Page last updated: 2024-12-04

2-hydroxysaclofen

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

Description

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

Cross-References

ID SourceID
PubMed CID1564
CHEMBL ID1256573
CHEBI ID111179
SCHEMBL ID340521
MeSH IDM0160863

Synonyms (52)

Synonym
HMS3266E03
BRD-A27924917-001-01-7
gtpl1068
2-hydroxy-s-(-)-saclofen
EU-0100079
2-hydroxysaclofen, >=98% (tlc), solid
LOPAC0_000079
3-amino-2-(4-chlorophenyl)-2-hydroxypropylsulfonic acid
2-hydroxy-saclofen
2-oh-saclofen
beta-(aminomethyl)-4-chloro-beta-hydroxybenzeneethanesulfonic acid
benzeneethanesulfonic acid, beta-(aminomethyl)-4-chloro-beta-hydroxy-
2-hydroxysaclofen
2-hydroxysaclofen, solid
NCGC00024513-03
NCGC00024513-02
NCGC00015077-03
CHEBI:111179
A 6566
( inverted question mark)-3-amino-2-(4-chlorophenyl)-2-hydroxy-propylsulfonic acid
NCGC00015077-05
117354-64-0
3-amino-2-(4-chlorophenyl)-2-hydroxypropane-1-sulfonic acid
HMS3260O19
CHEMBL1256573
CCG-204174
NCGC00015077-04
x5ifr0uf10 ,
unii-x5ifr0uf10
LP00079
AKOS015914257
3-amino-2-(4-chlorophenyl)-2-hydroxy-propane-1-sulfonic acid
SCHEMBL340521
NCGC00260764-01
tox21_500079
(rs)-3-amino-2-(4-chlorophenyl)-2-hydroxypropyl-sulfonic acid
mfcd00069282
J-003609
HY-100812
sr-01000075621
SR-01000075621-1
SR-01000075621-3
DTXSID30922408
benzeneethanesulfonicacid, b-(aminomethyl)-4-chloro-b-hydroxy-
FT-0734558
HMS3675C13
(r)-3-amino-2-(4-chlorophenyl)-2-hydroxypropane-1-sulfonic acid
Q27071902
HMS3411C13
SDCCGSBI-0050067.P002
PD015460
CS-0020454

Research Excerpts

Dosage Studied

The dose-response curve of R-(--)-baclofen for its inhibitory effect on the electrically-induced vasopressor response was shifted to the right. The GABAA-receptor antagonist bicuculline did not have an effect on cocaine self-administration.

ExcerptRelevanceReference
" The dose-response curve of R-(--)-baclofen for its inhibitory effect on the electrically-induced vasopressor response was shifted to the right by the GABAB-receptor antagonist 2-hydroxysaclofen, but was not affected by the GABAA-receptor antagonist bicuculline."( GABAB receptor-mediated inhibition of the neurogenic vasopressor response in the pithed rat.
Kohlenbach, A; Schlicker, E, 1990
)
0.47
" Separate groups of rats received bilateral intra-VTA injections of the GABA-A antagonist picrotoxin (34 ng/side, n = 7; 68 ng/side, n = 8), GABA-A agonist muscimol (14 ng/side, n = 8), GABA-B agonist baclofen (56 ng/side, n = 7; 100 ng/side, n = 6), picrotoxin (68 ng/side) co-injected with the GABA-B antagonist 2-hydroxysaclofen (100 ng/side, n = 7; 2 microg/side, n = 8) or artificial cerebrospinal fluid (aCSF, n = 6) to assess the effects of the various compounds on the cocaine self-administration dose-response curve."( Contribution of ventral tegmental GABA receptors to cocaine self-administration in rats.
Backes, EN; Hemby, SE, 2008
)
0.52
" Finally, in vitro results demonstrated that GABA (ranging from 10 to 50 μg/μL) markedly inhibited preimplantation embryo development in a dose-response manner."( GABA consumption during early pregnancy impairs endometrial receptivity and embryo development in mice.
Cao, K; Liang, H; Luo, W; Tan, D; Tan, Y; Tian, N; Wang, X; Zhang, Q, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine 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 (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency0.01580.004023.8416100.0000AID485290
Microtubule-associated protein tauHomo sapiens (human)Potency3.16230.180013.557439.8107AID1460
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency18.33980.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.00010.540617.639296.1227AID2364; AID2528
chromobox protein homolog 1Homo sapiens (human)Potency0.01060.006026.168889.1251AID488953
M-phase phosphoprotein 8Homo sapiens (human)Potency100.00000.177824.735279.4328AID488949
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (23)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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.
AID1346001Rat GABAB1 (GABAB receptors)1997Nature, Mar-20, Volume: 386, Issue:6622
Expression cloning of GABA(B) receptors uncovers similarity to metabotropic glutamate receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (154)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (2.60)18.7374
1990's94 (61.04)18.2507
2000's29 (18.83)29.6817
2010's19 (12.34)24.3611
2020's8 (5.19)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.69

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index18.69 (24.57)
Research Supply Index5.06 (2.92)
Research Growth Index6.12 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.69)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other157 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]