Page last updated: 2024-12-05

oxiracetam

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

Description

Oxiracetam is a racetam derivative, a class of drugs that are thought to enhance cognitive function. It is structurally similar to piracetam, the first racetam drug developed, and is thought to act as a positive allosteric modulator of the AMPA subtype of glutamate receptors. Oxiracetam has been shown to improve learning and memory in animal models, and it has been investigated for its potential therapeutic effects in conditions such as Alzheimer's disease, age-related cognitive decline, and stroke. However, human clinical trials have yielded mixed results, and the use of oxiracetam for these indications remains investigational. Oxiracetam is generally well tolerated, but side effects such as headaches, dizziness, and gastrointestinal upset have been reported. The synthesis of oxiracetam involves a multi-step process starting with the reaction of pyrrolidine with ethyl acrylate. This forms a pyrrolidine derivative which is then subjected to a series of reactions including acylation, reduction, and ring closure to yield the final oxiracetam molecule. The exact mechanism of action of oxiracetam is not fully understood, but it is thought to involve interactions with several neurotransmitter systems, including glutamate, acetylcholine, and dopamine. It is being studied for its potential to improve cognitive function in a variety of conditions, including age-related cognitive decline, Alzheimer's disease, and stroke. While the research on oxiracetam is ongoing, its potential benefits for improving cognitive function and its relatively low toxicity make it an interesting subject for further study.'

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

Cross-References

ID SourceID
PubMed CID4626
CHEMBL ID36633
CHEBI ID134788
SCHEMBL ID526050
MeSH IDM0120871

Synonyms (94)

Synonym
AC-670
4-hydroxypiracetam
(+-)-oxiracetam
1-pyrrolidineacetamide, 4-hydroxy-2-oxo-, (+-)-
(+-)-4-hydroxy-2-oxo-1-pyrrolidineacetamide
1-pyrrolidineacetamide, 4-hydroxy-2-oxo-
ccris 4221
4-hydroxy-2-oxo-1-pyrrolidineacetamide
cgp 21690e
oxiracetamum [inn-latin]
hydroxypiracetam
brn 1529719
isf 2522
isf-2522
oxiracetam
cgp-21690e
neuractiv
oriest
ct-848 ,
neuromet
EU-0100933
LOPAC0_000933
oxiracetam (inn)
D07346
62613-82-5
NCGC00094242-02
NCGC00094242-01
NCGC00015768-02
CHEBI:134788
O 3011
4-hydroxy-2-oxopyrrolidine-n-acetamide
NCGC00015768-04
gnf-pf-1005 ,
CHEMBL36633
2-(4-hydroxy-2-oxopyrrolidin-1-yl)acetamide
A21970
HMS3262L08
EN300-75437
dtxcid7025180
cas-62613-82-5
dtxsid9045180 ,
tox21_110218
AKOS013252523
CCG-205014
S4270
NCGC00015768-03
FT-0673341
FT-0673343
oxiracetam [inn:ban]
unii-p7u817352g
oxiracetamum
p7u817352g ,
FT-0630731
LP00933
AB05478
oxiracetam(random configuration)
2-(4-hydroxy-2-oxo-1-pyrrolidinyl)acetamide
O0398
SCHEMBL526050
oxiracetam [mi]
oxiracetam [mart.]
oxiracetam [who-dd]
oxiracetam [inn]
oxiracetam [jan]
4-hydroxy-2-oxo-pyrrolidinacetamide
NCGC00261618-01
tox21_500933
2-(4-hydroxypyrrolidin-2-on-1-yl) acetamide
oxiractam
4-hydroxypyrrolidin-2-on-1-yl acetamide
4-hydroxy-2-oxopyrrolidin-1-yl-acetamide
IHLAQQPQKRMGSS-UHFFFAOYSA-N
Q-201526
HY-B1715
CS-8012
mfcd00242951
isf2522
sr-01000076046
SR-01000076046-1
HMS3652J06
SW220157-1
BCP06209
Q415099
DB13601
AS-11801
r-oxiracetam; (r)-isf-2522;(r)-(+)-oxiracetam
BCP31146
SDCCGSBI-0050907.P002
HMS3885B17
NCGC00015768-07
AMY5769
CS3412
A861378
Z1178486698

Research Excerpts

Overview

Oxiracetam is a nootropic drug that improves clinical outcomes for some central nervous system (CNS) disorders. It was tested as a potential treatment for cognitive decline in patients with multi-infarct dementia (MID) and primary degenerative dementia (PDD)

ExcerptReferenceRelevance
"Oxiracetam (ORC) is a commonly used nootropic drug for improving cognition and memory impairments. "( Oxiracetam ameliorates cognitive deficits in vascular dementia rats by regulating the expression of neuronal apoptosis/autophagy-related genes associated with the activation of the Akt/mTOR signaling pathway.
Dong, Y; Jiang, X; Liu, Z; Lv, P; Qi, Q; Xu, J, 2019
)
3.4
"Oxiracetam is a nootropic drug that is commonly used to treat cognitive deficits of cerebrovascular origins."( (S)-Oxiracetam is the Active Ingredient in Oxiracetam that Alleviates the Cognitive Impairment Induced by Chronic Cerebral Hypoperfusion in Rats.
Guo, Y; Jiang, H; Li, W; Liu, H; Nie, Z; Pu, X; Sun, Y; Wang, C; Xiong, X; Zhang, K; Zhang, X; Zhao, X, 2017
)
1.73
"Oxiracetam is a nootropic drug that improves clinical outcomes for some central nervous system (CNS) disorders."( Oxiracetam can improve cognitive impairment after chronic cerebral hypoperfusion in rats.
Li, L; Nie, L; Yao, XL; Yao, ZH; Zhang, SF, 2016
)
2.6
"Oxiracetam is a recently synthesized nootropic that was tested as a potential treatment for cognitive decline in patients with multi-infarct dementia (MID) and primary degenerative dementia (PDD). "( Oxiracetam in the treatment of multi-infarct dementia and primary degenerative dementia.
Dysken, MW; Katz, R; Kuskowski, M; Stallone, F, 1989
)
3.16
"Oxiracetam is a new psychotropic drug that has been shown to positively affect processes both in animals and in patients with impaired brain function. "( Activity of oxiracetam in patients with organic brain syndrome: a neuropsychological study.
Arrigo, A; Corsico, R; Gualtieri, S; Moglia, A; Sinforiani, E; Zandrini, C, 1986
)
2.09

Actions

ExcerptReferenceRelevance
"1) Oxiracetam did not inhibit 3H-QNB binding in the cerebral cortex and hippocampus."( [Biochemical studies of oxiracetam (CT-848) on cholinergic neurons].
Mochizuki, D; Shinoda, Y; Sugiyama, S, 1992
)
1.1

Treatment

Oxiracetam treatment is able to restore the labeled choline content in the cells from SH rats, as well as the incorporation of choline into its derivatives PC and CPG, to the levels found in the WK or more. Treatment with oxir acetam for 14 days after the occlusion showed a tendency to an improvement in the disturbed circadian rhythm.

ExcerptReferenceRelevance
"Oxiracetam-treated DBA mice demonstrated a significant increase in spatial learning performance as determined by the Morris task."( Enhancement of hippocampally-mediated learning and protein kinase C activity by oxiracetam in learning-impaired DBA/2 mice.
Clark, VJ; Fordyce, DE; Paylor, R; Wehner, JM, 1995
)
1.24
"Oxiracetam treatment is able to restore the labeled choline content in the cells from SH rats, as well as the incorporation of choline into its derivatives PC and CPG, to the levels found in the WK or more."( Choline incorporation into phospholipids in brain areas from spontaneously hypertensive rats: effect of oxiracetam treatment.
Avellini, L; Belfiore, P; Brunetti, M; De Medio, GE; Gaiti, A; Mariani, O; Nardella, C; Terracina, L, 1991
)
1.22
"Treatment with oxiracetam (400 mg/kg/d p.o.) for 14 days after the occlusion showed a tendency to an improvement in the disturbed circadian rhythm but did not influence the size of brain infarction."( Effect of oxiracetam on cerebrovascular impairment in rats.
Hasegawa, Y; Inukai, T; Kometani, M; Nakao, N; Okada, M; Takemori, E, 1991
)
1.02
"Pretreatment with oxiracetam and D-pyroglutamic acid at doses ranging from 50 to 500 mg/kg SC dose-dependently prevented the disruptive effect of AP-5."( Oxiracetam and D-pyroglutamic acid antagonize a disruption of passive avoidance behaviour induced by the N-methyl-D-aspartate receptor antagonist 2-amino-5-phosphonovalerate.
Paoli, F; Pepeu, G; Spignoli, G, 1990
)
2.05

Pharmacokinetics

After a single oral dose (800 mg), serum oxiracetam levels reached a peak (25 +/- 6 micrograms/ml) within 1-3 h and declined thereafter with a half-life of 3 to 6 h. The pharmacokinetic profiles of racemic oxir acetam and its pure enantiomers in rats were evaluated and compared.

ExcerptReferenceRelevance
" In plasma, the terminal elimination half-life (T1/2) ranged from 10."( Pharmacokinetics of oxiracetam in patients with renal impairment after a 800 mg single oral dose.
Coppens, H; Darragon, T; Dubois, JP; Lambrey, G; Lecaillon, JB; Pozet, N; Reumond, G; Traeger, J,
)
0.45
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" The developed method was successfully applied to pharmacokinetic studies of piracetam in rats following single oral administration dose of 50 mg/kg."( Determination of piracetam in rat plasma by LC-MS/MS and its application to pharmacokinetics.
Hu, L; Lin, D; Wang, X; Wu, H; Xu, R; Yang, X; Ye, F; Zhu, J, 2010
)
0.36
" In conclusion, a simple, sensitive and specific HPLC-MS/MS method was successfully applied to the pharmacokinetic study in rats after an intravenous administration at a high dose of 2g/kg."( Simultaneous determination of oxiracetam and its degraded substance in rat plasma by HPLC-MS/MS and its application to pharmacokinetic study after a single high-dose intravenous administration.
He, Z; Liu, X; Ma, P; Sun, J; Wan, X; Wang, H; Xi, L; Zhang, X, 2014
)
0.69
" The pharmacokinetic profiles of racemic oxiracetam and its pure enantiomers in rats were evaluated and compared by enantioselective high-performance liquid chromatography, which was performed on a Chiralpak ID column with a mobile phase of hexane-ethanol-trifluoroacetic acid (78:22:0."( Comparative pharmacokinetic studies of racemic oxiracetam and its pure enantiomers after oral administration in rats by a stereoselective HPLC method.
Chen, X; He, J; Li, J; Lu, Y; Xing, H; Yang, S; Yang, W; Yang, Y; Zhang, Q; Zhao, D, 2015
)
0.94
" The method was successfully applied to a pharmacokinetic study of individual enantiomer and racemic oxiracetam in beagle dogs after oral administration."( Enantioselective HPLC determination of oxiracetam enantiomers and application to a pharmacokinetic study in beagle dogs.
Chen, X; He, J; Li, J; Lu, Y; Yang, W; Yang, Y; Zhang, Q; Zhao, D; Zheng, Y, 2015
)
0.9
"A pharmacokinetic comparison and conformational stability study of S-oxiracetam (S-ORT) and R-oxiracetam (R-ORT) in beagle dogs was used to investigate the possible mechanism of different effects of two oxiracetam enantiomers through a random crossover design."( Pharmacokinetic comparisons of S-oxiracetam and R-oxiracetam in beagle dogs.
Ji, H; Jia, Y; Li, T; Wang, W; Xie, H, 2016
)
0.95

Compound-Compound Interactions

Edaravone combined with oxiracetam can inhibit the neuronal apoptosis in CI rats. Transplantation of BMSCs can promote the recovery of neurologic function in MCAO rats.

ExcerptReferenceRelevance
" Transplantation of BMSCs can promote the recovery of neurologic function in MCAO rats, and the effect of BMSCs combined with oxiracetam was better than the either one."( Bone marrow stromal cells combined with oxiracetam influences the expression of B-cell lymphoma 2 in rats with ischemic stroke.
Fei, Y; Guan, Y; Li, F; Pan, Y; Wang, C; Zhang, J; Zhu, L,
)
0.6
" The clinical efficacy of nicergoline combined with oxiracetam in the treatment of vascular cognitive impairment after stroke was analyzed."( Clinical efficacy and safety of nicergoline combined with oxiracetam in the treatment of vascular cognitive impairment.
Ma, Z; Qiao, P; Wang, B; Zhong, L, 2020
)
1.05
"The present clinical study was conducted to investigate the effect of oxiracetam combined with ginkgo biloba extract in treating patients with acute intracerebral hemorrhage."( Effects of oxiracetam combined with ginkgo biloba extract in the treatment of acute intracerebral hemorrhage: A clinical study.
Guo, SF; Li, XX; Liu, SH; Pang, SL; Zhuang, SJ, 2020
)
1.18
"Oxiracetam combined with Ginkgo biloba extract in the treatment of acute cerebral hemorrhage has a significant improvement effect."( Effects of oxiracetam combined with ginkgo biloba extract in the treatment of acute intracerebral hemorrhage: A clinical study.
Guo, SF; Li, XX; Liu, SH; Pang, SL; Zhuang, SJ, 2020
)
2.39
"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
)
1.22
" 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
)
1.19
"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
)
1.31

Bioavailability

ExcerptReferenceRelevance
" The rate of absorption was high in all species."( Absorption and disposition of 14C-labelled oxiracetam in rat, dog and man.
Bentley, P; Gschwind, HP; Schütz, H; Wigger, N,
)
0.39
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" The orally bioavailable lead imidazolopiperazine confers complete causal prophylactic protection (15 milligrams/kilogram) in rodent models of malaria and shows potent in vivo blood-stage therapeutic activity."( Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
Barnes, SW; Bonamy, GM; Bopp, SE; Borboa, R; Bright, AT; Chatterjee, A; Che, J; Cohen, S; Dharia, NV; Diagana, TT; Fidock, DA; Froissard, P; Gagaring, K; Gettayacamin, M; Glynne, RJ; Gordon, P; Groessl, T; Kato, N; Kuhen, KL; Lee, MC; Mazier, D; McNamara, CW; Meister, S; Nagle, A; Nam, TG; Plouffe, DM; Richmond, W; Roland, J; Rottmann, M; Sattabongkot, J; Schultz, PG; Tuntland, T; Walker, JR; Winzeler, EA; Wu, T; Zhou, B; Zhou, Y, 2011
)
0.37
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

The in vitro study used a cell injury controller to damage SH-SY5Y cells and evaluate the effect of oxiracetam at a dosage of 100 nM. At the dosage used, selegiline is more effective than oxir acetam in improving higher cognitive functions.

ExcerptRelevanceReference
" Analysis of the results demonstrates that, at the dosage used, selegiline is more effective than oxiracetam in improving higher cognitive functions and reducing impairment in daily living."( Selegiline versus oxiracetam in patients with Alzheimer-type dementia.
Falsaperla, A; Monici Preti, PA; Oliani, C,
)
0.68
" or identical placebo capsules in the same dosing schedule."( Double-blind, placebo-controlled, clinical, psychometric and neurophysiological investigations with oxiracetam in the organic brain syndrome of late life.
Grünberger, J; Linzmayer, L; Pietschmann, H; Saletu, B, 1985
)
0.49
"3 and 1 mg/kg ip for most compounds), the presence of a bell-shaped dose-response curve and, generally, a reduction of biological activity after po administration."( Synthesis and pharmacological activity of a series of dihydro-1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-diones, a novel class of potent cognition enhancers.
Banfi, S; Biagetti, R; Cerri, A; Dorigotti, L; Farina, C; Magnani, M; Pfeiffer, U; Pinza, M; Pozzi, O; Riccaboni, MT, 1993
)
0.29
" For the best separation and low back pressure, orthogonal experiments were carried out with V (cyclohexanol): V (dodecanol), V (GMA): V (DVB) and BPO dosage as the three main factors."( [Optimization of preparation of poly ( glycidyl methacrylate-divinylbenzene) monolithic column with orthogonal experiments for separation of small molecules].
Liu, Z; Ma, W; Ning, F; Xu, H, 2010
)
0.36
" A saturating phenomenon of (S)-ORC was observed when the dosage ranged from 200 mg/kg to 800 mg/kg."( Comparative pharmacokinetic studies of racemic oxiracetam and its pure enantiomers after oral administration in rats by a stereoselective HPLC method.
Chen, X; He, J; Li, J; Lu, Y; Xing, H; Yang, S; Yang, W; Yang, Y; Zhang, Q; Zhao, D, 2015
)
0.67
"The in vitro study used a cell injury controller to damage SH-SY5Y cells and evaluate the effect of oxiracetam at a dosage of 100 nM."( Oxiracetam alleviates anti-inflammatory activity and ameliorates cognitive impairment in the early phase of traumatic brain injury.
Cho, SM; Choi, H; Han, SW; Hong, EP; Jeon, JP; Jung, H; Kim, JT; Kim, N; Lee, A; Lee, Y; Park, CH; Youn, DH, 2023
)
2.57
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
organooxygen compoundAn organochalcogen compound containing at least one carbon-oxygen bond.
organonitrogen compoundAny heteroorganic entity containing at least one carbon-nitrogen bond.
[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 (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency39.81070.003245.467312,589.2998AID1705
thioredoxin reductaseRattus norvegicus (Norway rat)Potency37.68580.100020.879379.4328AID588453
arylsulfatase AHomo sapiens (human)Potency4.77551.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.02240.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency25.11890.540617.639296.1227AID2364; AID2528
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency8.49210.134610.395030.1313AID1347049
M-phase phosphoprotein 8Homo sapiens (human)Potency0.89130.177824.735279.4328AID488949
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency8.49210.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (51)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
AID125744Amnesia-reversal activity in scopolamine-induced amnesia model of mice at 1 mg/kg i.p.1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
Synthesis and amnesia-reversal activity of a series of 7- and 5-membered 3-acylamino lactams.
AID125742Amnesia-reversal activity in ECS-induced amnesia model of mice at 10 mg/kg i.p.1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
Synthesis and amnesia-reversal activity of a series of 7- and 5-membered 3-acylamino lactams.
AID449704NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID191747Percent reversal of scopolamine-induced amnesia rat at 30 mg/kg po1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Synthesis and pharmacological activity of a series of dihydro-1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-diones, a novel class of potent cognition enhancers.
AID449703NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay 2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID191746Percent reversal of scopolamine-induced amnesia rat at 10 mg/kg po1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Synthesis and pharmacological activity of a series of dihydro-1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-diones, a novel class of potent cognition enhancers.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID125741Amnesia-reversal activity in ECS-induced amnesia model of mice at 1 mg/kg i.p.1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
Synthesis and amnesia-reversal activity of a series of 7- and 5-membered 3-acylamino lactams.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID449705NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID191745Percent reversal of scopolamine-induced amnesia rat following 10 mg/kg i.p.1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Synthesis and pharmacological activity of a series of dihydro-1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-diones, a novel class of potent cognition enhancers.
AID191743Percent reversal of scopolamine-induced amnesia rat following 1.0 mg/kg i.p.1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Synthesis and pharmacological activity of a series of dihydro-1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-diones, a novel class of potent cognition enhancers.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID449706NOVARTIS: Inhibition Frequency Index (IFI) - the number of HTS assays where a compound showed > 50% inhibition/induction, expressed as a percentage of the number of assays in which the compound was tested.2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID125743Amnesia-reversal activity (AA) evaluated in ECS-induced amnesia model of mice at a dose of 100 mg/kg1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
Synthesis and amnesia-reversal activity of a series of 7- and 5-membered 3-acylamino lactams.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC 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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID1347151Optimization of GU AMC 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.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction 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.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
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.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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).
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.
AID602156Novartis GNF Liver Stage Dataset: Malariabox Annotation2011Science (New York, N.Y.), Dec-09, Volume: 334, Issue:6061
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (155)

TimeframeStudies, This Drug (%)All Drugs %
pre-199043 (27.74)18.7374
1990's57 (36.77)18.2507
2000's10 (6.45)29.6817
2010's27 (17.42)24.3611
2020's18 (11.61)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials22 (12.72%)5.53%
Reviews4 (2.31%)6.00%
Case Studies1 (0.58%)4.05%
Observational0 (0.00%)0.25%
Other146 (84.39%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized, Double-blind, Positive Drug/Placebo Parallel Controlled, Multicenter, Phase II Exploratory Clinical Trial of L-oxiracetam Injection to Improve Memory and Cognitive Impairment in Patients With Craniocerebral Injury [NCT04205565]Phase 2200 participants (Actual)Interventional2017-11-08Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]