Page last updated: 2024-11-04

1-hydroxy-3-amino-2-pyrrolidone

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

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

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" These data suggest that despite their brain bioavailability and marked potency at the glycine receptor in vitro, ACC and ACBC are rapidly inactivated and thus have limited in vivo utility."( Neuropharmacological characterization of 1-aminocyclopropane-1-carboxylate and 1-aminocyclobutane-1-carboxylate, ligands of the N-methyl-D-aspartate-associated glycine receptor.
Cler, JA; Compton, RP; Emmett, MR; Iyengar, S; Mick, S; Rao, TS; Sun, ET; Wood, PL, 1990
)
0.28
") injections of HA-966, demonstrating the bioavailability of this glycine receptor antagonist."( 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.
Cler, J; Emmett, MR; Iyengar, S; Mick, S; Oei, E; Rao, TS; Wood, PL, 1990
)
0.28
") did not affect cGMP responses, suggesting poor bioavailability in brain."( Indole-2-carboxylates, novel antagonists of the N-methyl-D-aspartate (NMDA)-associated glycine recognition sites: in vivo characterization.
Cler, JA; Cordi, AA; Dappen, MS; Emmett, MR; Gray, NM; Iyengar, S; Mick, SJ; Monahan, JB; Rao, TS; Wood, PL, 1993
)
0.29

Dosage Studied

ExcerptRelevanceReference
" The icb dose-response data indicated a unimolecular interaction for these compounds."( 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.
Cler, JA; Emmett, MR; Iyengar, S; Mick, SJ; Rao, TS; Wood, PL, 1990
)
0.28
" An evaluation of the parenteral dose-response curve for HA-966, revealed no effect on basal activity within the cerebellum."( 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.
Cler, J; Emmett, MR; Iyengar, S; Mick, S; Oei, E; Rao, TS; Wood, PL, 1990
)
0.28
" In its presence, the dose-response curve for RP 67580 was dose-dependently shifted to the left."( The glycine B receptor partial agonist, (+)-HA966, enhances induction of antinociception by RP 67580 and CP-99,994.
Millan, MJ; Seguin, L, 1994
)
0.29
"05) prevented the increase in the percentage of open-arm entries and the time spent in the open arms of elevated plus-maze test induced by ethanol, exhibiting a U-shaped dose-response curve."( D-cycloserine blocks the effects of ethanol and HA-966 in rats tested in the elevated plus-maze.
Moraes Ferreira, VM; Morato, GS, 1997
)
0.3
" The scopolamine-induced abolishment of rCBF response was restored by the administration of FK960 at relatively wide dosing range from 1 to 1000 microg/kg (i."( 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
Inoue, T; Kakiuchi, T; Matsuoka, N; Nishimura, S; Nishiyama, S; Noda, A; Tsukada, H; Yamazaki, S, 1999
)
0.3
"Systemic opioid dosing until adequate analgesia in neuropathic pain may involve intolerable and untreatable side effects."( The glycine/NMDA receptor antagonist (+)-HA966 enhances the peripheral effect of morphine in neuropathic rats.
Christensen, D; Kayser, V; Martinez, V, 2002
)
0.31
" (+)-HA-966 was evaluated as pretreatment on a complete dose-response for cocaine self-administration."( Effects on cocaine and food self-administration of (+)-HA-966, a partial agonist at the glycine/NMDA modulatory site, in rats.
Carnovali, F; Cervo, L; Cocco, A, 2004
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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]

Market Indicators

Research Demand Index: 9.35

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index9.35 (24.57)
Research Supply Index5.29 (2.92)
Research Growth Index4.64 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (9.35)

All Compounds (24.57)

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]