Page last updated: 2024-11-08

abanoquil

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

Cross-References

ID SourceID
PubMed CID164089
CHEMBL ID324090
SCHEMBL ID528781
MeSH IDM0163194

Synonyms (25)

Synonym
bdbm50033109
2-(6,7-dimethoxy-3,4-dihydro-1h-isoquinolin-2-yl)-6,7-dimethoxy-quinolin-4-ylamine
abanoquil
abanoquil [inn:ban]
L002329
90402-40-7
CHEMBL324090 ,
2-(6,7-dimethoxy-3,4-dihydro-1h-isoquinolin-2-yl)-6,7-dimethoxyquinolin-4-amine
4-amino-2-(3,4-dihydro-6,7-dimethoxy-2(1h)-isoquinolyl)-6,7-dimethoxyquinoline
4-amin-2-(3,4-dihydro-6,7-dimethoxy-2(1h)-isoquinolyl)-6,7-dimethoxyquinoline
f738mwy53l ,
unii-f738mwy53l
uk 52046
2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1h)-yl)-6,7-dimethoxyquinolin-4-amine
abanoquil [inn]
SCHEMBL528781
DTXSID40238163
ANZIISNSHPKVRV-UHFFFAOYSA-N
2-(6,7-dimethoxy-3,4-dihydro-1h-isoquinolin-2-yl) -6,7-dimethoxyquinolin-4-ylamine
Q4118279
MS-26658
CS-0026151
HY-106612
2-(6,7-dimethoxy-3,4-dihydro-1h-isoquinolin-2-yl)-6,7-dimethoxy-quinolin-4-amine
AKOS040747728

Research Excerpts

Overview

Abanoquil (UK 52,046) is a novel, quinoline-derivative, alpha 1-adrenoceptor antagonist. It possesses antiarrhythmic activity at doses which have little or no effect on blood pressure.

ExcerptReferenceRelevance
"1. Abanoquil (UK 52,046) is a novel, quinoline-derivative, alpha 1-adrenoceptor antagonist which, on the basis of animal studies, possesses antiarrhythmic activity at doses which have little or no effect on blood pressure. "( Studies with abanoquil (UK-52,046) a novel quinoline alpha 1-adrenoceptor antagonist: I. Effects on blood pressure, heart rate and pressor responsiveness in normotensive subjects.
Elliott, HL; Howie, CA; Reid, JL; Schafers, RF, 1991
)
1.27

Pharmacokinetics

ExcerptReferenceRelevance
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Dosage Studied

ExcerptRelevanceReference
" The doses of phenylephrine required to increase systolic BP by 20 mm Hg (PS20) were calculated using a quadratic fit to the individual dose-response curves."( Dose-dependent alpha 1-adrenoceptor antagonist activity of the anti-arrhythmic drug, abanoquil (UK-52,046), without reduction in blood pressure in man.
Guy, S; Harron, DW; Shanks, RG; Tham, TC, 1992
)
0.51
" (as a bolus or by increments) produced significant alpha 1-adrenoceptor antagonism (with rightward shifts of more than two-fold in the phenylephrine pressor dose-response curves) but no significant effects on supine or erect blood pressure and heart rate."( Studies with abanoquil (UK-52,046) a novel quinoline alpha 1-adrenoceptor antagonist: I. Effects on blood pressure, heart rate and pressor responsiveness in normotensive subjects.
Elliott, HL; Howie, CA; Reid, JL; Schafers, RF, 1991
)
0.65
"1) of the pressor dose-response curve for diastolic blood pressure."( Studies with abanoquil (UK-52,046) a novel quinoline alpha 1-adrenoceptor antagonist: II. Duration of action, pharmacokinetics and concentration-effect relationships in normotensive subjects.
Elliott, HL; Meredith, PA; Miller, SH; Reid, JL; Schafers, RF, 1991
)
0.65
" At rest the haemodynamic effects to two dose-response regimens were determined."( Haemodynamic dose-response effects of UK-52,046 in ischaemic disease with or without impaired left ventricular function.
Silke, B; Taylor, SH; Tham, TC; Verma, SP; Zezulka, AV, 1990
)
0.28
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (8)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-1A adrenergic receptorBos taurus (cattle)Ki0.00000.00000.50723.7020AID36460
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.00000.00000.929610.0000AID35328
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.00000.00000.970810.0000AID35328
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.00000.00000.937510.0000AID35328
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.00000.00000.575110.0000AID35603
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.00000.00000.360910.0000AID35328
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.00000.00000.272610.0000AID36618
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.00010.00000.471310.0000AID37183; AID37335
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (37)

Processvia Protein(s)Taxonomy
regulation of vasoconstrictionAlpha-1A adrenergic receptorBos taurus (cattle)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorBos taurus (cattle)
regulation of cardiac muscle contractionAlpha-1A adrenergic receptorBos taurus (cattle)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
protein heterodimerization activityAlpha-1A adrenergic receptorBos taurus (cattle)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
nucleusAlpha-1A adrenergic receptorBos taurus (cattle)
cytoplasmAlpha-1A adrenergic receptorBos taurus (cattle)
plasma membraneAlpha-1A adrenergic receptorBos taurus (cattle)
caveolaAlpha-1A adrenergic receptorBos taurus (cattle)
nuclear membraneAlpha-1A adrenergic receptorBos taurus (cattle)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID35328Binding affinity against Alpha-1D adrenergic receptor, from human clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID35603Binding affinity against Alpha-1D adrenergic receptor, from rat clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID239800Binding affinity for alpha 1b adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID37183Binding affinity against Alpha-1B adrenergic receptor from hamster clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID36460Binding affinity against Alpha-1A adrenergic receptor from bovine clone1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID37335Binding affinity against Alpha-1B adrenergic receptor from human clone1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID239799Binding affinity for alpha 1a adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID36618Binding affinity against Alpha-1A adrenergic receptor from human clone1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID239801Binding affinity for alpha 1d adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (21)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902 (9.52)18.7374
1990's16 (76.19)18.2507
2000's3 (14.29)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]

Market Indicators

Research Demand Index: 11.86

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 Index11.86 (24.57)
Research Supply Index3.33 (2.92)
Research Growth Index5.19 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.86)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (22.73%)5.53%
Reviews1 (4.55%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other16 (72.73%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]