Page last updated: 2024-11-06

etisulergine

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

Description

etisulergine: RN given refers to parent cpd; CQ 32084 is synonomous to HCl; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID68847
CHEMBL ID38992
SCHEMBL ID219311
MeSH IDM0099256

Synonyms (18)

Synonym
etisulergine
CHEMBL38992
etisulergina [inn-spanish]
64795-23-9
n,n-diethyl-n'-(6-methylergolin-8alpha-yl)sulfamide
unii-28n73q6o7y
etisulerginum
cq 32-084
etisulerginum [inn-latin]
etisulergina
28n73q6o7y ,
etisulergine [inn]
SCHEMBL219311
n,n-diethyl-n'-(6-methylergolin-8.alpha.-yl)sulfamide
bdbm50225361
Q27254335
(6ar,9s,10ar)-9-(diethylsulfamoylamino)-7-methyl-6,6a,8,9,10,10a-hexahydro-4h-indolo[4,3-fg]quinoline
DTXSID101024323
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (20)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC50 (µMol)5.00000.00040.629810.0000AID203936; AID203937
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC50 (µMol)5.00000.00040.908610.0000AID203936; AID203937
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)3.30000.00021.874210.0000AID32964
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)5.00000.00031.38338.4000AID203936; AID203937
D(2) dopamine receptorBos taurus (cattle)IC50 (µMol)0.08200.00100.79948.0000AID62437; AID62438; AID62441; AID62442
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)3.30000.00021.270410.0000AID32964
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC50 (µMol)5.00000.00051.48357.8000AID203936; AID203937
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC50 (µMol)5.00000.00311.73607.8000AID203936; AID203937
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC50 (µMol)5.00000.00501.79627.8000AID203936; AID203937
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC50 (µMol)5.00000.00040.615610.0000AID203936; AID203937
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00501.50894.6000AID203936; AID203937
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00501.42824.6000AID203936; AID203937
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)IC50 (µMol)5.00000.00501.35984.6000AID203936; AID203937
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)IC50 (µMol)5.00000.00501.35984.6000AID203936; AID203937
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)IC50 (µMol)5.00000.00021.13514.6000AID203936; AID203937
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)3.30000.00001.819410.0000AID32964
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00501.35524.6000AID203936; AID203937
DBos taurus (cattle)IC50 (µMol)0.08200.00100.47208.0000AID62437; AID62438; AID62441; AID62442
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC50 (µMol)5.00000.00030.70285.3660AID203936
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)IC50 (µMol)5.00000.00041.17424.6000AID203936; AID203937
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (11)

Processvia Protein(s)Taxonomy
synaptic transmission, dopaminergicD(2) dopamine receptorBos taurus (cattle)
negative regulation of prolactin secretionD(2) dopamine receptorBos taurus (cattle)
negative regulation of lactationD(2) dopamine receptorBos taurus (cattle)
positive regulation of mammary gland involutionD(2) dopamine receptorBos taurus (cattle)
hyaloid vascular plexus regressionD(2) dopamine receptorBos taurus (cattle)
synaptic transmission, dopaminergicDBos taurus (cattle)
vasodilationDBos taurus (cattle)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
Golgi membraneD(2) dopamine receptorBos taurus (cattle)
endoplasmic reticulum membraneDBos taurus (cattle)
dendritic spineDBos taurus (cattle)
ciliary membraneDBos taurus (cattle)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (21)

Assay IDTitleYearJournalArticle
AID62310Dopamine receptor binding affinity by displacing the radioligand [3H]-dopamine from dopamine receptor.1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Structure-activity relationships of dopaminergic 5-hydroxy-2-aminotetralin derivatives with functionalized N-alkyl substituents.
AID203935In vitro inhibitory activity against serotonin receptor from rat frontal cortex using [3H]spiperone as radioligand1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine.
AID62430Dopamine receptor binding affinity by displacing the radioligand [3H]spiroperidol from dopamine receptor.1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Structure-activity relationships of dopaminergic 5-hydroxy-2-aminotetralin derivatives with functionalized N-alkyl substituents.
AID182642Compound was evaluated for the in vivo inhibition of basal prolactin for a time 4 hr after injection in male rats1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide.
AID62438In vitro inhibitory activity against dopamine receptor from calf caudate using [3H]spiperone as radioligand1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine.
AID32964In vitro inhibitory activity was evaluated against,[3H]WB 4101 whole rat brain alpha 1-adrenoceptor1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide.
AID36920In vitro inhibitory activity was evaluated against,[3H]clonidine (Clon) rat brain minus cerebellum Alpha-2 adrenergic receptor1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide.
AID191322Compound was evaluated for the contralateral turning in 6-hydroxy-dopamine-lesioned rats administered intraperitoneally at the dose 1 mg/kg1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Structure-activity relationships of dopaminergic 5-hydroxy-2-aminotetralin derivatives with functionalized N-alkyl substituents.
AID203936In vitro inhibitory activity against serotonin receptor from whole rat brain using [3H]5-HT as radioligand1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine.
AID174604Compound was evaluated for the contralateral turning in 6-hydroxy-dopamine-lesioned rats administered intraperitoneally at the dose 1 mg/kg1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Structure-activity relationships of dopaminergic 5-hydroxy-2-aminotetralin derivatives with functionalized N-alkyl substituents.
AID62442In vitro inhibitory activity was evaluated against,[3H]spiperone calf caudate (SPC) dopamine receptor1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide.
AID182951In vivo inhibitory activity against ovum implantation in female rat after subcutaneous administration1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine.
AID182949In vivo inhibitory activity against basal prolactin in male rat after subcutaneous administration1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine.
AID62441In vitro inhibitory activity was evaluated against,[3H]dopamine (DA),calf caudate dopamine receptor1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide.
AID203938In vitro inhibitory activity was evaluated against,[3H]spiperone rat frontal cortex (SPFC) serotonin receptor1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide.
AID203937In vitro inhibitory activity was evaluated against,[3H]serotonin (5-HT) whole rat brain serotonin receptor1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide.
AID36861In vitro inhibitory activity against alpha-1 adrenergic receptor from whole rat brain using [3H]WB-4101 as radioligand1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine.
AID185915Compound was evaluated for the contralateral turning in 6-hydroxy-dopamine-lesioned rats administered intraperitoneally at the dose 1 mg/kg1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Structure-activity relationships of dopaminergic 5-hydroxy-2-aminotetralin derivatives with functionalized N-alkyl substituents.
AID182954In vivo inhibitory against lactation in female rat after peroral administration1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine.
AID62437In vitro inhibitory activity against dopamine receptor from calf caudate using [3H]dopamine as radioligand1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine.
AID36919In vitro inhibitory activity against alpha-2 adrenergic receptor from rat brain minus cerebellum using [3H]clonidine as radioligand1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-199013 (86.67)18.7374
1990's2 (13.33)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)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 (%)
Trials1 (6.67%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other14 (93.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]