Compounds > a 61603
Page last updated: 2024-08-01 03:20:30

a 61603

Description

A 61603: a potent alpha1-adrenergic receptor agonist; structure given in first source [MeSH]

N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl]methanesulfonamide : no description available [CHeBI]

Cross-References

ID SourceID
PubMed CID4038180
CHEMBL ID109783
SCHEMBL ID8856920
CHEBI ID103854
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

Drug Classes (1)

ClassDescription
tetralinsCompounds containing a tetralin skeleton.

Protein Targets (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency35.4813AID2517

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.0331AID36078
Alpha-1A adrenergic receptorBos taurus (cattle)Ki0.0302AID36463
Alpha-1B adrenergic receptorMesocricetus auratus (golden hamster)Ki2.6468AID37070; AID37185; AID37188
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki1.5727AID36377; AID37070
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki2.9000AID37070
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki2.9000AID37070
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki1.4427AID35598; AID35739; AID35742
Alpha-1A adrenergic receptorHomo sapiens (human)Ki1.3490AID35739
Alpha-1B adrenergic receptorHomo sapiens (human)Ki2.0893AID37185
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.3462AID35739; AID36151; AID37046

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Alpha-1A adrenergic receptorHomo sapiens (human)EC500.0093AID36421

Bioassays (54)

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
ISSN: 1091-6490		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
ISSN: 2211-1247		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0022-2623		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
ISSN: 0007-1188		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
ISSN: 0022-3565		A-61603, a potent alpha 1-adrenergic receptor agonist, selective for the alpha 1A receptor subtype.

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

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%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
7-hydroxy-2-n,n-dipropylaminotetralin
0
tetralins00low000000
8-hydroxy-2-(di-n-propylamino)tetralin
0
phenols;
tertiary amino compound;
tetralins		serotonergic antagonist00low000000
2-(n-phenethyl-n-propyl)amino-5-hydroxytetralin
0
tetralins00low000000
am 580
0
amidobenzoic acid;
tetralins		antineoplastic agent;
retinoic acid receptor alpha/beta agonist		00low000000
liranaftate
0
tetralins00low000000
nadolol
0
tetralins00low000000
tramazoline
0
tetralins00low000000
tetralin
0
ortho-fused bicyclic hydrocarbon;
tetralins		00low000000
6-Methoxy-1-tetralone
0
tetralins00low000000
2-aminotetralin
0
tetralins00low000000
be 2254
0
tetralins00low000000
5,6-dihydroxy-2-dimethylaminotetralin
0
tetralins00low000000
n 0437, (-)-isomer
0
tetralins00low000000
mibefradil
0
tetralinsT-type calcium channel blocker00low000000
5,6,7,8-tetrahydro-1-naphthol
0
tetralins00low000000
sertraline
0
dichlorobenzene;
secondary amino compound;
tetralins		antidepressant;
serotonin uptake inhibitor		00low000000
acetyl methyl tetramethyl tetralin
0
tetralins00low000000
tamibarotene
0
dicarboxylic acid monoamide;
retinoid;
tetralins		antineoplastic agent;
retinoic acid receptor alpha/beta agonist		00low000000
aj 76
0
secondary amino compound;
tetralins		dopaminergic antagonist00low000000
oxoline
0
aromatic ketone;
tetralins		geroprotector00low000000
lasofoxifene
0
aromatic ether;
N-alkylpyrrolidine;
naphthols;
tetralins		antineoplastic agent;
bone density conservation agent;
cardioprotective agent;
estrogen receptor agonist;
estrogen receptor antagonist		00low000000
isoshinanolone
0
tetralins00low000000
3-(4-chlorophenyl)-2-methyl-3,3a,4,5-tetrahydrobenzo[g]indazole
0
tetralins00low000000
N1-(5-oxo-5,6,7,8-tetrahydronaphthalen-2-yl)acetamide
0
tetralins00low000000
eptazocine
0
tetralins00low000000
1-(1H-imidazol-5-ylsulfonyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-piperidinecarboxamide
0
tetralins00low000000
4-oxo-4-[5-(1,2,3,4-tetrahydronaphthalen-1-ylsulfamoyl)-2,3-dihydroindol-1-yl]butanoic acid
0
tetralins00low000000
2-phenoxy-N-[5-(5,6,7,8-tetrahydronaphthalen-2-yl)-1,3,4-oxadiazol-2-yl]acetamide
0
tetralins00low000000
1-(phenylmethyl)-3-(1,2,3,4-tetrahydronaphthalen-1-yl)thiourea
0
tetralins00low000000
4-phenyl-2-propionamidotetraline
0
tetralins00low000000
N-[5-(5,6,7,8-tetrahydronaphthalen-2-yl)-1,3,4-oxadiazol-2-yl]cyclohexanecarboxamide
0
tetralins00low000000
2-chloro-N-[5-(5,6,7,8-tetrahydronaphthalen-2-yl)-1,3,4-oxadiazol-2-yl]benzamide
0
tetralins00low000000
2-(4-chlorophenoxy)-N-[5-(5,6,7,8-tetrahydronaphthalen-2-yl)-1,3,4-oxadiazol-2-yl]acetamide
0
tetralins00low000000
2,6-difluoro-N-[5-(5,6,7,8-tetrahydronaphthalen-2-yl)-1,3,4-oxadiazol-2-yl]benzamide
0
tetralins00low000000
2,4-dichloro-N-[5-(5,6,7,8-tetrahydronaphthalen-2-yl)-1,3,4-oxadiazol-2-yl]benzamide
0
tetralins00low000000
8-methoxy-2-propionamidotetralin
0
tetralins00low000000
sr 59230a
0
tetralins00low000000
7-hydroxy-2-(n-n-propyl-n-(3-iodo-2'-propenyl)-amino)tetralin
0
organoiodine compound;
phenols;
tertiary amino compound;
tetralins		dopamine agonist00low000000
pseudopteroxazole
0
tetralinsmetabolite00low000000
8-hydroxy-2-(di-n-propylamino)tetralin, (r)-isomer
0
tetralins00low000000
uh 232
0
tetralins00low000000
4-[(2,1,3-benzothiadiazol-4-ylsulfonylamino)methyl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-cyclohexanecarboxamide
0
tetralins00low000000
nepicastat
0
1,3-dihydroimidazole-2-thiones;
organofluorine compound;
primary amino compound;
tetralins		EC 1.14.17.1 (dopamine beta-monooxygenase) inhibitor00low000000
NNC 55-0396 (free base)
0
benzimidazoles;
cyclopropanecarboxylate ester;
organofluorine compound;
tertiary amino compound;
tetralins		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
neuroprotective agent;
potassium channel blocker;
T-type calcium channel blocker		00low000000
(S)-Isosclerone
0
tetralins00low000000
PB28
0
aromatic ether;
piperazines;
tetralins		anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
sigma-2 receptor agonist		00low000000
(+)-lyoniresinol-3-alpha-O-beta-D-glucopyranoside
0
beta-D-glucoside;
dimethoxybenzene;
lignan;
monosaccharide derivative;
polyphenol;
primary alcohol;
tetralins		antibacterial agent;
antifungal agent;
metabolite		00low000000
eptazocine hydrobromide
0
tetralins00low000000
lyoniresinol
0
dimethoxybenzene;
lignan;
polyphenol;
primary alcohol;
tetralins		antineoplastic agent;
metabolite		00low000000
N-[2-methyl-5-(2-thiazolo[5,4-b]pyridinyl)phenyl]-5,6,7,8-tetrahydronaphthalene-2-sulfonamide
0
tetralins00low000000
N-methyl-N-(3-pyridinylmethyl)-5-(5,6,7,8-tetrahydronaphthalen-2-yloxymethyl)-3-isoxazolecarboxamide
0
tetralins00low000000
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
oxymetazoline
1
carboxamidine;
imidazolines;
phenols		alpha-adrenergic agonist;
nasal decongestant;
sympathomimetic agent;
vasoconstrictor agent		1996199628.0low001000
phenylpropanolamine
1
2004200420.0high000100
prazosin
1
aromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor		1997199727.0low001000
5-methylurapidil
1
1997199727.0low001000
wb 4101
1
aromatic ether;
benzodioxine;
secondary amino compound		alpha-adrenergic antagonist1997199727.0low001000
phenylephrine
2
phenols;
phenylethanolamines;
secondary amino compound		alpha-adrenergic agonist;
cardiotonic drug;
mydriatic agent;
nasal decongestant;
protective agent;
sympathomimetic agent;
vasoconstrictor agent		1996199727.5low002000
phenylpropanolamine
1
amphetamines;
phenethylamine alkaloid		plant metabolite2002200222.0low000100
indoramin
1
tryptamines1997199727.0low001000
st 1059
2
aromatic ether;
primary amino compound;
secondary alcohol		alpha-adrenergic agonist;
sympathomimetic agent;
vasoconstrictor agent		2002200421.0medium000200
niguldipine
1
diarylmethane1997199727.0low001000
tamsulosin
1
5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamidealpha-adrenergic antagonist;
antineoplastic agent		1997199727.0low001000
rec 15-2739
1
1997199727.0low001000
rs 17053
1
indoles1997199727.0low001000
abt 866
2
2002200421.0high000200
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
gamma-aminobutyric acid
1
amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid		human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule		2004200420.0low000100
thymine
3
pyrimidine nucleobase;
pyrimidone		Escherichia coli metabolite;
human metabolite;
mouse metabolite		2006201215.7low000210
2-amino-5-phosphonovalerate
1
non-proteinogenic alpha-amino acidNMDA receptor antagonist2004200420.0low000100
bisindolylmaleimide i
1
2000200024.0low001000
buspirone
1
azaspiro compound;
N-alkylpiperazine;
N-arylpiperazine;
organic heteropolycyclic compound;
piperidones;
pyrimidines		anxiolytic drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
sedative;
serotonergic agonist		2007200717.0low000100
chelerythrine
1
benzophenanthridine alkaloid;
organic cation		antibacterial agent;
antineoplastic agent;
EC 2.7.11.13 (protein kinase C) inhibitor		2007200717.0low000100
cirazoline
2
aromatic ether2003201117.0low000110
clonidine
6
clonidine;
imidazoline		1997200723.5low003300
isoproterenol
2
catechols;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
sympathomimetic agent		2002201814.0low000110
methiothepin
1
aryl sulfide;
dibenzothiepine;
N-alkylpiperazine;
tertiary amino compound		antipsychotic agent;
dopaminergic antagonist;
geroprotector;
serotonergic antagonist		2007200717.0low000100
nifedipine
2
C-nitro compound;
dihydropyridine;
methyl ester		calcium channel blocker;
human metabolite;
tocolytic agent;
vasodilator agent		1999201915.0low001010
oxymetazoline
2
carboxamidine;
imidazolines;
phenols		alpha-adrenergic agonist;
nasal decongestant;
sympathomimetic agent;
vasoconstrictor agent		2003200719.0low000200
pd 98059
1
aromatic amine;
monomethoxyflavone		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector		2000200024.0low001000
phenoxybenzamine
1
aromatic amine2003200321.0low000100
potassium chloride
2
inorganic chloride;
inorganic potassium salt;
potassium salt		fertilizer2007200717.0low000200
szl 49
1
2003200321.0low000100
prazosin
16
aromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor		1997201521.4medium007810
propranolol
2
naphthalenes;
propanolamine;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic		1998200423.0low001100
ritanserin
1
organofluorine compound;
piperidines;
thiazolopyrimidine		antidepressant;
antipsychotic agent;
anxiolytic drug;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist		2007200717.0low000100
5-methylurapidil
6
1996200723.2low002400
wb 4101
7
aromatic ether;
benzodioxine;
secondary amino compound		alpha-adrenergic antagonist1997200823.4low004300
reserpine
1
alkaloid ester;
methyl ester;
yohimban alkaloid		adrenergic uptake inhibitor;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
first generation antipsychotic;
plant metabolite;
xenobiotic		2007200717.0low000100
dibenzylchlorethamine
1
2003200321.0low000100
carbachol
1
ammonium salt;
carbamate ester		cardiotonic drug;
miotic;
muscarinic agonist;
nicotinic acetylcholine receptor agonist;
non-narcotic analgesic		2006200618.0low000100
phenylephrine
23
phenols;
phenylethanolamines;
secondary amino compound		alpha-adrenergic agonist;
cardiotonic drug;
mydriatic agent;
nasal decongestant;
protective agent;
sympathomimetic agent;
vasoconstrictor agent		1996201919.7medium0081140
methoxamine
2
amphetaminesalpha-adrenergic agonist;
antihypotensive agent		1999200721.0low001100
phenylalanine
1
amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
phenylalanine;
proteinogenic amino acid		algal metabolite;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
Escherichia coli metabolite;
human xenobiotic metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite		2000200024.0low001000
arginine
1
arginine;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		biomarker;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical		2012201212.0low000010
quinoxalines
1
mancude organic heterobicyclic parent;
naphthyridine;
ortho-fused heteroarene		2001200123.0low000100
yohimbine
1
methyl 17-hydroxy-20xi-yohimban-16-carboxylatealpha-adrenergic antagonist;
dopamine receptor D2 antagonist;
serotonergic antagonist		2007200717.0low000100
bicuculline
1
benzylisoquinoline alkaloid;
isoquinoline alkaloid;
isoquinolines		agrochemical;
central nervous system stimulant;
GABA-gated chloride channel antagonist;
GABAA receptor antagonist;
neurotoxin		2004200420.0low000100
colforsin
1
acetate ester;
cyclic ketone;
labdane diterpenoid;
organic heterotricyclic compound;
tertiary alpha-hydroxy ketone;
triol		adenylate cyclase agonist;
anti-HIV agent;
antihypertensive agent;
plant metabolite;
platelet aggregation inhibitor;
protein kinase A agonist		2007200717.0low000100
u 73122
1
aromatic ether;
aza-steroid;
maleimides		EC 3.1.4.11 (phosphoinositide phospholipase C) inhibitor2004200420.0low000100
chlorethylclonidine
6
1997200723.5low003300
gr 127935
1
1,2,4-oxadiazole;
benzamides;
N-alkylpiperazine;
N-arylpiperazine		2007200717.0low000100
ml 9
1
2006200618.0low000100
u 73343
1
2004200420.0low000100
loe 908
1
201920195.0low000010
tamsulosin
2
5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamidealpha-adrenergic antagonist;
antineoplastic agent		1999201517.0low001010
rec 15-2739
1
1998199826.0low001000
angiotensin ii
1
amino acid zwitterion;
angiotensin II		human metabolite2012201212.0low000010
atropine
1
2002200222.0low000100
bmy 7378
11
1996201520.7medium004520
rs 100329
3
piperazines2006201215.7medium000210
6-cyano-7-nitroquinoxaline-2,3-dione
1
quinoxaline derivative2004200420.0low000100
silodosin
1
indolecarboxamide1998199826.0low001000
15-hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic acid
1
1999199925.0low001000
tetrodotoxin
1
azatetracycloalkane;
oxatetracycloalkane;
quinazoline alkaloid		animal metabolite;
bacterial metabolite;
marine metabolite;
neurotoxin;
voltage-gated sodium channel blocker		2004200420.0low000100
hv 723
2
1997199826.5medium002000
rs 17053
4
1999201519.2high002110
rs 79948-197
1
2001200123.0low000100
oxadiazoles
1
2007200717.0low000100
brimonidine tartrate
1
2001200123.0low000100
atrial natriuretic factor
1
polypeptide1998199826.0low001000
neuropeptide y
1
2000200024.0low001000
lucifer yellow
1
organic lithium saltfluorochrome2004200420.0low000100
jth 601
1
1999199925.0low001000
pyrimidinones
1
2000200024.0low001000
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Abdominal Migraine0
1
2007200717.0low000100
Aging0
1
2004200420.0low000100
Alveolitis, Fibrosing0
1
201720177.0low000010
Aortic Coarctation0
1
2012201212.0low000010
Body Weight0
1
2004200420.0low000100
Cardiac Failure0
4
201720196.2low000040
Cardiac Hypertrophy0
2
1998199826.0low002000
Cardiac Remodeling, Ventricular0
1
201720177.0low000010
Cardiomegaly0
2
1998199826.0low002000
Cardiomyopathies0
1
201720177.0low000010
Cardiomyopathies, Primary0
1
201720177.0low000010
Cirrhosis0
1
201720177.0low000010
Coarctation of Aorta0
1
2012201212.0low000010
Congenital Zika Syndrome0
1
202020204.0low000010
Disease Models, Animal0
2
201720205.5low000020
Fibrosis0
1
201720177.0low000010
Goldblatt Syndrome0
1
2012201212.0low000010
Heart Failure0
4
201720196.2low000040
Hypertension, Renovascular0
1
2012201212.0low000010
Ischemia0
1
2003200321.0low000100
Migraine Disorders0
1
2007200717.0low000100
Muscle Contraction0
7
1998200721.7medium002500
Necrosis0
1
201720177.0low000010
Pulmonary Fibrosis0
1
201720177.0low000010
Right Ventricular Dysfunction0
2
201720196.0low000020
Zika Virus Infection0
1
202020204.0low000010

Dosage (2)

ArticleYear
Effect of inter-renal aortic coarctation-induced hypertension on function and expression of vascular α(1A)- and α(1D)-adrenoceptors.
Canadian journal of physiology and pharmacology, , Volume: 90, Issue:1		2012
Enhancement of alpha-adrenoceptor-mediated responses in prostate of testosterone-treated rat.
European journal of pharmacology, , Oct-25, Volume: 453, Issue:2-3		2002