Page last updated: 2024-11-10

ly 53857

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

Description

LY 53857: RN given refers to maleate[1:1](8beta)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3034814
CHEMBL ID1356280
MeSH IDM0101813
PubMed CID6437377
CHEMBL ID1399645
SCHEMBL ID2970215
MeSH IDM0101813

Synonyms (48)

Synonym
gtpl183
ly53857
3-hydroxybutan-2-yl (2r,4r,7r)-6-methyl-11-(propan-2-yl)-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(16),9,12,14-tetraene-4-carboxylate
ly-53,857
BIOMOL-NT_000165
LOPAC0_000721
BPBIO1_000595
NCGC00163176-01
CCG-204806
CHEMBL1356280
ergoline-8.beta.-carboxylic acid, 1-isopropyl-6-methyl-, 2-hydroxy-1-methylpropyl ester
4-isopropyl-7-methyl-9-(2-hydroxy-1-methylpropoxycarbonyl)-4,6,6.alpha.,7,8,9,10,10.alpha.-octahydroindolo(4,3-fg)quinoline
ergoline-8-carboxylic acid, 6-methyl-1-(1-methylethyl)-, 2-hydroxy-1-methylpropyl ester, (8.beta.)-
32896-53-0
4-isopropyl-7-methyl-9-(2-hydroxy-1-methylpropoxycarbonyl)-4,6,6alpha,7,8,9,10,10alpha-octahydroindolo(4,3-fg)quinoline
ergoline-8-carboxylic acid, 6-methyl-1-(1-methylethyl)-, 2-hydroxy-1-methylpropyl ester, (8beta)-
ly-53857 free base
ergoline-8beta-carboxylic acid, 1-isopropyl-6-methyl-, 2-hydroxy-1-methylpropyl ester
unii-ok43yc00i7
ok43yc00i7 ,
6-methyl-1-(1-methylethyl)ergoline-8beta-carboxylic acid 2-hydroxy-1-methylpropyl ester
Q27083222
3-hydroxybutan-2-yl (6ar,9r,10ar)-7-methyl-4-propan-2-yl-6,6a,8,9,10,10a-hexahydroindolo[4,3-fg]quinoline-9-carboxylate
AKOS040752793
EU-0100721
ergoline-8-carboxylic acid, 6-methyl-1-(1-methylethyl)-, 2-hydroxy-1-methylpropyl ester, (8beta)-, (z)-2-butenedioate (1:1) (salt)
lilly 53857
ly-53857
ly 53857
ly-53,857 maleate
NCGC00094069-01
ergoline-8beta-carboxylic acid 2-hydroxy-1-methylpropyl ester maleate
L-107
6-methyl-1-(1-methylethyl)-
60634-51-7
l37tvx7u5m ,
ly 53,857
unii-l37tvx7u5m
SCHEMBL2970215
CHEMBL1399645
ergoline-8-carboxylic acid, 6-methyl-1-(1-methylethyl)-, 2-hydroxy-1-methylpropyl ester, (8.beta.)-, (2z)-2-butenedioate (1:1) (salt)
4-isopropyl-7-methyl-9-(2-hydroxy-1-methylpropoxycarbonyl)-4,6,6.alpha.,7,8,9,10,10.alpha.-octahydroindolo(4,3-fg)quinoline maleate
ergoline-8-carboxylic acid, 6-methyl-1-(1-methylethyl)-, 2-hydroxy-1-methylpropyl ester, (8.beta.)-, (2z)-2-butenedioate (1:1)
sr-01000075553
SR-01000075553-1
(z)-but-2-enedioic acid;3-hydroxybutan-2-yl (6ar,9r,10ar)-7-methyl-4-propan-2-yl-6,6a,8,9,10,10a-hexahydroindolo[4,3-fg]quinoline-9-carboxylate
Q27282651
AKOS040748823

Research Excerpts

Dosage Studied

LY 53857 shifts the pressor dose-response curve to 5-HT in a parallel way at low doses but in a noncompetitive way at higher doses.

ExcerptRelevanceReference
" However, LY 53857 differs from ketanserin in that it shifts the pressor dose-response curve to 5-HT in a parallel way at low doses but in a noncompetitive way at higher doses."( Comparison between ketanserin and LY 53857 on vascular and cardiac 5-HT2 and alpha 1-adrenergic receptors in the pithed rat.
Chaouche-Teyara, K; Cherqui, C; Dabiré, H; Fournier, B; Schmitt, H,
)
0.13
" A maximally effective dose of LY53857 (1 mg/kg) produced larger shifts of the dose-response curves to serotonin, 5-methoxytryptamine and alpha-methyl-serotonin than did a maximally effective dose of ketanserin (1 mg/kg)."( A pharmacologic examination of receptors mediating serotonin-induced bronchoconstriction in the anesthetized guinea pig.
Buckner, CK; Dea, D; Krell, RD; Liberati, N, 1991
)
0.28
" Cumulative dose-response curves were constructed for either cinanserin or 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) in animals that had received a maximal hypotensive dose of prazosin that had, in addition to decreasing blood pressure, decreased heart rate and background activity in all three nerves."( Are drugs that act both on serotonin receptors and alpha 1-adrenoceptors more potent hypotensive agents than those that act only on alpha 1-adrenoceptors?
Ramage, AG, 1988
)
0.27
" Several 5-HT agonists were administered, in a dose-response fashion, to conscious rats and the effect on the levels of prolactin in plasma was measured."( Effect of selective serotonin (5-HT) agonists and 5-HT2 antagonist on prolactin secretion.
Bethea, CL; Lorens, SA; Urban, JH; Van de Kar, LD, 1989
)
0.28
" In rats with chemical lesions of serotonergic neurons the dose-response curves of RU 24969 for PRA and PRC as well as corticotropin, corticosterone and prolactin shifted to the left, suggesting functional up-regulation of postsynaptic 5-HT receptors."( Neuroendocrine evidence for denervation supersensitivity of serotonin receptors: effects of the 5-HT agonist RU 24969 on corticotropin, corticosterone, prolactin and renin secretion.
Bethea, CL; Bonadonna, AM; Carnes, M; Kunimoto, K; Maslowski, RJ; Piechowski, RA; Rittenhouse, PA; Van de Kar, LD, 1989
)
0.28
" LY 53857, significantly and dose dependently shifted to the right the dose-response curves to both 5-HT and DOI."( Characterization of DOI, a putative 5-HT2 receptor agonist in the rat.
Chaouche-Teyara, K; Cherqui, C; Dabiré, H; Fournier, B; Laubie, M; Schmitt, H, 1989
)
0.28
" Dose-response relationships were established for 5-HT in experiments in which each mouse was treated with a single dose of 5-HT without antagonist or after LY53857."( Serotonin-induced pulmonary responses are mediated by the 5-HT2 receptor in the mouse.
Cohen, ML; Drazen, JM; Martin, TR, 1994
)
0.29
"05) by the greatest dosage of LY 53,857 (LY: 5-HT1C and 5-HT2 antagonist) (1."( Serotonergic agonists and antagonists affect endurance performance in the rat.
Ahlborn, EN; Bailey, SP; Davis, JM, 1993
)
0.29
"0 mg/kg) in combination with m-CPP produced a slight leftward shift of the dose-response curve of m-CPP."( Meta-chlorophenylpiperazine induced changes in locomotor activity are mediated by 5-HT1 as well as 5-HT2C receptors in mice.
Gleason, SD; Shannon, HE, 1998
)
0.3
" Dose-response curves were obtained for the effects of several 5-HT2 receptor antagonists on response magnitude."( Effect of 5-HT2 receptor antagonists on a cranial nerve reflex in the rabbit: evidence for inverse agonism.
Harvey, JA; Hood, H; Romano, AG; Welsh, SE, 1999
)
0.3
" To probe the role of 5-HT2R in this increased amplitude, dose-response studies were done with the selective antagonists mianserin or LY53857 and the 5-HT2R agonist (+/-)-1-(2,5-Dimethoxy-4-iodophenyl)-2-aminopropane hydrochloride (DOI)."( Up-regulation of 5-HT2 receptors is involved in the increased H-reflex amplitude after contusive spinal cord injury.
Johnson, CS; Lee, JK; Wrathall, JR, 2007
)
0.34
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (14)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency45.85770.125919.1169125.8920AID2549; AID504841
phosphopantetheinyl transferaseBacillus subtilisPotency39.81070.141337.9142100.0000AID1490
TDP1 proteinHomo sapiens (human)Potency3.28600.000811.382244.6684AID686978; AID686979
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency1.77830.011212.4002100.0000AID1030
67.9K proteinVaccinia virusPotency13.35730.00018.4406100.0000AID720579; AID720580
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency50.11870.036619.637650.1187AID2112
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency19.95260.251215.843239.8107AID504327
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency39.81070.177814.390939.8107AID2147
Chain A, Ferritin light chainEquus caballus (horse)Potency44.66845.623417.292931.6228AID2323
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.12590.100020.879379.4328AID588453
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency44.66840.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency8.91250.540617.639296.1227AID2364; AID2528
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency79.43280.010323.856763.0957AID2662
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency7.94330.00419.962528.1838AID493199
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (11)

Assay IDTitleYearJournalArticle
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.
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.
AID624218Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2B1998Naunyn-Schmiedeberg's archives of pharmacology, Jan, Volume: 357, Issue:1
[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor.
AID624228Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT2B1993Molecular pharmacology, Mar, Volume: 43, Issue:3
Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor.
AID1346919Rat 5-HT2A receptor (5-Hydroxytryptamine receptors)1994Molecular pharmacology, Feb, Volume: 45, Issue:2
Species variations in transmembrane region V of the 5-hydroxytryptamine type 2A receptor alter the structure-activity relationship of certain ergolines and tryptamines.
AID1346903Rat 5-HT2B receptor (5-Hydroxytryptamine receptors)1993Molecular pharmacology, Mar, Volume: 43, Issue:3
Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor.
AID1346867Human 5-HT2B receptor (5-Hydroxytryptamine receptors)1998Naunyn-Schmiedeberg's archives of pharmacology, Jan, Volume: 357, Issue:1
[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor.
AID624222Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT2A1994Molecular pharmacology, Feb, Volume: 45, Issue:2
Species variations in transmembrane region V of the 5-hydroxytryptamine type 2A receptor alter the structure-activity relationship of certain ergolines and tryptamines.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)1994Molecular pharmacology, Feb, Volume: 45, Issue:2
Species variations in transmembrane region V of the 5-hydroxytryptamine type 2A receptor alter the structure-activity relationship of certain ergolines and tryptamines.
AID624223Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A1994Molecular pharmacology, Feb, Volume: 45, Issue:2
Species variations in transmembrane region V of the 5-hydroxytryptamine type 2A receptor alter the structure-activity relationship of certain ergolines and tryptamines.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (132)

TimeframeStudies, This Drug (%)All Drugs %
pre-199038 (28.79)18.7374
1990's69 (52.27)18.2507
2000's20 (15.15)29.6817
2010's3 (2.27)24.3611
2020's2 (1.52)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.56

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 Index12.56 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Reviews1 (0.75%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
Other132 (99.25%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]