butylphthalide and edaravone: Design, synthesis and evaluations as potential anti-ischemic stroke agents.
AID700914Lipophilicity, log P of the compound in octanol-buffer at pH 7 by HPLC analysis2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Synthesis physicochemical profile and PAMPA study of new NO-donor edaravone co-drugs.
AID1210128Activity of human recombinant UGT1A7 expressed in insect cells assessed as intrinsic clearance for enzyme mediated glucuronidation per mg protein by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1294863Cytotoxicity against human A549 cells assessed as inhibition of cell viability at 25 uM after 48 hrs by MTT assay relative to control2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Synthesis, molecular properties prediction and anticancer, antioxidant evaluation of new edaravone derivatives.
AID1439605Cytoprotective activity against H2O2-induced oxidative damage in rat PC12 cells assessed as necrotic cells at 10 uM preincubated for 24 hrs followed by H2O2 addition measured after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric m2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Novel antioxidants' synthesis and their anti-oxidative activity through activating Nrf2 signaling pathway.
AID298289Hydroxy radical scavenging activity by ESR spin-trapping method2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
New series of antiprion compounds: pyrazolone derivatives have the potent activity of inhibiting protease-resistant prion protein accumulation.
AID700909Half life in Wistar rat liver homogenate at 200 uM by RP-HPLC analysis2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Synthesis physicochemical profile and PAMPA study of new NO-donor edaravone co-drugs.
AID1609879Neuroprotective activity against H2O2-induced cell damage in human SH-SY5Y cells assessed as increase in cell viability preincubated for 24 hrs followed by H2O2 addition and measured after 4 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Design, synthesis and biological evaluation of cinnamic acid derivatives with synergetic neuroprotection and angiogenesis effect.
AID181671Compound tested to inhibit (LPO) lipid peroxidation was determined in rat brain microsomes2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Phenolic thiazoles as novel orally-active neuroprotective agents.
AID1210115Activity of human recombinant UGT1A7 expressed in insect cells assessed as enzyme mediated glucuronidation at 12.5 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1294862Cytotoxicity against human PC3 cells assessed as inhibition of cell viability at 25 uM after 48 hrs by MTT assay relative to control2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Synthesis, molecular properties prediction and anticancer, antioxidant evaluation of new edaravone derivatives.
AID1210146Drug metabolism in human liver microsomes assessed as drug glucuronidation in presence of 50 estradiol by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1210158Drug metabolism in human liver microsomes assessed as intrinsic clearance for drug glucuronidation per mg tissue in absence of BSA by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID283747Antioxidant effect against hydrogen peroxide-induced impairment in PC12 cells assessed as cell viability at 0.4 uM by MTT assay relative to control2007Journal of natural products, Apr, Volume: 70, Issue:4
Mixed lignan-neolignans from Tarenna attenuata.
AID1071844Antioxidant activity assessed as riboflavin/EDTA-induced superoxide anion radical scavenging activity by ESR spin trapping method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID698763Anticerebral ischemic activity in Sprague-Dawley rat middle cerebral artery occlusion model assessed as reduction in neurological deficit score at 3 mg/kg, ig for 7 consecutive days by Longa's method2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of a potential anti-ischemic stroke agent: 3-pentylbenzo[c]thiophen-1(3H)-one.
AID1210133Activity of human recombinant UGT2B7 expressed in insect cells assessed as enzyme mediated glucuronidation per mg protein by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID698768Antioxidant activity in rat PC12 cells assessed as inhibition of hydrogen peroxide induced cytotoxicity at 10 uM treated for 2 hrs prior to H2O2 challenge measured after 1 hr by MTT assay (Rvb = 52.45%)2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of a potential anti-ischemic stroke agent: 3-pentylbenzo[c]thiophen-1(3H)-one.
AID1668118Inhibition of lipid peroxidation2020Bioorganic & medicinal chemistry, 05-15, Volume: 28, Issue:10
Chemical reactivity and uses of 1-phenyl-3-methyl-5-pyrazolone (PMP), also known as edaravone.
AID1325486Antioxidant activity in 10% C57BL/6J mouse plasma assessed as inhibition of NpEP-derived singlet oxygen-induced lipid oxidation by DPPP-based fluorescence assay2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID1500523Antioxidant activity assessed as inhibition of DPPH radical at 100 uM incubated for 20 mins measured for 60 mins relative to control2017European journal of medicinal chemistry, Sep-29, Volume: 138Structure-activity relations of rosmarinic acid derivatives for the amyloid β aggregation inhibition and antioxidant properties.
AID698778Inhibition of arachidonic acid-induced platelet aggregation in rabbit platelet rich plasma by Born's turbidimetric method2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of a potential anti-ischemic stroke agent: 3-pentylbenzo[c]thiophen-1(3H)-one.
AID228894Effect to inhibit MPTP mediated dopamine loss was determined in rodent; ND=No data2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Phenolic thiazoles as novel orally-active neuroprotective agents.
AID1210135Activity of human recombinant UGT2B17 expressed in insect cells assessed as enzyme mediated glucuronidation by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1210143Drug metabolism in human kidney microsomes assessed as drug glucuronidation in presence of 200 to 100 uM naloxone by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1500524Antioxidant activity assessed as inhibition of DPPH radical at 500 uM incubated for 20 mins measured for 60 mins relative to control2017European journal of medicinal chemistry, Sep-29, Volume: 138Structure-activity relations of rosmarinic acid derivatives for the amyloid β aggregation inhibition and antioxidant properties.
AID85746The concentration producing 50% toxicity in HT-22 hippocampal cell line.2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
New quinolinic derivatives as centrally active antioxidants.
AID698759Anticerebral ischemic activity in Sprague-Dawley rat middle cerebral artery occlusion model assessed as reduction in infarct size in brain at 3 mg/kg, ig for 7 consecutive days by TTC assay2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of a potential anti-ischemic stroke agent: 3-pentylbenzo[c]thiophen-1(3H)-one.
AID412353Lipophilicity, ionic log P by shake flask method2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Edaravone derivatives containing NO-donor functions.
AID1325479Antioxidant activity assessed as inhibition of AAPH-derived peroxyl radicals-induced PGR consumption2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID13254871-octanol-water partition coefficient, log P of the compound2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID1210119Activity of human recombinant UGT1A4 expressed in insect cells assessed as enzyme mediated glucuronidation at 500 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1264238Neuroprotective activity against oxygen-glucose deprivation-induced neuronal cell death in Sprague-Dawley rat CGN cells assessed as cell viability at 50 uM preincubated for 24 hrs followed by induction of oxygen-glucose deprivation measured after 24 hrs b2015European journal of medicinal chemistry, Oct-20, Volume: 103Design, synthesis and biological evaluation of tricyclic diterpene derivatives as novel neuroprotective agents against ischemic brain injury.
AID1265941Inhibition of N-alpha-biotinyl-amyloid beta (1 to 42 residues) (unknown origin) oligomerization incubated for 1 hr by sandwich biotin-avidin assay2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Diversification of edaravone via palladium-catalyzed hydrazine cross-coupling: Applications against protein misfolding and oligomerization of beta-amyloid.
AID1348581Antioxidant activity assessed as free radical scavenging activity at 25 mg/ml by ESR method2018European journal of medicinal chemistry, Jan-01, Volume: 143Pyrano[3,2-a]carbazole alkaloids as effective agents against ischemic stroke in vitro and in vivo.
AID698749Antioxidant activity in Sprague-Dawley rat middle cerebral artery occlusion model assessed as increase in superoxide dismutase activity at 3 mg/kg, ig for 7 consecutive days2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of a potential anti-ischemic stroke agent: 3-pentylbenzo[c]thiophen-1(3H)-one.
AID1210162Activity of human recombinant UGT1A9 expressed in insect cells assessed as enzyme mediated glucuronidation at 12.5 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1264259Antioxidant activity in Sprague-Dawley rat transient middle cerebral artery occlusion model assessed as reduction in SOD level in ipsilateral cortex at 3 mg/kg, iv measured at 24 hrs post middle cerebral artery occlusion2015European journal of medicinal chemistry, Oct-20, Volume: 103Design, synthesis and biological evaluation of tricyclic diterpene derivatives as novel neuroprotective agents against ischemic brain injury.
AID1265940Inhibition of amyloid beta (1 to 40 residues) (unknown origin) aggregation at 25 uM incubated for 72 hrs by Thioflavin T assay2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Diversification of edaravone via palladium-catalyzed hydrazine cross-coupling: Applications against protein misfolding and oligomerization of beta-amyloid.
AID1210159Drug metabolism in human liver microsomes assessed as drug glucuronidation in presence of BSA by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1683017Glutathione peroxidase-like catalytic anti-lipid peroxidation activity assessed as inhibition of AAPH-induced lipid peroxidation incubated for 3 hrs in presence of (+/-)-trans-5-Hydroxy-1,2-diselenan-4-yl dodecanoate using soybean lecithin/cholesterol-lip
AID1210130Activity of human recombinant UGT1A9 expressed in insect cells assessed as enzyme mediated glucuronidation per mg protein by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID600292Vasorelaxant activity in rat aortic ring assessed as inhibition of phenylephrine-induced contraction relative to control2009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Synthesis, biological evaluation of prenylflavonoids as vasorelaxant and neuroprotective agents.
AID700915Permeability of the compound by PAMPA-HDM method2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Synthesis physicochemical profile and PAMPA study of new NO-donor edaravone co-drugs.
AID1055903Cytotoxicity against HCEC after 24 hrs by sulforhodamine B assay2013European journal of medicinal chemistry, , Volume: 70Identification of sulfonic acids as efficient ecto-5'-nucleotidase inhibitors.
AID1210151Drug metabolism in human kidney microsomes assessed as drug glucuronidation per mg tissue in presence of BSA by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID349359Antioxidant activity assessed as inhibition of ROS-induced linoleic acid peroxidation at 1 mM after 15 mins at 100 degC by modified TBARS assay relative to control2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Antioxidative and thrombolytic TMP nitrone for treatment of ischemic stroke.
AID1055907Inhibition of human recombinant ecto-5'-nucleotidase expressed in african green monkey COS7 cells using adenosine monophosphate as substrate at 1 mM preincubated for 10 mins before substrate addition measured after 10 mins by capillary electrophoresis2013European journal of medicinal chemistry, , Volume: 70Identification of sulfonic acids as efficient ecto-5'-nucleotidase inhibitors.
AID1179806Antioxidant activity assessed as reduction of Cu2+ to Cu+ after 3 mins by PAO-SO method2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Antioxidant effects of the highly-substituted carbazole alkaloids and their related carbazoles.
AID1240302Neuroprotective activity against H2O2-induce cell damage in rat PC12 cells assessed as cell viability at 10 uM preincubated for 1 hr followed by H2O2 induction measured after 3 hrs by MTT assay (Rvb = 50.85%)2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Novel hybrids of 3-n-butylphthalide and edaravone: Design, synthesis and evaluations as potential anti-ischemic stroke agents.
AID1210123Activity of human recombinant UGT1A6 expressed in insect cells assessed as enzyme mediated glucuronidation by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1775870Neuroprotective activity against oxygen glucose deprivation/reperfusion-induced cell death in human SH-SY5Y cells assessed as cell viability at 3 uM preincubated for 8 hrs followed by OGD and reperfusion for 12 hrs by CCK8 assay relative to control2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.
AID140764Percent survival of NMRI mice after 5 hours of intraperitoneal administration of 150 mg/kg of compound.2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
New quinolinic derivatives as centrally active antioxidants.
AID1210112Activity of human recombinant UGT2B7 expressed in insect cells assessed as enzyme mediated glucuronidation at 500 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID698742Anticoagulant activity in rabbit plasma assessed as length of activated partial thromboplastin time2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of a potential anti-ischemic stroke agent: 3-pentylbenzo[c]thiophen-1(3H)-one.
AID1891148Neuroprotective activity in Sprague-Dawley rat model of middle cerebral artery occlusion-induced ischemia-reperfusion injury assessed as decrease in cerebral infarct volume at 5 mg/kg, ip preincubated for 1 hrs followed by MCAO operation and further incub2022European journal of medicinal chemistry, Jun-05, Volume: 236Synthesis and biological evaluation of 1,2,4-triazole derivatives as potential Nrf2 activators for the treatment of cerebral ischemic injury.
AID298288Antiprion activity in F3 cells assessed as inhibition of protease-resistant prion protein accumulation2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
New series of antiprion compounds: pyrazolone derivatives have the potent activity of inhibiting protease-resistant prion protein accumulation.
AID1348565Neuroprotective activity against H2O2-induced damage in Sprague-Dawley rat primary cortical neurons assessed as cell viability at 10 uM after 24 hrs by MTT assay (Rvb = 70 +/- 2.6%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Pyrano[3,2-a]carbazole alkaloids as effective agents against ischemic stroke in vitro and in vivo.
AID1439606Cytoprotective activity against H2O2-induced oxidative damage in rat PC12 cells assessed as viable cells at 10 uM preincubated for 24 hrs followed by H2O2 addition measured after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric met2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Novel antioxidants' synthesis and their anti-oxidative activity through activating Nrf2 signaling pathway.
AID1210139Activity of human recombinant UGT2B17 expressed in insect cells assessed as enzyme mediated glucuronidation in presence of 5 to 35 uM androsterone by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1210114Activity of human recombinant UGT2B17 expressed in insect cells assessed as enzyme mediated glucuronidation at 500 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1201923Neuroprotective activity in rat PC12 cells assessed as decrease in 6-OHDA-induced apoptosis at 200 uM incubated for 6 hrs prior to 6-OHDA challenge measured after 24 hrs by annexin V/propidium iodide staining-based fluorescence microscopic analysis2015European journal of medicinal chemistry, May-05, Volume: 95Synthetic phenylethanoid glycoside derivatives as potent neuroprotective agents.
AID1504804Cytoprotection against H2O2-induced cell injury in rat PC12 cells assessed as increase in cell viability at 20 uM preincubated for 12 hrs followed by H2O2 addition measured after 12 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis, biological evaluation and structure-activity relationship studies of hederacolchiside E and its derivatives as potential anti-Alzheimer agents.
AID1854711Neuroprotective activity against in OGD/R-induced mouse BV-2 cell injury assessed as cell viability at 1 uM measured after 24 hrs by MTT assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment.
AID1210138Activity of human recombinant UGT1A1 expressed in insect cells assessed as enzyme mediated glucuronidation in presence of 10 to 50 uM estradiol by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID600290Neuroprotective activity against oxygen-glucose deprivation-induced cell injury in rat PC12 cells assessed as cell viability at 30 uM2009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Synthesis, biological evaluation of prenylflavonoids as vasorelaxant and neuroprotective agents.
AID1240297Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation at 0.1 mM preincubated for 5 mins followed by ADP addition measured after 5 mins by Born's turbidimetric method in presence of NBP relative to 2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Novel hybrids of 3-n-butylphthalide and edaravone: Design, synthesis and evaluations as potential anti-ischemic stroke agents.
AID1055906Inhibition of rat recombinant ecto-5'-nucleotidase expressed in african green monkey COS7 cells using adenosine monophosphate as substrate at 1 mM preincubated for 10 mins before substrate addition measured after 10 mins by capillary electrophoresis2013European journal of medicinal chemistry, , Volume: 70Identification of sulfonic acids as efficient ecto-5'-nucleotidase inhibitors.
AID1264258Antioxidant activity in Sprague-Dawley rat transient middle cerebral artery occlusion model assessed as reduction in GSH level in ipsilateral cortex at 3 mg/kg, iv measured at 24 hrs post middle cerebral artery occlusion2015European journal of medicinal chemistry, Oct-20, Volume: 103Design, synthesis and biological evaluation of tricyclic diterpene derivatives as novel neuroprotective agents against ischemic brain injury.
AID700907Stability in 0.1 M HCl/MeOH 60/40 (v/v) mixture by RP-HPLC analysis2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Synthesis physicochemical profile and PAMPA study of new NO-donor edaravone co-drugs.
AID1210120Activity of human recombinant UGT1A1 expressed in insect cells assessed as enzyme mediated glucuronidation by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID698767Antioxidant activity in rat PC12 cells assessed as inhibition of hydroxyl radical-induced cytotoxicity at 10 uM treated for 2 hrs prior to H2O2/Fe+ challenge measured after 1 hr by MTT assay (Rvb = 61.95%)2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of a potential anti-ischemic stroke agent: 3-pentylbenzo[c]thiophen-1(3H)-one.
AID1240296Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation at 0.1 mM preincubated for 5 mins followed by ADP addition measured after 5 mins by Born's turbidimetric method relative to control2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Novel hybrids of 3-n-butylphthalide and edaravone: Design, synthesis and evaluations as potential anti-ischemic stroke agents.
AID1437167Inhibition of self-induced Amyloid beta (1 to 42) (unknown origin) aggregation at 25 uM after 24 hrs by thioflavin T-based fluorometric assay relative to control2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's therapy.
AID1210156Drug metabolism in human liver microsomes assessed as drug glucuronidation in absence of BSA by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1210131Activity of human recombinant UGT1A9 expressed in insect cells assessed as intrinsic clearance for enzyme mediated glucuronidation per mg protein by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID349365Inhibition of ADP-induced New Zealand rabbit platelet aggregation at 2 mM treated for 1 min prior to ADP challenge by turbidimetric method relative to control2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Antioxidative and thrombolytic TMP nitrone for treatment of ischemic stroke.
AID412358Dissociation constant, pKa by potentiometric titration2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Edaravone derivatives containing NO-donor functions.
AID1348568Neuroprotective activity against H2O2-induced damage in Sprague-Dawley rat primary cortical neurons assessed as cell viability at 50 uM after 24 hrs by MTT assay (Rvb = 70 +/- 2.6%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Pyrano[3,2-a]carbazole alkaloids as effective agents against ischemic stroke in vitro and in vivo.
AID1071837Antioxidant activity assessed as hydroxyl radical scavenging activity2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1071843Antioxidant activity assessed as AAPH-induced alkoxyl radical scavenging activity by ESR spin trapping method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID412355Antioxidant activity against CuSO4-induced LDL oxidation in human assessed as increase the lag time of the oxidation at 10 uM by TBARS assay2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Edaravone derivatives containing NO-donor functions.
AID1210106Activity of human recombinant UGT1A6 expressed in insect cells assessed as enzyme mediated glucuronidation at 500 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1210111Activity of human recombinant UGT2B4 expressed in insect cells assessed as enzyme mediated glucuronidation at 500 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1179805Antioxidant activity assessed as ABTS+ radical scavenging capacity after 16 hrs by UV spectrophotometry2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Antioxidant effects of the highly-substituted carbazole alkaloids and their related carbazoles.
AID1210124Activity of human recombinant UGT1A6 expressed in insect cells assessed as enzyme mediated glucuronidation per mg protein by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1439604Cytoprotective activity against H2O2-induced oxidative damage in rat PC12 cells assessed as late apoptotic cells at 10 uM preincubated for 24 hrs followed by annexin V-FITC/propidium iodide staining-based flow cytometric method (Rvb = 10.7%)2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Novel antioxidants' synthesis and their anti-oxidative activity through activating Nrf2 signaling pathway.
AID1325477Antioxidant activity in 10% C57BL/6J mouse plasma assessed as inhibition of AAPH-derived peroxyl radicals-induced pyranine consumption at 50 uM2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID1071846Antioxidant activity assessed as rosebengal-induced singlet oxygen radical scavenging activity by ESR spin trapping method relative to 4-OH-TEMP2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1210126Activity of human recombinant UGT1A7 expressed in insect cells assessed as enzyme mediated glucuronidation by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1210148Drug metabolism in human kidney microsomes assessed as drug glucuronidation per mg tissue in absence of BSA by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1437172Selectivity index, ratio of IC50 for recombinant human MAO-A to IC50 for recombinant human MAO-B2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's therapy.
AID1240308Antioxidant activity in rat PC12 cells assessed as reduction of H2O2/Fe2+-mediated hydroxyl radical formation at 10 uM preincubated for 1 hr followed by H2O2/Fe2+ addition by Griess assay in presence of NBP2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Novel hybrids of 3-n-butylphthalide and edaravone: Design, synthesis and evaluations as potential anti-ischemic stroke agents.
AID1210142Drug metabolism in human liver microsomes assessed as drug glucuronidation in presence of 200 to 100 uM naloxone by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1071849Antioxidant activity assessed as AAPH-induced alkoxyl radical scavenging activity by ESR spin trapping method relative to CYPMPO2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1325480Antioxidant activity in 10% C57BL/6J mouse plasma assessed as inhibition of AAPH-derived peroxyl radicals-induced lipid hydroperoxide formation by DPPP-based fluorescence assay2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID1210116Activity of human recombinant UGT2B17 expressed in insect cells assessed as enzyme mediated glucuronidation at 12.5 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1775904Neuroprotective activity in mouse model of transient middle cerebral artery occlusion-induced cerebral ischemia-reperfusion injury assessed as reduction in infarct volume at 3 mg/kg, iv treated for 3 hrs after onset of reperfusion by TTC staining based as2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.
AID1437171Inhibition of recombinant human MAO-A at 10 uM using kynuramine as substrate after 30 mins by fluorescence assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's therapy.
AID1240310Antioxidant activity in rat PC12 cells assessed as reduction of NADH-mediated superoxide anion radical formation at 10 uM preincubated for 1 hr followed by NADH addition by NBT assay2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Novel hybrids of 3-n-butylphthalide and edaravone: Design, synthesis and evaluations as potential anti-ischemic stroke agents.
AID1401200Antiischemic stroke activity in Sprague-Dawley rat middle cerebral artery occlusion-induced ischemia-reperfusion injury model assessed as decrease in neurological score at 0.2 mg/kg, icv as nanoparticle measured after 72 hrs by Longa's method2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis, and evaluation of NDGA analogues as potential anti-ischemic stroke agents.
AID85744The minimum tolerated concentration by MTT reduction assay in HT-22 hippocampal cell line.2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
New quinolinic derivatives as centrally active antioxidants.
AID1210147Drug metabolism in human kidney microsomes assessed as drug glucuronidation in absence of BSA by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1071840Antioxidant activity assessed as rosebengal-induced singlet oxygen radical scavenging activity by ESR spin trapping method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1210150Drug metabolism in human kidney microsomes assessed as drug glucuronidation in presence of BSA by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID283751Antioxidant effect assessed as DPPH radical scavenging activity2007Journal of natural products, Apr, Volume: 70, Issue:4
Mixed lignan-neolignans from Tarenna attenuata.
AID211833Ability to inhibit KCN induced toxicity in mice 1 hr before the oral administration of the compound; NS= non significant effect when tested at 30 mg/kg (po)2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Phenolic thiazoles as novel orally-active neuroprotective agents.
AID412357Distribution coefficient, log D at pH 7.4 by shake flask method2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Edaravone derivatives containing NO-donor functions.
AID1240299Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of arachidonic acid-induced platelet aggregation at 0.1 mM preincubated for 5 mins followed by arachidonic acid addition measured after 5 mins by Born's turbidimetric method relat2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Novel hybrids of 3-n-butylphthalide and edaravone: Design, synthesis and evaluations as potential anti-ischemic stroke agents.
AID1055905Cytotoxicity against human NCI-H157 cells at 100 uM after 24 hrs by sulforhodamine B assay2013European journal of medicinal chemistry, , Volume: 70Identification of sulfonic acids as efficient ecto-5'-nucleotidase inhibitors.
AID698757Anticerebral ischemic activity in Sprague-Dawley rat middle cerebral artery occlusion model assessed as reduction of water content in brain at 3 mg/kg, ig for 7 consecutive days2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of a potential anti-ischemic stroke agent: 3-pentylbenzo[c]thiophen-1(3H)-one.
AID1683014Glutathione peroxidase-like catalytic antioxidant activity in pH 7 phosphate buffer assessed as catalytic reduction of H2O2 by measuring initial velocity at 100 uM and 25 degreeC using GSH as mono-thiol co-substrate in presence of NADPH by UV absorbance a
AID298287Antiprion activity in ScN2a cells assessed as inhibition of protease-resistant prion protein accumulation2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
New series of antiprion compounds: pyrazolone derivatives have the potent activity of inhibiting protease-resistant prion protein accumulation.
AID283748Antioxidant effect against hydrogen peroxide-induced impairment in PC12 cells assessed as cell viability at 2 uM by MTT assay relative to control2007Journal of natural products, Apr, Volume: 70, Issue:4
Mixed lignan-neolignans from Tarenna attenuata.
AID232026Safety ratio of MTC to that of PC502000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
New quinolinic derivatives as centrally active antioxidants.
AID1294864Cytotoxicity against HEK293T cells assessed as inhibition of cell viability at 25 uM after 48 hrs by MTT assay relative to control2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Synthesis, molecular properties prediction and anticancer, antioxidant evaluation of new edaravone derivatives.
AID1179807Cytotoxicity against human HCT116 cells assessed as reduction cell viability at 100 uM after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Antioxidant effects of the highly-substituted carbazole alkaloids and their related carbazoles.
AID1325476Antioxidant activity assessed as inhibition of Meo-AMVN-derived peroxyl radicals-induced fucoxanthin consumption at 50 uM2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID1210113Activity of human recombinant UGT2B15 expressed in insect cells assessed as enzyme mediated glucuronidation at 500 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1210122Activity of human recombinant UGT1A1 expressed in insect cells assessed as intrinsic clearance for enzyme mediated glucuronidation per mg protein by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1210152Drug metabolism in human kidney microsomes assessed as intrinsic clearance for drug glucuronidation per mg tissue in presence of BSA by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1376810Neuroprotective activity against 12.5 mM glutamate-induced toxicity in rat PC12 cells assessed as cell viability after 24 hrs by MTT assay2017Journal of natural products, 06-23, Volume: 80, Issue:6
Neuroprotective Activity of Cerebrosides from Typhonium giganteum by Regulating Caspase-3 and Bax/Bcl-2 Signaling Pathways in PC12 Cells.
AID1294868Antioxidant activity assessed as DPPH free radical scavenging activity incubated for 30 mins in dark condition by spectrophotometric method2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Synthesis, molecular properties prediction and anticancer, antioxidant evaluation of new edaravone derivatives.
AID1854710Neuroprotective activity against in OGD/R-induced mouse BV-2 cell injury assessed as cell viability at 0.1 uM measured after 24 hrs by MTT assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment.
AID1240311Antioxidant activity in rat PC12 cells assessed as reduction of NADH-mediated superoxide anion radical formation at 10 uM preincubated for 1 hr followed by NADH addition by NBT assay in presence of NBP2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Novel hybrids of 3-n-butylphthalide and edaravone: Design, synthesis and evaluations as potential anti-ischemic stroke agents.
AID1210108Activity of human recombinant UGT1A8 expressed in insect cells assessed as enzyme mediated glucuronidation at 500 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1210109Activity of human recombinant UGT1A9 expressed in insect cells assessed as enzyme mediated glucuronidation at 500 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1179804Antioxidant activity assessed as DPPH radical scavenging capacity after 30 mins by UV spectrophotometry2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Antioxidant effects of the highly-substituted carbazole alkaloids and their related carbazoles.
AID1775907Neuroprotective activity in mouse model of transient middle cerebral artery occlusion-induced cerebral ischemia-reperfusion injury assessed as reduction neurological score at 3 mg/kg, iv treated for 3 hrs after onset of reperfusion by TTC staining based a2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.
AID1071850Antioxidant activity assessed as riboflavin/EDTA-induced superoxide anion radical scavenging activity by ESR spin trapping method relative to CYPMPO2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID349372Neuroprotective effect against middle cerebral artery occlusion-induced focal cerebral ischemia in Sprague-Dawley rat assessed as reduction in infarct area at 62 mg/kg, ip administered 1 hr after MCA occlusion measured after 24 hrs of reperfusion by TTC s2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Antioxidative and thrombolytic TMP nitrone for treatment of ischemic stroke.
AID1210153Cmax in human at 0.5 mg/kg2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1210155Activity of human recombinant UGT1A9 expressed in insect cells assessed as enzyme mediated glucuronidation in presence of 100 to 1000 uM propofol by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1210117Activity of human recombinant UGT1A6 expressed in insect cells assessed as enzyme mediated glucuronidation at 12.5 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1264235Neuroprotective activity against glutamate-induced neuronal cell death in Sprague-Dawley rat CGN cells at 50 uM preincubated for 24 hrs followed by glutamate challenge measured after 24 hrs relative to control2015European journal of medicinal chemistry, Oct-20, Volume: 103Design, synthesis and biological evaluation of tricyclic diterpene derivatives as novel neuroprotective agents against ischemic brain injury.
AID1692584Antioxidant activity assessed as hydroxyl radical scavenging activity incubated for 60 mins in water bath by Fenton reaction-based method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
From Seeds of
AID298291Superoxide dismutase like activity assessed as inhibition of WST1 tetrazolium formation at 1 mM in presence of 2 mM Cu(II)2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
New series of antiprion compounds: pyrazolone derivatives have the potent activity of inhibiting protease-resistant prion protein accumulation.
AID1591948Neuroprotective activity against oxygen-glucose deprivation/reperfusion injury in mouse Neuro2a cells assessed as cell viability at 50 uM added 4 hrs prior to oxygen-glucose deprivation induction by MTT assay (Rvb 61 +/- 5%)
AID1210134Activity of human recombinant UGT2B7 expressed in insect cells assessed as intrinsic clearance for enzyme mediated glucuronidation per mg protein by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID700916Permeability of the compound assessed as membrane retention after 1 to 6 hrs by PAMPA-HDM method relative to control2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Synthesis physicochemical profile and PAMPA study of new NO-donor edaravone co-drugs.
AID698769Antithrombotic activity in Sprague-Dawley rat arteriovenous shunt model assessed as reduction of thrombus dry weight at 3 mg/kg, po qd for 5 consecutive days2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of a potential anti-ischemic stroke agent: 3-pentylbenzo[c]thiophen-1(3H)-one.
AID1439603Cytoprotective activity against H2O2-induced oxidative damage in rat PC12 cells assessed as early apoptotic cells at 10 uM preincubated for 24 hrs followed by H2O2 addition measured after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytom2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Novel antioxidants' synthesis and their anti-oxidative activity through activating Nrf2 signaling pathway.
AID1325492Plasma concentration in rat cerebral ischemia model at 1.5 to 3 mg/kg administered as infusion2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID1210141Drug metabolism in human kidney microsomes assessed as drug glucuronidation in presence of 100 to 1000 uM propofol by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1891102Neuroprotective activity against SNP induced rat PC-12 cells assessed as increase in cell viability at 5 uM preincubated for 2 hrs followed by SNP stimulation for 24 hrs by MTT assay relative to control2022European journal of medicinal chemistry, Jun-05, Volume: 236Synthesis and biological evaluation of 1,2,4-triazole derivatives as potential Nrf2 activators for the treatment of cerebral ischemic injury.
AID698745Antioxidant activity in Sprague-Dawley rat middle cerebral artery occlusion model assessed as decrease in malondialdehyde level in brain at 3 mg/kg, ig for 7 consecutive days2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of a potential anti-ischemic stroke agent: 3-pentylbenzo[c]thiophen-1(3H)-one.
AID349360Antioxidant activity assessed as inhibition of ROS-induced linoleic acid peroxidation at 2 mM after 15 mins at 100 degC by modified TBARS assay relative to control2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Antioxidative and thrombolytic TMP nitrone for treatment of ischemic stroke.
AID1071838Antioxidant activity assessed as DMPO/H2O2-induced hydroxyl radical scavenging activity by fast-flow EPR technique2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID698779Inhibition of adenosine diphosphate-induced platelet aggregation in rabbit platelet rich plasma by Born's turbidimetric method2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of a potential anti-ischemic stroke agent: 3-pentylbenzo[c]thiophen-1(3H)-one.
AID1437173Antioxidant activity assessed as trolox equivalent of AAPH radical scavenging activity at 1 uM preincubated for 15 mins followed by AAPH addition measured every min for 90 mins by ORAC-FL assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's therapy.
AID1210104Activity of human recombinant UGT1A1 expressed in insect cells assessed as enzyme mediated glucuronidation at 500 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1668119Antioxidant activity assessed as copper-chelating scavenging activity2020Bioorganic & medicinal chemistry, 05-15, Volume: 28, Issue:10
Chemical reactivity and uses of 1-phenyl-3-methyl-5-pyrazolone (PMP), also known as edaravone.
AID1071842Antioxidant activity assessed as t-butylhyroperoxide-induced alkylperoxyl radical scavenging activity by ESR spin trapping method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1854712Neuroprotective activity against in OGD/R-induced mouse BV-2 cell injury assessed as cell viability at 10 uM measured after 24 hrs by MTT assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment.
AID1210140Drug metabolism in human liver microsomes assessed as drug glucuronidation in presence of 100 to 1000 uM propofol by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID283750Antioxidant effect against hydrogen peroxide-induced impairment in PC12 cells assessed as cell viability at 50 uM by MTT assay relative to control2007Journal of natural products, Apr, Volume: 70, Issue:4
Mixed lignan-neolignans from Tarenna attenuata.
AID698754Antioxidant activity in Sprague-Dawley rat middle cerebral artery occlusion model assessed as increase in glutathione level in brain at 3 mg/kg, ig for 7 consecutive days2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of a potential anti-ischemic stroke agent: 3-pentylbenzo[c]thiophen-1(3H)-one.
AID1210136Activity of human recombinant UGT2B17 expressed in insect cells assessed as enzyme mediated glucuronidation per mg protein by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1071847Antioxidant activity assessed as DMSO/H2O2-induced methyl radical scavenging activity by ESR spin trapping method relative to DMPO2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID298290Superoxide dismutase like activity assessed as inhibition of WST1 tetrazolium formation at 1 mM2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
New series of antiprion compounds: pyrazolone derivatives have the potent activity of inhibiting protease-resistant prion protein accumulation.
AID1210127Activity of human recombinant UGT1A7 expressed in insect cells assessed as enzyme mediated glucuronidation per mg protein by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID700903Stability in human serum at 250 uM by RP-HPLC analysis2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Synthesis physicochemical profile and PAMPA study of new NO-donor edaravone co-drugs.
AID1210154Activity of human recombinant UGT2B7 expressed in insect cells assessed as enzyme mediated glucuronidation in presence of 200 to 100 uM naloxone by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1775873Cytotoxicity against human SH-SY5Y cells assessed as cell viability under normoxic/normal sugar condition at 10 to 30 uM by CCK-8 assay2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.
AID1265939Inhibition of amyloid beta (1 to 40 residues) (unknown origin) aggregation incubated for 72 hrs by Thioflavin T assay2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Diversification of edaravone via palladium-catalyzed hydrazine cross-coupling: Applications against protein misfolding and oligomerization of beta-amyloid.
AID700904Stability in 5% DMSO/0.1 M KCl by RP-HPLC analysis2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Synthesis physicochemical profile and PAMPA study of new NO-donor edaravone co-drugs.
AID1210121Activity of human recombinant UGT1A1 expressed in insect cells assessed as enzyme mediated glucuronidation per mg protein by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID349364Neuroprotective effect against H202-induced Sprague-Dawley rat cortical neuron injury assessed as cell viability at 100 uM treated 30 mins before H202 challenge measured after 24 hrs by MTT assay2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Antioxidative and thrombolytic TMP nitrone for treatment of ischemic stroke.
AID1609880Neuroprotective activity against H2O2-induced cell damage in human HBMEC2 cells assessed as increase in cell viability preincubated for 24 hrs followed by H2O2 addition and measured after 4 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Design, synthesis and biological evaluation of cinnamic acid derivatives with synergetic neuroprotection and angiogenesis effect.
AID1891103Neuroprotective activity against SNP induced rat PC-12 cells assessed as increase in cell viability at 1 uM preincubated for 2 hrs followed by SNP stimulation for 24 hrs by MTT assay relative to control2022European journal of medicinal chemistry, Jun-05, Volume: 236Synthesis and biological evaluation of 1,2,4-triazole derivatives as potential Nrf2 activators for the treatment of cerebral ischemic injury.
AID1210110Activity of human recombinant UGT1A10 expressed in insect cells assessed as enzyme mediated glucuronidation at 500 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID499981Neuroprotective activity in rat PC12 cells assessed as protection against H2O2-induced cell damage at 12.5 ug/ml after 1 hr by MTT assay relative to control2010Journal of natural products, Aug-27, Volume: 73, Issue:8
Neuroprotective xanthone glycosides from Swertia punicea.
AID698744Inhibition of arachidonic acid-induced platelet aggregation in rabbit platelet rich plasma at 0.1 mM by Born's turbidimetric method2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of a potential anti-ischemic stroke agent: 3-pentylbenzo[c]thiophen-1(3H)-one.
AID1071841Antioxidant activity assessed as DMSO/H2O2-induced methyl radical scavenging activity by ESR spin trapping method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1775906Neuroprotective activity in mouse model of transient middle cerebral artery occlusion-induced cerebral ischemia-reperfusion injury assessed as reduction in infarct volume at 0.3 mg/kg, iv treated for 3 hrs after onset of reperfusion by TTC staining based 2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.
AID1210118Activity of human recombinant UGT1A8 expressed in insect cells assessed as enzyme mediated glucuronidation at 12.5 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID1683016Glutathione peroxidase-like catalytic anti-lipid peroxidation activity assessed as inhibition of AAPH-induced lipid peroxidation incubated for 3 hrs using soybean lecithin/cholesterol-liposomes by TBARS assay
AID1210137Activity of human recombinant UGT2B17 expressed in insect cells assessed as intrinsic clearance for enzyme mediated glucuronidation per mg protein by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Glucuronidation of edaravone by human liver and kidney microsomes: biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform.
AID412354Vasodilation activity in Wistar rat aorta assessed as relaxation of phenylephrine-induced contraction2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Edaravone derivatives containing NO-donor functions.
AID139507Body temperature of NMRI mice after 30 minutes of intraperitoneal administration of 150 mg/kg compound.2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
New quinolinic derivatives as centrally active antioxidants.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
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.
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.
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.
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.
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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS 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.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
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.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,093)

TimeframeStudies, This Drug (%)All Drugs %
pre-199029 (2.65)18.7374
1990's37 (3.39)18.2507
2000's315 (28.82)29.6817
2010's474 (43.37)24.3611
2020's238 (21.77)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 77.09

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index77.09 (24.57)
Research Supply Index7.09 (2.92)
Research Growth Index5.43 (4.65)
Search Engine Demand Index136.19 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (77.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials69 (6.12%)5.53%
Reviews86 (7.62%)6.00%
Case Studies34 (3.01%)4.05%
Observational9 (0.80%)0.25%
Other930 (82.45%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (53)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Compound Edaravone Injection for Acute Ischemic Stroke, a Multi-center, Randomized, Double-blind, Parallel, and Active-controlled PhaseⅢTrial [NCT02430350]Phase 31,200 participants (Actual)Interventional2015-05-31Completed
An Observational Trial of Edaravone Dexborneol Combining With Mechanical Thrombectomy in the Treatment of Acute Ischemic Stroke [NCT05121883]200 participants (Anticipated)Observational [Patient Registry]2021-11-01Recruiting
Dose Finding Study of MCI-186 in Acute Ischemic Stroke [NCT03346538]Phase 217 participants (Actual)Interventional2017-11-17Terminated(stopped due to Business objectives have changed.)
Phase I Study of Oral Edaravone in Healthy Adult Males (Single- and Multiple-dose Study) [NCT04481750]Phase 174 participants (Actual)Interventional2018-03-20Completed
Sublingual Y-2(Edaravone And Borneol) Tablet For Acute Ischemic And Hemorrhagic Patients-the SALVAGE Trial [NCT03495206]Phase 124 participants (Anticipated)Interventional2018-10-25Recruiting
Improving Neuroprotective Strategy for Ischemic Stroke With Sufficient Recanalization After Thrombectomy by Edaravone Dexborneol (INSIST-ED): a Prospective, Randomized, Double Blinded, Multi-centre Study [NCT04667637]Phase 2200 participants (Actual)Interventional2021-02-23Completed
Efficacy and Safety of Nerve Growth Factor or Edaravone on Alcohol-induced Brain Injury [NCT03968042]Phase 2150 participants (Anticipated)Interventional2019-06-30Recruiting
An Expanded Controlled Study of MCI-186 for Treatment of Amyotrophic Lateral Sclerosis in Double-Blind, Parallel-Group, Placebo-Controlled Manner (Phase 3) [NCT00424463]Phase 3181 participants (Actual)Interventional2007-01-31Completed
A Phase 1, Randomized, Open-Label, Three-Treatment, Three-Period Crossover Study to Assess Bioequivalence and Safety of TTYP01 Tablets to Radicava® Injection, and Radicava ORS® in Healthy Adult Subjects Under Fasting Conditions [NCT06107205]Phase 130 participants (Anticipated)Interventional2023-09-27Recruiting
A Phase 3b, Multicenter, Randomized, Double-blind Extension Study to Evaluate the Continued Efficacy and Safety of Oral Edaravone Administered for an Additional Period of up to 48 Weeks Following Study MT-1186-A02 in Subjects With Amyotrophic Lateral Scle [NCT05151471]Phase 3202 participants (Actual)Interventional2022-01-11Terminated(stopped due to Futility Analysis of parent study MT-1186-A02 was met.)
A Phase 3b, Multicenter, Randomized, Double-Blind Study to Evaluate Efficacy and Safety of Oral Edaravone Administered for a Period of 48 Weeks in Subjects With Amyotrophic Lateral Sclerosis (ALS) [NCT04569084]Phase 3384 participants (Actual)Interventional2020-11-13Terminated(stopped due to Futility was met.)
Edaravone in the Treatment of Aquaporin-4 Antibody-positive Optic Neuritis [NCT05540262]18 participants (Anticipated)Interventional2022-01-15Recruiting
An Open-Label, Single-Dose Study to Evaluate the Pharmacokinetics of MCI-186 in Subjects With Severe Hepatic Impairment Compared to Subjects With Normal Hepatic Function [NCT03664544]Phase 112 participants (Actual)Interventional2018-11-06Completed
Radicava® (Edaravone) Findings in Biomarkers From ALS (REFINE-ALS) [NCT04259255]300 participants (Anticipated)Observational2019-10-21Active, not recruiting
Treatment of Acute Ischemic STroke With Edaravone Dexborneol Ⅱ (TASTE-2) [NCT05249920]Phase 31,362 participants (Actual)Interventional2022-03-18Completed
Clinical Pharmacology Study of Oral Edaravone in Patients With Amyotrophic Lateral Sclerosis (ALS) [NCT04176224]Phase 19 participants (Actual)Interventional2019-04-17Completed
Clinical Pharmacology Study of Oral Edaravone in Healthy Adult Subjects (Food Effect Study) [NCT05342597]Phase 116 participants (Actual)Interventional2019-06-10Completed
A Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety, Pharmacodynamics and Pharmacokinetics of TW001 in Alzheimer Patients [NCT05323812]Phase 260 participants (Anticipated)Interventional2023-03-01Recruiting
An Exploratory Study of MCI-186 for Treatment of Amyotrophic Lateral Sclerosis (Severity Classification III) in Double-Blind, Parallel-Group, Placebo-Controlled Manner [NCT00415519]Phase 325 participants (Actual)Interventional2006-12-31Completed
Multicenter, Open-label Extension Study Following the Studies MT-1186-A03 or A04 to Evaluate the Safety of Oral Edaravone in Subjects With Amyotrophic Lateral Sclerosis (ALS) [NCT05568615]Phase 315 participants (Actual)Interventional2022-10-26Completed
A Confirmatory Study of MCI-186 for Treatment of Amyotrophic Lateral Sclerosis in Double-blind, Parallel-group, Placebo-controlled Manner. [NCT00330681]Phase 3206 participants (Actual)Interventional2006-05-31Completed
Edaravone-Sodium Ozagrel (Thromboxane A2 Synthase Inhibitor) Comparative Post-Marketing Study on Acute Ischemic Stroke [NCT00200356]Phase 4401 participants (Actual)Interventional2004-08-31Completed
Effects of Edaravone in Patients With Acute Myocardial Infarction [NCT00265239]Phase 4104 participants (Actual)Interventional2001-04-30Completed
A Multicenter, Randomized, Double-blind, Placebo-controlled Phase III Clinical Trial to Evaluate the Efficacy and Safety of Edaravone Dexborneol Sequential Therapy in the Treatment of Patients With Acute Ischemic Stroke [NCT06176781]Phase 3880 participants (Anticipated)Interventional2023-12-28Not yet recruiting
Effectiveness and Safety of Edaravone Dexborneol in Acute Ischemic Stroke: a Multicenter, Prospective, Patient-centered, Real-world Cohort Study [NCT05644223]4,750 participants (Anticipated)Observational [Patient Registry]2023-01-01Recruiting
Study on the Safety, Tolerance and Pharmacokinetics of Single-dose, Increasing and Loading Dose and Maintenance Dose Sequential Intravenous Infusion of Compound Edaravone Injection in Chinese Healthy Volunteers [NCT04219865]Phase 140 participants (Actual)Interventional2019-06-05Completed
Effect of Edaravone on the Ischemia-Reperfusion(I/R) Injury in Kidney Transplantation Patients: A Single-Center, Double-Blinded, Randomised Controlled Trial [NCT02644915]150 participants (Anticipated)Interventional2016-03-31Not yet recruiting
An Experiment to Evaluate the Drug-drug Interaction of Formula Edaravone and Formula 2-Aminoethanesulfonic Acid in Compound Edaravone Injection [NCT04218513]Phase 124 participants (Actual)Interventional2019-05-10Completed
Effect of Edaravone on Radiation-induced Temporal Lobe Necrosis in Patients With Nasopharyngeal Carcinoma After Radiotherapy [NCT01865201]Phase 2154 participants (Actual)Interventional2009-03-31Completed
Treatment Effect of Edaravone in Patients With Amyotrophic Lateral Sclerosis (ALS) in a Representative Iranian Population [NCT03272802]Phase 2/Phase 320 participants (Anticipated)Interventional2017-03-16Active, not recruiting
Protective Effects of Edaravone Dexborneol in Patients With Acute Ischemic Stroke by Improving Ischemic Penumbra and Collateral Circulation of Hypoperfusion Areas [NCT05024526]80 participants (Anticipated)Interventional2021-04-01Recruiting
Clinical Pharmacology Study of Oral Edaravone in Amyotrophic Lateral Sclerosis Patients With Gastrostomy [NCT04254913]Phase 16 participants (Actual)Interventional2020-01-24Completed
Phase 1 Study of Autologous Peripheral Hematopoietic Stem Cell Transplantation in Ischemic Stroke [NCT01518231]Phase 140 participants (Anticipated)Interventional2012-01-31Recruiting
Multicenter Randomized Open-Label Comparison Study on the Efficacy and Safety of Argatroban Monotherapy With Argatroban-Edaravone Combination Therapy [NCT00153946]Phase 4814 participants (Actual)Interventional2004-08-31Completed
A Phase IIa, Multi-centre, Randomised, Double-blind, Placebo Controlled, Clinical Study Investigating the Safety, Tolerability and Pharmacokinetics of MCI-186 in Subjects With Acute Ischemic Stroke [NCT00821821]Phase 236 participants (Actual)Interventional2009-02-28Completed
A Phase 3, Multi-center, Open-label, Safety Extension Study of Oral Edaravone Administered Over 96 Weeks in Subjects With Amyotrophic Lateral Sclerosis (ALS) [NCT04577404]Phase 3124 participants (Actual)Interventional2020-10-29Completed
Safety Study of Oral Edaravone Administered in Subjects With ALS [NCT04165824]Phase 3185 participants (Actual)Interventional2019-11-18Completed
A Randomized, Single-Blind, Placebo-Controlled, Three-Way Crossover Study to Evaluate the Effect of MCI-186 at Therapeutic and Supra-Therapeutic Doses on the QT/QTc Interval in Healthy Subjects [NCT04029090]Phase 127 participants (Actual)Interventional2018-09-18Completed
Mechanism and Early Intervention Research on Acute Lung Injury During Emergence Surgery of Acute Stanford A Aortic Dissection [NCT01894334]220 participants (Anticipated)Interventional2013-04-30Active, not recruiting
A Phase I, Single Center, Randomized, Single-Ascending Dose, Pharmacokinetic and Safety Study (Part A), Bioavailability Comparison Study (Part B) and Food Effect Study (Part C) in Healthy Adult Subjects. [NCT04370431]Phase 172 participants (Actual)Interventional2020-04-24Completed
Compound Edaravone Injection for Acute Ischemic Stroke, a Multi-center, Randomized, Double-blind, Multi-dose, Parallel, and Controlled Phase II Trial [NCT01929096]Phase 2400 participants (Actual)Interventional2013-08-31Completed
Efficacy and Safety of Edaravone Dexborneol in Addition to Standard of Care in Patients With Hypertensive Intracerebral Hemorrhage: a Randomized, Double-Blind, Placebo-Controlled Trial [NCT04714177]Phase 2390 participants (Anticipated)Interventional2021-03-01Not yet recruiting
A Multi-Center, Open-Label, Single-Dose Study to Evaluate the Pharmacokinetics of MCI-186 in Subjects With Mild or Moderate Hepatic Impairment Compared to Subjects With Normal Hepatic Function [NCT03289234]Phase 122 participants (Actual)Interventional2016-11-16Completed
An Open-Label, Single-Dose Study to Evaluate the Pharmacokinetics of MCI-186 in Subjects With Mild or Moderate Renal Impairment Compared to Subjects With Normal Renal Function [NCT03289208]Phase 130 participants (Actual)Interventional2016-10-27Completed
Edaravone Dexborneol for Treatment of Acute Ischemic Stroke With Endovascular Therapy in Extended Time Windows (EXISTENT):a Prospective, Randomized, Open-label, Multi-centre Study [NCT04817527]Phase 2200 participants (Anticipated)Interventional2021-10-01Recruiting
Clinical Pharmacology Study of Oral Edaravone in Healthy Adult Males (Drug Interaction Study and Preliminary Regimen-Finding Study) [NCT04481789]Phase 184 participants (Actual)Interventional2018-10-17Completed
Phase Ⅲ Trial of Compound Edaravone Injection for Treatment of Acute Ischemic Stroke -- a Multi-center, Randomized, Double-blind, Parallel, Multi-doses and Active-controlled Study [NCT04984577]Phase 2240 participants (Anticipated)Interventional2021-09-30Not yet recruiting
Efficacy and Safety Study of MCI-186 for Treatment of the Patients With Amyotrophic Lateral Sclerosis (ALS) 2 [NCT01492686]Phase 3137 participants (Actual)Interventional2011-12-31Completed
The Safety and Effectiveness of Cholinergic Receptor Block Therapy in the Treatment of Amyotrophic Lateral Sclerosis [NCT04391361]Phase 230 participants (Anticipated)Interventional2020-11-01Not yet recruiting
A Phase I, Randomized, Open-Label, Crossover-Design, Single-Dose Study to Investigate the Safety, Tolerability and Comparative Bioavailability of Oral Edaravone Administered Orally and Via a Nasogastric Tube (NGT) in Healthy Adult Subjects [NCT04776135]Phase 136 participants (Actual)Interventional2021-02-26Completed
Effect of Early Versus Late Initiation of Edaravone Dexborneol on Neural Function in Patients With Acute Ischemic Stroke-A Multicenter, Randomized, Double-blind, Placebo-controlled, Trial [NCT05885919]Phase 3212 participants (Anticipated)Interventional2023-07-01Not yet recruiting
Bioequivalence Study of Oral Suspension and Intravenous Formulation of Edaravone in Healthy Adult Subjects [NCT04493281]Phase 142 participants (Actual)Interventional2019-03-22Completed
Effect of Thrombolysis Combined With Edaravone Dexborneol for Acute Ischemic Stroke Patients: a Multicenter, Randomized, Double-Blind, Placebo-Controlled Trial [NCT05035953]Phase 2200 participants (Anticipated)Interventional2021-09-13Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00200356 (10) [back to overview]Barthel Index Score
NCT00200356 (10) [back to overview]NIH Stroke Scale Score at 1 Month
NCT00200356 (10) [back to overview]Modified Rankin Scale Score
NCT00200356 (10) [back to overview]Japan Stroke Scale (Motor Function) Score at 3 Months
NCT00200356 (10) [back to overview]Japan Stroke Scale (Motor Function) Score at 14 Days
NCT00200356 (10) [back to overview]Japan Stroke Scale (Motor Function) Score at 1 Month
NCT00200356 (10) [back to overview]Baseline NIH Stroke Scale Score
NCT00200356 (10) [back to overview]the Rate of Patients With a Modified Rankin Scale Score of 0-1
NCT00200356 (10) [back to overview]NIH Stroke Scale Score at 3 Months
NCT00200356 (10) [back to overview]NIH Stroke Scale Score at 14 Days
NCT00265239 (4) [back to overview]Nonfatal Ischemic Stroke
NCT00265239 (4) [back to overview]Cardiac Death
NCT00265239 (4) [back to overview]Nonfatal Myocardial Reinfarction
NCT00265239 (4) [back to overview]Refractory Angina Pectoris
NCT00330681 (9) [back to overview]Change From Baseline in % Forced Vital Capacity (%FVC) in Full Analysis Set (FAS) Population at 24 Weeks
NCT00330681 (9) [back to overview]Percentage of Participants With Laboratory Tests for Which the Incidence of Abnormal Changes Was 5% or Higher in Either Group
NCT00330681 (9) [back to overview]Change From Baseline in ALS Assessment Questionnaire (40 Items) (ALSAQ40) in Full Analysis Set (FAS) Population at 24 Weeks
NCT00330681 (9) [back to overview]Change From Baseline in Modified Norris Scale Score in Full Analysis Set (FAS) Population at 24 Weeks
NCT00330681 (9) [back to overview]Change From Baseline in Revised ALS Functional Rating Scale (ALSFRS-R) Score in Full Analysis Set (FAS) Population at 24 Weeks
NCT00330681 (9) [back to overview]Percentage of Participants With Adverse Drug Reactions
NCT00330681 (9) [back to overview]Percentage of Participants With Adverse Events
NCT00330681 (9) [back to overview]Death or a Specified State of Disease Progression
NCT00330681 (9) [back to overview]Percentage of Participants With Abnormal Changes in Sensory Examinations
NCT00415519 (7) [back to overview]Change From Baseline in % Forced Vital Capacity (%FVC) in Full Analysis Set (FAS) Population at 24 Weeks
NCT00415519 (7) [back to overview]Change From Baseline in Revised ALS Functional Rating Scale (ALSFRS-R) Score in Full Analysis Set (FAS) Population at 24 Weeks
NCT00415519 (7) [back to overview]Percentage of Participants With Adverse Drug Reactions
NCT00415519 (7) [back to overview]Percentage of Participants With Adverse Events
NCT00415519 (7) [back to overview]Death or a Specified State of Disease Progression
NCT00415519 (7) [back to overview]Percentage of Participants With Abnormal Changes in Sensory Examinations
NCT00415519 (7) [back to overview]The Percentage of Participants With an Abnormal Change in Laboratory Tests That Occurred in More Than Two Patients
NCT00424463 (7) [back to overview]Number of Participants With Death or a Specified State of Disease Progression
NCT00424463 (7) [back to overview]Percentage of Participants With Abnormal Changes in Sensory Examinations
NCT00424463 (7) [back to overview]Percentage of Participants With Laboratory Tests for Which the Incidence of Abnormal Changes Was 5% or Higher in Either Group
NCT00424463 (7) [back to overview]Change From Baseline in % Forced Vital Capacity (%FVC) in Full Analysis Set (FAS) Population at 24 Weeks
NCT00424463 (7) [back to overview]Change From Baseline in Revised ALS Functional Rating Scale (ALSFRS-R) Score in Full Analysis Set (FAS) Population at 24 Weeks
NCT00424463 (7) [back to overview]Percentage of Participants With Adverse Drug Reactions
NCT00424463 (7) [back to overview]Percentage of Participants With Adverse Events
NCT00821821 (2) [back to overview]Plasma MCI-186 Pharmacokinetics
NCT00821821 (2) [back to overview]Number of Participants That Experienced Adverse Events
NCT01492686 (9) [back to overview]Percentage of Participants With Abnormal Values in Sensory Examinations
NCT01492686 (9) [back to overview]Change From Baseline in % Forced Vital Capacity (%FVC) in Full Analysis Set (FAS) Population at 24 Weeks
NCT01492686 (9) [back to overview]Change From Baseline in ALS Assessment Questionnaire (40 Items) (ALSAQ40) in Full Analysis Set (FAS) Population at 24 Weeks
NCT01492686 (9) [back to overview]Change From Baseline in Modified Norris Scale Score in Full Analysis Set (FAS) Population at 24 Weeks
NCT01492686 (9) [back to overview]Change From Baseline in Revised ALS Functional Rating Scale (ALSFRS-R) Score in Full Analysis Set (FAS) Population at 24 Weeks
NCT01492686 (9) [back to overview]Percentage of Participants With Adverse Drug Reactions
NCT01492686 (9) [back to overview]Percentage of Participants With Adverse Events
NCT01492686 (9) [back to overview]"Laboratory Tests Percentage of Participants With Adverse Events by System Organ Class (SOC) of Investigations (PT, MedDRA Ver. 17.0)"
NCT01492686 (9) [back to overview]Number of Participants With Death or a Specified State of Disease Progression
NCT03289208 (4) [back to overview]AUC0-∞
NCT03289208 (4) [back to overview]AUC0-last
NCT03289208 (4) [back to overview]Cmax
NCT03289208 (4) [back to overview]
NCT03289234 (4) [back to overview]AUC0-last
NCT03289234 (4) [back to overview]Cmax
NCT03289234 (4) [back to overview]
NCT03289234 (4) [back to overview]AUC0-∞
NCT03664544 (13) [back to overview]Incidence of Adverse Events (AEs) and Serious Adverse Events
NCT03664544 (13) [back to overview]Pharmacokinetic Parameters of MCI-186: Volume of Distribution During the Terminal Phase (VZ)
NCT03664544 (13) [back to overview]Pharmacokinetic Parameters of MCI-186: Volume of Distribution at Steady State (Vss)
NCT03664544 (13) [back to overview]Pharmacokinetic Parameters of MCI-186: Unbound Total Clearance (Clu)
NCT03664544 (13) [back to overview]Pharmacokinetic Parameters of MCI-186: Unbound Area Under the Concentration-time Curve From Time Zero to Infinity (AUCu0-∞)
NCT03664544 (13) [back to overview]Pharmacokinetic Parameters of MCI-186: Area Under the Concentration-time Curve From Time Zero to the Last Quantifiable Concentration (AUC0-last)
NCT03664544 (13) [back to overview]Pharmacokinetic Parameters of MCI-186: Total Clearance (CL)
NCT03664544 (13) [back to overview]Pharmacokinetic Parameters of MCI-186: Time to Reach Peak Concentration (Tmax)
NCT03664544 (13) [back to overview]Pharmacokinetic Parameters of MCI-186: Terminal Elimination Rate Constant (λZ)
NCT03664544 (13) [back to overview]Pharmacokinetic Parameters of MCI-186: Peak Drug Concentration (Cmax)
NCT03664544 (13) [back to overview]Pharmacokinetic Parameters of MCI-186: Mean Residence Time (MRT)
NCT03664544 (13) [back to overview]Pharmacokinetic Parameters of MCI-186: Half-life (t½)
NCT03664544 (13) [back to overview]Pharmacokinetic Parameters of MCI-186: Area Under the Concentration-time Curve From Time Zero to Infinity (AUC0-∞)
NCT04165824 (2) [back to overview]Number of Participants With Treatment Emergency Adverse Events
NCT04165824 (2) [back to overview]Number of Treatment Emergency Adverse Events

Barthel Index Score

"The Barthel Index of Activities of Daily Living measures functional disability by quantifying patient performance in 10 activities of daily life. These activities can be grouped according to self-care (feeding, grooming, bathing, dressing, bowel and bladder care, and toilet use) and mobility (ambulation, transfers, and stair climbing). 5-point increments are used in scoring, with a maximal score of 100 indicating that a patient is fully independent in physical functioning, and a lowest score of 0 representing a totally dependent bed-ridden state.~The number of patients with 95-100 Barthel Index was evaluated at at 3 months after treatment initiation." (NCT00200356)
Timeframe: 3 months

Interventionparticipants (Number)
Edaravone148
Ozagrel133

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NIH Stroke Scale Score at 1 Month

The NIH stroke scale is a systematic assessment tool that provides a quantitative measure of stroke-related neurologic deficit. Values range from 0 (no deficit) to 42(dead). The number of patients with NIH stroke scale score of 0-1 at 1 month after treatment initiation. (NCT00200356)
Timeframe: 1 month

Interventionparticipants (Number)
Edaravone117
Ozagrel119

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Modified Rankin Scale Score

The number of patients with an Modified Rankin Scale score of 0-1 was evaluated at 6 months after treatment initiation. The Modified Rankin Scale has 6 items, where 0 = No symptoms at all, 1 = No significant disability despite symptoms, 2 = Slight disability, 3 = Moderate disability, 4 = Moderately severe disability, 5 = Severe disability. The higher scores reflect increased disability. (NCT00200356)
Timeframe: 6 months

Interventionparticipants (Number)
Edaravone112
Ozagrel108

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Japan Stroke Scale (Motor Function) Score at 3 Months

The Japan stroke scale (motor function) is a systematic assessment tool that provides a quantitative measure of stroke-related neurologic deficit. Values range from -0.26 (no deficit) to 31.29 (worst). The mean of Japan stroke scale (motor function) score at 3 months after treatment initiation. (NCT00200356)
Timeframe: 3 months

Interventionunits on a scale (Mean)
Edaravone2.507
Ozagrel2.927

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Japan Stroke Scale (Motor Function) Score at 14 Days

The Japan stroke scale (motor function) is a systematic assessment tool that provides a quantitative measure of stroke-related neurologic deficit. Values range from -0.26 (no deficit) to 31.29 (worst). The mean of Japan stroke scale (motor function) score at 14 days after treatment initiation. (NCT00200356)
Timeframe: 14 days

Interventionunits on a scale (Mean)
Edaravone4.521
Ozagrel4.686

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Japan Stroke Scale (Motor Function) Score at 1 Month

The Japan stroke scale (motor function) is a systematic assessment tool that provides a quantitative measure of stroke-related neurologic deficit. Values range from -0.26 (no deficit) to 31.29 (worst). The mean of Japan stroke scale (motor function) score at 1 month after treatment initiation. (NCT00200356)
Timeframe: 1 month

Interventionunits on a scale (Mean)
Edaravone3.632
Ozagrel3.680

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Baseline NIH Stroke Scale Score

The NIH stroke scale is a systematic assessment tool that provides a quantitative measure of stroke-related neurologic deficit. Values range from 0 (no deficit) to 42(dead). (NCT00200356)
Timeframe: Before treatment initiation

Interventionscores on a scale (Mean)
Edaravone3.7
Ozagrel3.8

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the Rate of Patients With a Modified Rankin Scale Score of 0-1

The number of patients with mRS score of 0-1 (good outcome) at 3 months after treatment initiation. The mRS has 6 items, where 0 = No symptoms at all, 1 = No significant disability despite symptoms, 2 = Slight disability, 3 = Moderate disability, 4 = Moderately severe disability, 5 = Severe disability. The higher scores reflect increased disability. (NCT00200356)
Timeframe: 3 months

,
Interventionparticipants (Number)
Score(0-1)012345Death
Edaravone109466337221922
Ozagrel98395940292431

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NIH Stroke Scale Score at 3 Months

The NIH stroke scale is a systematic assessment tool that provides a quantitative measure of stroke-related neurologic deficit. Values range from 0 (no deficit) to 42(dead). The number of patients with NIH stroke scale score of 0-1 at 3 months after treatment initiation. (NCT00200356)
Timeframe: 3 months

Interventionparticipants (Number)
Edaravone135
Ozagrel140

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NIH Stroke Scale Score at 14 Days

The NIH stroke scale is a systematic assessment tool that provides a quantitative measure of stroke-related neurologic deficit. Values range from 0 (no deficit) to 42(dead). The number of patients with NIH stroke scale score of 0-1 at 14 days after treatment initiation. (NCT00200356)
Timeframe: 14 days

Interventionparticipants (Number)
Edaravone98
Ozagrel108

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Nonfatal Ischemic Stroke

number of nonfatal ischemic stroke (NCT00265239)
Timeframe: 415days

Interventionevents (Number)
Edaravone Group0
Placebo Group1

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Cardiac Death

number of cardiac death (NCT00265239)
Timeframe: 415±32 days

Interventionevents (Number)
Edaravone Group0
Placebo Group0

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Nonfatal Myocardial Reinfarction

number of nonfatal myocardial reinfarction (NCT00265239)
Timeframe: 415days

Interventionevents (Number)
Edaravone Group0
Placebo Group2

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Refractory Angina Pectoris

number of refractory angina pectoris (NCT00265239)
Timeframe: 415days

Interventionevents (Number)
Edaravone Group1
Placebo Group5

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Change From Baseline in % Forced Vital Capacity (%FVC) in Full Analysis Set (FAS) Population at 24 Weeks

(NCT00330681)
Timeframe: baseline and 24 weeks

Interventionpercentage of FVC (Least Squares Mean)
MCI-186-14.57
Placebo of MCI-186-17.49

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Percentage of Participants With Laboratory Tests for Which the Incidence of Abnormal Changes Was 5% or Higher in Either Group

(NCT00330681)
Timeframe: 24 weeks

,
Interventionpercentage of participants (Number)
White blood cell counturinary glucose
MCI-18626.9
Placebo of MCI-1865.82.9

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Change From Baseline in ALS Assessment Questionnaire (40 Items) (ALSAQ40) in Full Analysis Set (FAS) Population at 24 Weeks

The ALSAQ40 score is a measure of QoL for patients with ALS. The ALSAQ40 evaluates domains that include physical mobility, ADL and independence, eating and drinking, communication, and emotional reactions. Worst=200, Best=40 (NCT00330681)
Timeframe: baseline and 24 weeks

Interventionunits on a scale (Least Squares Mean)
MCI-18619.6
Placebo of MCI-18619.13

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Change From Baseline in Modified Norris Scale Score in Full Analysis Set (FAS) Population at 24 Weeks

The Modified Norris Scale is a measure of movement disorder for patients with ALS. Worst=0, Best=102 (NCT00330681)
Timeframe: baseline and 24 weeks

Interventionunits on a scale (Least Squares Mean)
MCI-186-14.12
Placebo of MCI-186-16.15

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Change From Baseline in Revised ALS Functional Rating Scale (ALSFRS-R) Score in Full Analysis Set (FAS) Population at 24 Weeks

ALSFRS-R Score: 0=worst; 48=best (NCT00330681)
Timeframe: baseline and 24 weeks

Interventionunits on a scale (Least Squares Mean)
MCI-186-5.7
Placebo of MCI-186-6.35

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Percentage of Participants With Adverse Drug Reactions

(NCT00330681)
Timeframe: 24 weeks

Interventionpercentage of participants (Number)
MCI-18613.7
Placebo of MCI-18619.2

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Percentage of Participants With Adverse Events

(NCT00330681)
Timeframe: 24 weeks

Interventionpercentage of participants (Number)
MCI-18689.2
Placebo of MCI-18688.5

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Death or a Specified State of Disease Progression

"Any of death, disability of independent ambulation, loss of upper arm function, tracheotomy, use of respirator, and use of tube feeding was defined as an event." (NCT00330681)
Timeframe: 24 weeks

,
Interventionparticipants (Number)
deathdisability of independent ambulationloss of upper arm functiontracheotomyuse of respiratoruse of tube feeding
MCI-1862282015
Placebo of MCI-1862234233

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Percentage of Participants With Abnormal Changes in Sensory Examinations

(NCT00330681)
Timeframe: 24 weeks

,
Interventionpercentage of participants (Number)
NumbnessStaggeringVibratory sensation
MCI-186120
Placebo of MCI-18613.81

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Change From Baseline in % Forced Vital Capacity (%FVC) in Full Analysis Set (FAS) Population at 24 Weeks

No primary endpoint was used, because various exploratory analyses were performed. (NCT00415519)
Timeframe: baseline and 24 weeks

Interventionpercentage of FVC (Least Squares Mean)
MCI-186-18.75
Placebo of MCI-186-15.69

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Change From Baseline in Revised ALS Functional Rating Scale (ALSFRS-R) Score in Full Analysis Set (FAS) Population at 24 Weeks

"No primary endpoint was used, because various exploratory analyses were performed.~0=worst; 48=best" (NCT00415519)
Timeframe: baseline and 24 weeks

Interventionunits on a scale (Least Squares Mean)
MCI-186-6.52
Placebo of MCI-186-6

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Percentage of Participants With Adverse Drug Reactions

No primary endpoint was used, because various exploratory analyses were performed. (NCT00415519)
Timeframe: 24 weeks

Interventionpercentage of participants (Number)
MCI-18623.1
Placebo of MCI-1868.3

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Percentage of Participants With Adverse Events

No primary endpoint was used, because various exploratory analyses were performed. (NCT00415519)
Timeframe: 24 weeks

Interventionpercentage of participants (Number)
MCI-18692.3
Placebo of MCI-186100

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Death or a Specified State of Disease Progression

"No primary endpoint was used, because various exploratory analyses were performed.~Any of death, disability of independent ambulation, loss of upper arm function, tracheotomy, use of respirator, and use of tube feeding was defined as an event." (NCT00415519)
Timeframe: 24 weeks

,
Interventionevents (Number)
deathdisability of independent ambulationloss of upper arm functiontracheotomyuse of respiratoruse of tube feeding
MCI-186141001
Placebo of MCI-186022000

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Percentage of Participants With Abnormal Changes in Sensory Examinations

No primary endpoint was used, because various exploratory analyses were performed. (NCT00415519)
Timeframe: 24 weeks

,
Interventionpercentage of participants (Number)
NumbnessStaggeringVibratory sensation
MCI-1860100
Placebo of MCI-186000

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The Percentage of Participants With an Abnormal Change in Laboratory Tests That Occurred in More Than Two Patients

No primary endpoint was used, because various exploratory analyses were performed. (NCT00415519)
Timeframe: 24 weeks

,
Interventionpercentage of participants (Number)
White blood cell count (WBC)Other laboratory tests except for WBC
MCI-18623.10
Placebo of MCI-1868.30

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Number of Participants With Death or a Specified State of Disease Progression

"Any of death, disability of independent ambulation, loss of upper arm function, tracheotomy, use of respirator, and use of tube feeding was defined as an event." (NCT00424463)
Timeframe: 24 weeks (from seventh cycle to twelfth cycle)

,,
InterventionParticipants (Count of Participants)
deathdisability of independent ambulationloss of upper arm functiontracheotomyuse of respiratoruse of tube feeding
MCI-186 - MCI-1861115011
MCI-186 - Placebo of MCI-186183001
Placebo of MCI-186 - MCI-1861207228

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Percentage of Participants With Abnormal Changes in Sensory Examinations

(NCT00424463)
Timeframe: 36 weeks (from seventh cycle to fifteenth cycle)

,,
Interventionpercentage of participant (Number)
NumbnessStaggeringVibratory sensation
MCI-186 - MCI-18602.10
MCI-186 - Placebo of MCI-186000
Placebo of MCI-186 - MCI-18602.30

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Percentage of Participants With Laboratory Tests for Which the Incidence of Abnormal Changes Was 5% or Higher in Either Group

(NCT00424463)
Timeframe: 36 weeks (from seventh cycle to fifteenth cycle)

,,
Interventionpercentage of participant (Number)
White blood cell countAlanine aminotransferaseUrinary glucose
MCI-186 - MCI-1864.26.36.3
MCI-186 - Placebo of MCI-18611.100
Placebo of MCI-186 - MCI-18610.24.53.4

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Change From Baseline in % Forced Vital Capacity (%FVC) in Full Analysis Set (FAS) Population at 24 Weeks

To investigate the sustainability of effects of edaravone, the analysis focusing on the comparison between the placebo and edaravone groups of patients who had received 6 cycles of edaravone treatment, i.e., the comparison of data from Cycles 7 to 12 between the edaravone-edaravone group and the edaravone-placebo group, was performed. (NCT00424463)
Timeframe: baseline (seventh cycle) and at 24 week (twelfth cycle)

Interventionpercentage of FVC (Mean)
MCI-186 - Placebo of MCI-186-10.6
MCI-186 - MCI-186-12.91
Placebo of MCI-186 - MCI-186-10.54

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Change From Baseline in Revised ALS Functional Rating Scale (ALSFRS-R) Score in Full Analysis Set (FAS) Population at 24 Weeks

0=worst; 48=best To investigate the sustainability of effects of edaravone, the analysis focusing on the comparison between the placebo and edaravone groups of patients who had received 6 cycles of edaravone treatment, i.e., the comparison of data from Cycles 7 to 12 between the edaravone-edaravone group and the edaravone-placebo group, was performed. (NCT00424463)
Timeframe: baseline (seventh cycle) and at 24 week (twelfth cycle)

Interventionunits on a scale (Mean)
MCI-186 - Placebo of MCI-186-5.5
MCI-186 - MCI-186-4.2
Placebo of MCI-186 - MCI-186-5.4

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Percentage of Participants With Adverse Drug Reactions

(NCT00424463)
Timeframe: 36 weeks (from seventh cycle to fifteenth cycle)

Interventionpercentage of participant (Number)
MCI-186 - Placebo of MCI-1864.4
MCI-186 - MCI-18610.4
Placebo of MCI-186 - MCI-18610.2

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Percentage of Participants With Adverse Events

(NCT00424463)
Timeframe: 36 weeks (from seventh cycle to fifteenth cycle)

Interventionpercentage of participant (Number)
MCI-186 - Placebo of MCI-18697.8
MCI-186 - MCI-18691.7
Placebo of MCI-186 - MCI-18692

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Plasma MCI-186 Pharmacokinetics

The geometric mean values of MCI-186 plasma concentration at the end of the infusion (at 72h) in cohorts 1 and 2 were determined. (NCT00821821)
Timeframe: 72 hours

Interventionng / ml (Geometric Mean)
MCI-186 Cohort1391
MCI-186 Cohort21595

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Number of Participants That Experienced Adverse Events

Additional Outcome Measures are included in Tables for Serious Adverse Events and Other Adverse Events to report their numbers and frequency. (NCT00821821)
Timeframe: 87days

,,
Interventionparticipants (Number)
DeathsSerious Adverse EventsOther Adverse Events
MCI-186 Cohort10012
MCI-186 Cohort20210
Placebo Group0110

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Percentage of Participants With Abnormal Values in Sensory Examinations

(NCT01492686)
Timeframe: baseline and 24 weeks

,
Interventionpercentage of Participants (Number)
Numbness (at baseline)Numbness (at 24 week)Staggering (at baseline)Staggering (at 24 week)
MCI-1862.97.21.42.9
Placebo of MCI-1867.49.48.83.1

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Change From Baseline in % Forced Vital Capacity (%FVC) in Full Analysis Set (FAS) Population at 24 Weeks

(NCT01492686)
Timeframe: baseline and 24 weeks

Interventionpercentage of FVC (Least Squares Mean)
MCI-186-15.61
Placebo of MCI-186-20.4

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Change From Baseline in ALS Assessment Questionnaire (40 Items) (ALSAQ40) in Full Analysis Set (FAS) Population at 24 Weeks

The ALSAQ40 score is a measure of QoL for patients with ALS. The ALSAQ40 evaluates domains that include physical mobility, Activities of daily living (ADL) and independence, eating and drinking, communication, and emotional reactions. 200=worst; 40=best (NCT01492686)
Timeframe: baseline and 24 weeks

Interventionunits on a scale (Least Squares Mean)
MCI-18617.25
Placebo of MCI-18626.04

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Change From Baseline in Modified Norris Scale Score in Full Analysis Set (FAS) Population at 24 Weeks

The Modified Norris Scale is a measure of movement disorder for patients with ALS. 0=worst; 102=best (NCT01492686)
Timeframe: baseline and 24 weeks

Interventionunits on a scale (Least Squares Mean)
MCI-186-15.91
Placebo of MCI-186-20.8

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Change From Baseline in Revised ALS Functional Rating Scale (ALSFRS-R) Score in Full Analysis Set (FAS) Population at 24 Weeks

0=worst; 48=best (NCT01492686)
Timeframe: baseline and 24 weeks

Interventionunits on a scale (Least Squares Mean)
MCI-186-5.01
Placebo of MCI-186-7.5

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Percentage of Participants With Adverse Drug Reactions

(NCT01492686)
Timeframe: 24 weeks

Interventionpercentage of Participants (Number)
MCI-1862.9
Placebo of MCI-1867.4

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Percentage of Participants With Adverse Events

(NCT01492686)
Timeframe: 24 weeks

Interventionpercentage of Participants (Number)
MCI-18684.1
Placebo of MCI-18683.8

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"Laboratory Tests Percentage of Participants With Adverse Events by System Organ Class (SOC) of Investigations (PT, MedDRA Ver. 17.0)"

(NCT01492686)
Timeframe: 24 weeks

,
Interventionpercentage of Participants (Number)
Blood bilirubin increasedBlood creatine phosphokinase increasedLiver function test abnormalWhite blood cell count decreased
MCI-186001.41.4
Placebo of MCI-1861.51.51.50

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Number of Participants With Death or a Specified State of Disease Progression

"Any of death, disability of independent ambulation, loss of upper limbs function, tracheotomy, use of respirator, use of tube feeding and loss of useful speech was defined as an event." (NCT01492686)
Timeframe: 24 weeks

,
InterventionCount of Participants (Number)
DeathDisability of independent ambulationLoss of upper limbs functionTracheotomyUse of respiratorUse of tube feedingLoss of useful speech
MCI-1860001001
Placebo of MCI-1860200013

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AUC0-∞

(NCT03289208)
Timeframe: pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h post-dose

Interventionng*hr/mL (Mean)
Mild Renal Function Group770.97
Moderate Renal Function Group826.44
Normal Renal Function Group644.85

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AUC0-last

(NCT03289208)
Timeframe: pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h post-dose

Interventionng*hr/mL (Mean)
Mild Renal Function Group758
Moderate Renal Function Group808.7
Normal Renal Function Group638.09

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Cmax

(NCT03289208)
Timeframe: pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h post-dose

Interventionng/mL (Mean)
Mild Renal Function Group545.4
Moderate Renal Function Group593.2
Normal Renal Function Group475.9

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(NCT03289208)
Timeframe: pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h post-dose

Interventionhour (Mean)
Mild Renal Function Group5.38
Moderate Renal Function Group7.31
Normal Renal Function Group2.87

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AUC0-last

(NCT03289234)
Timeframe: pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h post-dose

Interventionng*hr/mL (Mean)
Mild Hepatic Impairment716.86
Moderate Hepatic Impairment739.28
Normal Hepatic Function582.89

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Cmax

(NCT03289234)
Timeframe: pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h post-dose

Interventionng/mL (Mean)
Mild Hepatic Impairment538.1
Moderate Hepatic Impairment533.4
Normal Hepatic Function429

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(NCT03289234)
Timeframe: pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h post-dose

Interventionhour (Mean)
Mild Hepatic Impairment3.14
Moderate Hepatic Impairment4.37
Normal Hepatic Function5.41

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AUC0-∞

(NCT03289234)
Timeframe: pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h post-dose

Interventionng*hr/mL (Mean)
Mild Hepatic Impairment727.55
Moderate Hepatic Impairment751.52
Normal Hepatic Function594.96

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Incidence of Adverse Events (AEs) and Serious Adverse Events

Number of adverse events (NCT03664544)
Timeframe: Day -1 to Day 7

,
InterventionEvents (Number)
Adverse eventsSerious adverse eventsTreatment emergent adverse eventsAdverse Drug reactionTEAE leading to discontinuation of study drug
HP PK MCI-18600000
NHV PK MCI-18610110

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Pharmacokinetic Parameters of MCI-186: Volume of Distribution During the Terminal Phase (VZ)

Unchanged MCI-186 (NCT03664544)
Timeframe: Day 1 to 3 (Pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h)

InterventionL (Mean)
HP PK MCI-186359.85
NHV PK MCI-1861064.88

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Pharmacokinetic Parameters of MCI-186: Volume of Distribution at Steady State (Vss)

Unchanged MCI-186 (NCT03664544)
Timeframe: Day 1 to 3 (Pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h)

InterventionL (Mean)
HP PK MCI-186133.86
NHV PK MCI-186449.79

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Pharmacokinetic Parameters of MCI-186: Unbound Total Clearance (Clu)

Unchanged MCI-186 (NCT03664544)
Timeframe: Day 1 to 3 (Pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h)

InterventionL/h (Mean)
HP PK MCI-186529.83
NHV PK MCI-186702.10

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Pharmacokinetic Parameters of MCI-186: Unbound Area Under the Concentration-time Curve From Time Zero to Infinity (AUCu0-∞)

Unchanged MCI-186 (NCT03664544)
Timeframe: Day 1 to 3 (Pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h)

Interventionh*ng/mL (Mean)
HP PK MCI-18665.41
NHV PK MCI-18645.33

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Pharmacokinetic Parameters of MCI-186: Area Under the Concentration-time Curve From Time Zero to the Last Quantifiable Concentration (AUC0-last)

Unchanged MCI-186 (NCT03664544)
Timeframe: Day 1 to 3 (Pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h)

Interventionh*ng/mL (Mean)
HP PK MCI-186473.90
NHV PK MCI-186394.65

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Pharmacokinetic Parameters of MCI-186: Total Clearance (CL)

Unchanged MCI-186 (NCT03664544)
Timeframe: Day 1 to 3 (Pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h)

InterventionL/h (Mean)
HP PK MCI-18666.82
NHV PK MCI-18678.72

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Pharmacokinetic Parameters of MCI-186: Time to Reach Peak Concentration (Tmax)

Unchanged MCI-186 (NCT03664544)
Timeframe: Day 1 to 3 (Pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h)

Interventionh (Median)
HP PK MCI-1861.02
NHV PK MCI-1861.02

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Pharmacokinetic Parameters of MCI-186: Terminal Elimination Rate Constant (λZ)

Unchanged MCI-186 (NCT03664544)
Timeframe: Day 1 to 3 (Pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h)

Intervention/h (Mean)
HP PK MCI-1860.19
NHV PK MCI-1860.15

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Pharmacokinetic Parameters of MCI-186: Peak Drug Concentration (Cmax)

Unchanged MCI-186 (NCT03664544)
Timeframe: Day 1 to 3 (Pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h)

Interventionng/mL (Mean)
HP PK MCI-186347.6
NHV PK MCI-186280.3

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Pharmacokinetic Parameters of MCI-186: Mean Residence Time (MRT)

Unchanged MCI-186 (NCT03664544)
Timeframe: Day 1 to 3 (Pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h)

Interventionh (Mean)
HP PK MCI-1862.27
NHV PK MCI-1865.51

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Pharmacokinetic Parameters of MCI-186: Half-life (t½)

Unchanged MCI-186 (NCT03664544)
Timeframe: Day 1 to 3 (Pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h)

Interventionh (Mean)
HP PK MCI-1863.88
NHV PK MCI-1869.51

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Pharmacokinetic Parameters of MCI-186: Area Under the Concentration-time Curve From Time Zero to Infinity (AUC0-∞)

Unchanged MCI-186 (NCT03664544)
Timeframe: Day 1 to 3 (Pre-dose, 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h and 48h)

Interventionh*ng/mL (Mean)
HP PK MCI-186496.98
NHV PK MCI-186416.34

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Number of Participants With Treatment Emergency Adverse Events

(NCT04165824)
Timeframe: Up to 48 Weeks

InterventionParticipants (Count of Participants)
MT-1186175

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Number of Treatment Emergency Adverse Events

(NCT04165824)
Timeframe: up to 48 Weeks

Interventionevents (Number)
MT-1186961

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