Page last updated: 2024-09-20

1-hydroxy-3-amino-2-pyrrolidone

Description

1-hydroxy-3-amino-2-pyrrolidone: a CNS depressant; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID1232
CHEMBL ID351464
SCHEMBL ID253915
MeSH IDM0041521

Synonyms (52)

Synonym
1003-51-6
EU-0100134
1-hydroxy-3-amino-2-pyrrolidone
3-amino-1-hydroxy-2-pyrrolidinone
ha-966
NCGC00093624-02
NCGC00093624-01
(?)-ha-966
NCGC00015111-02
( inverted question mark)-ha-966
A 9699
( inverted question mark)-3-amino-1-hydroxy-2-pyrrolidone
NCGC00015111-04
3-amino-1-hydroxypyrrolidin-2-one
FT-0695028
CHEMBL351464 ,
HMS3260K10
3-amino-1-hydroxypyrrolidone
1-hydroxy-3-aminopyrrolidin-2-one
dl-1-hydroxy-3-amino-2-pyrrolidinone
1-hydroxy-3-amino-pyrrolidine-2-one
AKOS006272122
CCG-204229
3-amino-1-hydroxy-pyrrolidin-2-one
NCGC00015111-03
f2jlv9220t ,
unii-f2jlv9220t
FT-0645237
(+/-)-ha-966
LP00134
AB02803
SCHEMBL253915
70996-07-5
(+/-)-3-amino-1-hydroxy-2-pyrrolidone
NCGC00260819-01
tox21_500134
(y)-ha-966
3-amino-1-hydroxy-2-pyrrolidone
ha-966, (+/-)-
mfcd00069208
2-pyrrolidinone, 3-amino-1-hydroxy-
sr-01000075418
SR-01000075418-1
Q5628879
FT-0770580
bdbm50212605
SDCCGSBI-0050122.P002
DTXSID90905333
A849548
3-amino-1-hydroxy-pyrrolidin-2-one;3-amino-1-hydroxypyrrolidin-2-one
EN300-219911
CS-0200048

Protein Targets (10)

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
dopamine D1 receptorHomo sapiens (human)Potency0.00460.00521.30228.1995AID624455
thioredoxin reductaseRattus norvegicus (Norway rat)Potency37.68580.100020.879379.4328AID588453
ATAD5 protein, partialHomo sapiens (human)Potency9.19620.004110.890331.5287AID493107
USP1 protein, partialHomo sapiens (human)Potency0.25120.031637.5844354.8130AID504865
GLS proteinHomo sapiens (human)Potency5.62340.35487.935539.8107AID624146
Microtubule-associated protein tauHomo sapiens (human)Potency39.81070.180013.557439.8107AID1460
arylsulfatase AHomo sapiens (human)Potency1.90121.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency4.22840.035520.977089.1251AID504332
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 (20)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (196)

TimeframeStudies, This Drug (%)All Drugs %
pre-199036 (18.37)18.7374
1990's121 (61.73)18.2507
2000's27 (13.78)29.6817
2010's7 (3.57)24.3611
2020's5 (2.55)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 (%)
Trials0 (0.00%)5.53%
Reviews3 (1.52%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other195 (98.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research Highlights

Safety/Toxicity (1)

ArticleYear
Role of glycine in the N-methyl-D-aspartate-mediated neuronal cytotoxicity.
Journal of neurochemistry, Volume: 54, Issue: 3
1990
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioavailability (3)

ArticleYear
Indole-2-carboxylates, novel antagonists of the N-methyl-D-aspartate (NMDA)-associated glycine recognition sites: in vivo characterization.
Neuropharmacology, Volume: 32, Issue: 2
1993
In vivo antagonism of agonist actions at N-methyl-D-aspartate and N-methyl-D-aspartate-associated glycine receptors in mouse cerebellum: studies of 1-hydroxy-3-aminopyrrolidone-2.
Neuropharmacology, Volume: 29, Issue: 7
1990
Neuropharmacological characterization of 1-aminocyclopropane-1-carboxylate and 1-aminocyclobutane-1-carboxylate, ligands of the N-methyl-D-aspartate-associated glycine receptor.
Neuropharmacology, Volume: 29, Issue: 3
1990
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (10)

ArticleYear
Effects of intrastriatal injections of glutamate receptor antagonists on the severity of paroxysmal dystonia in the dtsz mutant.
European journal of pharmacology, Jun-01, Volume: 563, Issue: 1-3
2007
Effects on cocaine and food self-administration of (+)-HA-966, a partial agonist at the glycine/NMDA modulatory site, in rats.
Psychopharmacology, Volume: 173, Issue: 1-2
2004
The glycine/NMDA receptor antagonist (+)-HA966 enhances the peripheral effect of morphine in neuropathic rats.
Pain, Volume: 99, Issue: 3
2002
FK960 [N-(4-acetyl-1-piperazinyl)-p-fluorobenzamide monohydrate], a novel potential antidementia drug, restores the regional cerebral blood flow response abolished by scopolamine but not by HA-966: a positron emission tomography study with unanesthetized
Brain research, Jun-19, Volume: 832, Issue: 1-2
1999
D-cycloserine blocks the effects of ethanol and HA-966 in rats tested in the elevated plus-maze.
Alcoholism, clinical and experimental research, Volume: 21, Issue: 9
1997
EEG seizure activity and behavioral neurotoxicity produced by (+)-MK801, but not the glycine site antagonist L-687,414, in the rat.
Neuropharmacology, Volume: 35, Issue: 4
1996
The glycine B receptor partial agonist, (+)-HA966, enhances induction of antinociception by RP 67580 and CP-99,994.
European journal of pharmacology, Feb-21, Volume: 253, Issue: 1-2
1994
Anticonvulsant activity of antagonists and partial agonists for the NMDA receptor-associated glycine site in the kindling model of epilepsy.
Brain research, Aug-08, Volume: 653, Issue: 1-2
1994
In vivo antagonism of agonist actions at N-methyl-D-aspartate and N-methyl-D-aspartate-associated glycine receptors in mouse cerebellum: studies of 1-hydroxy-3-aminopyrrolidone-2.
Neuropharmacology, Volume: 29, Issue: 7
1990
Glycine, glycinamide and D-serine act as positive modulators of signal transduction at the N-methyl-D-aspartate (NMDA) receptor in vivo: differential effects on mouse cerebellar cyclic guanosine monophosphate levels.
Neuropharmacology, Volume: 29, Issue: 11
1990
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]