Page last updated: 2024-11-10

a 61603

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

Description

A 61603: a potent alpha1-adrenergic receptor agonist; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4038180
CHEMBL ID109783
CHEBI ID103854
SCHEMBL ID8856920
MeSH IDM0249353

Synonyms (19)

Synonym
BRD-A83650191-004-01-0
gtpl480
a61603
NCGC00024968-02
n-[5-(4,5-dihydro-1h-imidazol-2-yl)-2-hydroxy-5,6,7,8-tetrahydro-naphthalen-1-yl]-methanesulfonamide
bdbm50118703
L000090
CHEMBL109783 ,
n-(5-(4,5-dihydro-1h-imidazol-2-yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)methanesulfonamide
a 61603
n-[5-(4,5-dihydro-1h-imidazol-2-yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl]methanesulfonamide
SCHEMBL8856920
a61603;a-61603
methanesulfonamide,n-[5-(4,5-dihydro-1h-imidazol-2-yl)-5,6,7,8-tetrahydro-2-hydroxy-1-naphthalenyl]-,hydrobromide(1:1)
CHEBI:103854
n-[5-(4,5-dihydro-1h-imidazol-2yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl]methanesulphonamide
Q27074075
750531-54-5
AKOS040750020

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Dose-response curves for alpha-adrenoceptor agonists in testosterone-treated animals showed a leftward shift, indicating increased sensitivity of tissue to alpha-adrenoceptor agonists."( Enhancement of alpha-adrenoceptor-mediated responses in prostate of testosterone-treated rat.
Kaul, CL; Ramarao, P; Thiyagarajan, M, 2002
)
0.31
" The α(1D)-adrenoceptor antagonist, BMY-7378 (BMY) blocked noradrenaline-induced responses in the order SO > AC7 ≫ AC14; in contrast, the α(1A)-adrenoceptor antagonist RS-100329 (RS), produced a marginal shift to the right of the dose-response curve to noradrenaline, along with a strong decrease of the maximum pressor effect in the order SO > AC7 = AC14."( Effect of inter-renal aortic coarctation-induced hypertension on function and expression of vascular α(1A)- and α(1D)-adrenoceptors.
Gallardo-Ortiz, IA; Ibarra, M; López-Islas, I; López-Sánchez, P; Terrón, JA, 2012
)
0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
tetralinsCompounds containing a tetralin skeleton.
[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 (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency35.48130.003245.467312,589.2998AID2517
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.03310.00010.807410.0000AID36078
Alpha-1A adrenergic receptorBos taurus (cattle)Ki0.03020.00000.50723.7020AID36463
Alpha-1B adrenergic receptorMesocricetus auratus (golden hamster)Ki2.64680.00002.01679.6000AID37070; AID37185; AID37188
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki1.57270.00000.929610.0000AID36377; AID37070
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki2.90000.00000.970810.0000AID37070
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki2.90000.00000.937510.0000AID37070
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki1.44270.00000.575110.0000AID35598; AID35739; AID35742
Alpha-1A adrenergic receptorHomo sapiens (human)Ki1.34900.00000.272610.0000AID35739
Alpha-1B adrenergic receptorHomo sapiens (human)Ki2.08930.00000.471310.0000AID37185
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.34620.00000.965010.0000AID35739; AID36151; AID37046
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-1A adrenergic receptorHomo sapiens (human)EC50 (µMol)0.00930.00010.50987.1000AID36421
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (74)

Processvia Protein(s)Taxonomy
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
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)
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 (13)

Processvia Protein(s)Taxonomy
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorBos taurus (cattle)
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 (17)

Processvia Protein(s)Taxonomy
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
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)
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 (55)

Assay IDTitleYearJournalArticle
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.
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.
AID36377In vitro binding affinity towards alpha-2B adrenergic receptor of rat neonatal lung in radioligand binding assay2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID60508Percent response towards alpha 1A adrenergic receptor in canine prostate using phenylephrine as control agonist1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
AID234297Selectivity is the ratio of binding affinities of alpha 1A adrenergic receptor to alpha 1b adrenergic receptor1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
AID234283Selectivity is ratio of pKi (binding affinity) of Alpha-1D to that of alpha1A2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID234282Selectivity is ratio of pKi (binding affinity) of alpha-1B receptor to that of alpha-1A receptor.2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID37499Efficacy relative to phenylephrine (PE) constriction of rat spleen containing alpha-1B adrenergic receptor2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID235160Selectivity ratio as the ratio of Ki value towards Alpha1D receptor to that of Alpha1A receptor.2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID36764Efficacy relative to phenylephrine (PE) to constrict tissue containing the alpha-1A adrenergic receptor in rabbit urethra2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID37044Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
AID35742In vitro binding affinity towards alpha-1D adrenergic receptor of rat clone in radioligand binding assay2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID36463Binding affinity towards bovine clonal Alpha-1A adrenergic receptor1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
AID36421Effective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptor2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID37188In vitro binding affinity towards alpha-1B adrenergic receptor of hamster clone in radioligand binding assay2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID37046In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID180025Percent response towards alpha 1A adrenergic receptor in rat vas deferens using phenylephrine as control agonist1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
AID37497Effective concentration in vitro against rat spleen Alpha-1B adrenergic receptor indicates EC50 < 15% at a concentration of 10 uM2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID234280Relative affinities for alpha2B and alpha1A receptors2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID36151Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (0.009 - 0.015)2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID36078In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID41728Dose corresponding to a 5 mmHg increase in Intraurethral pressure (IUP) was determined in vivo in isoflurane anesthetized female beagles2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID180028Percent response towards alpha 1D adrenergic receptor in rat aorta using phenylephrine as control agonist1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
AID234277Selectivity is ratio of efficacy of alpha-1B to that of alpha1A adrenoceptor2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID233243Functional selectivity ratio as the ratio of EC50 value towards Alpha1B receptor to that of Alpha1A receptor.2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID41727Dose corresponding to a 20 mmHg increase in mean arterial pressure (MAP) was determined in vivo in isoflurane anesthetized female beagles2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID233244Functional selectivity ratio as the ratio of EC50 value towards Alpha1D receptor to that of Alpha1A receptor.2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID234278Selectivity is ratio of efficacy of Alpha-1D to that of alpha-1A adrenoceptor2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID234298Selectivity is the ratio of binding affinities of alpha 1A adrenergic receptor to alpha 1d adrenergic receptor1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
AID35739Binding affinity towards rat clonal Alpha-1D adrenergic receptor1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
AID235159Selectivity ratio as the ratio of Ki value towards Alpha1B receptor to that of Alpha1A receptor.2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID35157Functional agonism of the compounds to constrict tissue containing the alpha-1B adrenergic receptor in rat spleen2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID37185Binding affinity towards hamster clonal Alpha-1B adrenergic receptor1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
AID36096Functional agonism of the compounds to constrict tissue containing the alpha-2A adrenergic receptor in rat prostatic vas deferens; NT = not tested2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID35160In vitro agonist potency towards Alpha-1B adrenergic receptor in rat spleen1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
AID59114Uroselectivity was determined by measuring effective dose required for 20 mmHg increase of mean arterial pressure (MAP) in vivo in dog2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID229761Ratio of IUP ED delta5 to that of MAP ED delta202004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID36470In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
AID36766Functional agonism of the compounds to constrict tissue containing the alpha-1A adrenergic receptor in rabbit urethra2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID37036In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
AID35618In vitro agonist potency towards Alpha-1D adrenergic receptor in rat aorta1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
AID196269In vitro percent efficacy of compound was tested in rat spleen2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID35617Functional agonism of the compounds to constrict tissue containing the alpha-1D adrenergic receptor in rat aorta2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID224497In vitro percent efficacy of compound was tested in rabbit urethra2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID37070Binding affinity towards hamster cloned Alpha-1B adrenergic receptor; value ranges from (2.0 -4.4)2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID234281Relative affinities for alpha-2a and alpha-1A receptors2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID35589Efficacy relative to phenylephrine (PE) constrict tissue containing the alpha-1D adrenergic receptor in rat aorta2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID195188In vitro percent efficacy of compound was tested in rat aorta2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID35598Binding affinity towards rat cloned Alpha-1D adrenergic receptor; value ranges from (1.3 -1.6)2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID180026Percent response towards alpha 1B adrenergic receptor in rat spleen using phenylephrine as control agonist1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
AID234457Uroselectivity as the ratio of MAP ED20 to that of IUP ED5.2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID59116Uroselectivity was determined by measuring effective dose required for 5 mmHg increase of intraurethral pressure (IUP) in vivo in dog2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID35586Effective concentration in vitro against rat aorta Alpha-1D adrenergic receptor;* indicates EC50 < 15% at a concentration of 10 uM2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID1345908Human alpha1A-adrenoceptor (Adrenoceptors)1997British journal of pharmacology, Jul, Volume: 121, Issue:6
Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications for alpha1-adrenoceptor classification.
AID1345908Human alpha1A-adrenoceptor (Adrenoceptors)1995The Journal of pharmacology and experimental therapeutics, Jul, Volume: 274, Issue:1
A-61603, a potent alpha 1-adrenergic receptor agonist, selective for the alpha 1A receptor subtype.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (50)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's11 (22.00)18.2507
2000's24 (48.00)29.6817
2010's12 (24.00)24.3611
2020's3 (6.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 15.74

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 Index15.74 (24.57)
Research Supply Index3.95 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (15.74)

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%
Other51 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]