Compounds > cv 11194
Page last updated: 2024-12-10

cv 11194

Description

CV 11194: structure given in first source; an angiotensin II receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3025727
CHEMBL ID48242
SCHEMBL ID905714
SCHEMBL ID12787593
MeSH IDM0217784

Synonyms (19)

Synonym
2-butyl-3-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-benzoimidazole-4-carboxylic acid(cv11194)
2-butyl-3-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-benzoimidazole-4-carboxylic acid
bdbm50044402
cv 11194
CHEMBL48242 ,
cv-11194
L005054
2-butyl-3-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylic acid
2-butyl-1-((2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl)-1h-benzimidazole-7-carboxylic acid
2-butyl-1-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-1h-benzimidazole-7-carboxylic acid
136284-47-4
1h-benzimidazole-7-carboxylic acid, 2-butyl-1-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-
SCHEMBL905714
SCHEMBL12787593
FLOKGHWIQFCIJW-UHFFFAOYSA-N ,
2-butyl-1-[[2'-(1h-tetrazol-5-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylic acid
DTXSID70159756
2-butyl-3-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]benzoimidazole -4-carboxylic acid
2-butyl-3-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]benzoimidazole-4-carboxylic acid

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"In order to improve the oral bioavailability (BA) of 2-butyl-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimid azole - 7-carboxylic acid (3: CV-11194) and 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4- yl]methyl]-1H-benzimidazole-7-carboxylic acid (4: CV-11974), novel angiotensin II (AII) receptor antagonists, chemical modification to yield prodrugs has been examined."( Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of potential prodrugs of benzimidazole-7-carboxylic acids.
Furukawa, Y; Inada, Y; Kato, T; Kohara, Y; Kubo, K; Naka, T; Nishikawa, K; Shibouta, Y; Yoshimura, Y, 1993)		0.29
" This might be ascribed to their improved bioavailability by increased lipophilicity."( Synthesis and angiotensin II receptor antagonistic activities of benzimidazole derivatives bearing acidic heterocycles as novel tetrazole bioisosteres.
Imamiya, E; Inada, Y; Kohara, Y; Kubo, K; Naka, T; Wada, T, 1996)		0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Type-1 angiotensin II receptorBos taurus (cattle)IC50 (µMol)0.55000.18000.36500.5500AID568921
Type-1 angiotensin II receptorOryctolagus cuniculus (rabbit)IC50 (µMol)0.00010.00010.09130.5000AID568911
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (3)

Processvia Protein(s)Taxonomy
maintenance of blood vessel diameter homeostasis by renin-angiotensinType-1 angiotensin II receptorBos taurus (cattle)
regulation of vasoconstrictionType-1 angiotensin II receptorBos taurus (cattle)
phospholipase C-activating angiotensin-activated signaling pathwayType-1 angiotensin II receptorBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
angiotensin type I receptor activityType-1 angiotensin II receptorBos taurus (cattle)
angiotensin type II receptor activityType-1 angiotensin II receptorBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (20)

Assay IDTitleYearJournalArticle
AID181931Percent inhibition of angiotensin II (0.1 ug/kg iv) -induced pressor response 3h after administration of test compounds (1 mg/kg po) in conscious male Sprague-Dawley rats1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Synthesis and angiotensin II receptor antagonistic activities of benzimidazole derivatives bearing acidic heterocycles as novel tetrazole bioisosteres.
AID183922Inhibitory activity on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 5 h.1993Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of potential prodrugs of benzimidazole-7-carboxylic acids.
AID194464In vivo inhibition of angiotensin II (0.1 ug/kg) induced increase in blood pressure in conscious male rat at 3 mg/kg for 3h/7h.1993Journal of medicinal chemistry, Jun-11, Volume: 36, Issue:12
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of benzimidazoles.
AID39041In vitro for inhibition of specific binding of [125I]-angiotensin II (0.02 nM) to bovine adrenal cortex1993Journal of medicinal chemistry, Jun-11, Volume: 36, Issue:12
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of benzimidazoles.
AID183920Inhibitory activity on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 24 h.1993Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of potential prodrugs of benzimidazole-7-carboxylic acids.
AID26234Bioavailability determined from the ratio of AUC(plasma) for 0 to infinity after oral dosing of the test compound (10 mg/kg) to intravenous administration of CD-11194 (1 mg/kg) in rats1993Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of potential prodrugs of benzimidazole-7-carboxylic acids.
AID220582Percent inhibition of the Angiotensin-II (0.1micro g/kg, iv) induced pressor response after 7 hours of administration (3 mg/kg po) in rats1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of benzimidazolecarboxylic acids.
AID185269Percent inhibition of the Angiotensin-II (0.1ug/kg, iv) induced pressor response after 3 hours of administration (1 mg/kg po) in rats1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of benzimidazolecarboxylic acids.
AID568911Antagonist activity at angiotensin AT1 receptor in rabbit aortic strip assessed as inhibition of angiotensin 2-induced contractile response2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID183917Inhibitory activity on AII (100 ng/kg iv) -induced pressor response after administration at 0.1 mg/kg po in Dawley rats at 0.5 h1993Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of potential prodrugs of benzimidazole-7-carboxylic acids.
AID181933Percent inhibition of angiotensin II (0.1 ug/kg iv) -induced pressor response 7 hr after administration of test compounds (1 mg/kg po) in conscious male Sprague-Dawley rats1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Synthesis and angiotensin II receptor antagonistic activities of benzimidazole derivatives bearing acidic heterocycles as novel tetrazole bioisosteres.
AID39038Inhibition of specific binding of [125 I ] Angiotensin-II (0.2 nM) to bovine adrenal cortex1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of benzimidazolecarboxylic acids.
AID183923Inhibitory activity on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 7 h.1993Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of potential prodrugs of benzimidazole-7-carboxylic acids.
AID568921Displacement of [125I]-angiotensin 2 from angiotensin AT1 receptor in bovine adrenal cortical membranes2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID183921Inhibitory activity on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 3 h.1993Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of potential prodrugs of benzimidazole-7-carboxylic acids.
AID39039Inhibition of specific binding of [125I]angiotensin II (0.2 nM) to angiotensin II receptor in bovine adrenal cortex1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Synthesis and angiotensin II receptor antagonistic activities of benzimidazole derivatives bearing acidic heterocycles as novel tetrazole bioisosteres.
AID185393Percent inhibition of the Angiotensin-II (0.1ug/kg, iv) induced pressor response after 7 hours of administration (1 mg/kg po) in rats1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of benzimidazolecarboxylic acids.
AID183918Inhibitory activity on AII (100 ng/kg iv) -induced pressor response after administration at 0.1 mg/kg po in Dawley rats at 1 h1993Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of potential prodrugs of benzimidazole-7-carboxylic acids.
AID185270Percent inhibition of the Angiotensin-II (0.1ug/kg, iv) induced pressor response after 3 hours of administration (3 mg/kg po) in rats1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of benzimidazolecarboxylic acids.
AID183919Inhibitory activity on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 2 h.1993Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of potential prodrugs of benzimidazole-7-carboxylic acids.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (83.33)18.2507
2000's0 (0.00)29.6817
2010's1 (16.67)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: 12.24

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.24 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.18 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.24)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (33.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (66.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
candesartan cilexetil
candesartan cilexetil: a prodrug which is metabolized to an active form candesartan to exert its biological effects		4.330biphenyls
candesartan
candesartan: a nonpeptide angiotensin II receptor antagonist. candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension.		4.750benzimidazolecarboxylic acid;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
avapro
Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.		3.1510azaspiro compound;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
losartan
Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position		4.0140biphenylyltetrazole;
imidazoles		angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist
dup 532
DuP 532: angiotensin I receptor antagonist		3.1510
valsartan
Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.		3.1510biphenylyltetrazole;
monocarboxylic acid amide;
monocarboxylic acid		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
tasosartan
tasosartan: angiotensin II antagonist; structure given in first source		3.1510biphenyls
telmisartan
Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension.		3.1510benzimidazoles;
biphenyls;
carboxybiphenyl		angiotensin receptor antagonist;
antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
environmental contaminant;
xenobiotic
gr 117289
GR 117289: angiotensin AT1 receptor antagonist; structure given in first source. zolasartan : A member of the class of 1-benzofurans that is 3-bromo-1-benzofuran which is substituted by a 2-(1H-tetrazol-5-yl)phenyl group at position 2 and by a (2-butyl-5-carboxy-4-chloro-1H-imidazol-1-yl)methyl group at position 5. It is an angiotensin II receptor type 1 (AT1) antagonist and was in clinical trials for the treatment of hypertension (now discontinued).		3.15101-benzofurans;
biaryl;
imidazolyl carboxylic acid;
monocarboxylic acid;
organobromine compound;
organochlorine compound;
tetrazoles		angiotensin receptor antagonist;
antihypertensive agent
exp3174
losartan carboxylic acid: structure given in first source. losartan carboxylic acid : A biphenylyltetrazole that is losartan with the hydroxymethyl group at position 5 on the imidazole ring replaced with a carboxylic acid.		3.1510biphenylyltetrazole;
imidazoles;
organochlorine compound		metabolite
sc 51316
SC 51316: structure given in first source; an angiotensin II receptor antagonist		3.1510
3-((2'-carboxybiphenyl-4-yl)methyl)-2-cyclopropyl-7-methyl-3h-imidazo(4,5-b)pyridine
3-((2'-carboxybiphenyl-4-yl)methyl)-2-cyclopropyl-7-methyl-3H-imidazo(4,5-b)pyridine: a non-peptide angiotensin II-receptor antagonist; structure given in first source		3.1510
a 81988
A 81988: angiotensin II antagonist selective for type 1 receptors		3.1510
ici d8731
ICI D8731: structure given in first source; an angiotensin II receptor antagonist		3.1510
forasartan
forasartan: structure given in first source; an angiotensin AT(1) receptor antagonist; angiotensin II receptor antagonist; used in treatment of congestive heart failure. forasartan : A member of the class of pyridines that is pyridine which is substituted at positions 2 and 5 by o-(tetrazol-5-yl)phenyl and (3,5-dibutyl-1,2,4-triazol-1-yl)methyl groups, respectively. It is a nonpeptide antagonist of angiotensin II, type 1 (AT1) receptors, used for the treatment of hypertension.		3.1510benzenes;
pyridines;
tetrazoles;
triazoles		angiotensin receptor antagonist;
antihypertensive agent
up 269-6
UP 269-6: structure given in first source; angiotensin receptor antagonist		3.1510
mk 996
MK 996: an AT1-selective angiotensin II receptor antagonist; structure given in first source		3.1510
olmesartan
olmesartan: an active metabolite of CS 866		3.1510biphenylyltetrazoleangiotensin receptor antagonist;
antihypertensive agent
angiotensin ii
Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock. Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).		1.9810amino acid zwitterion;
angiotensin II		human metabolite
me 3221
ME 3221: an angiotensin II receptor antagonist; structure given in first source		3.1510
l 158809
L 158809: RN & structure given in first source; angiotensin receptor antagonist		3.1510
milfasartan
milfasartan: angiotensin I receptor antagonist; structure in first source		3.1510
dmp 811
DMP 811: angiotensin II receptor antagonist; structure given in first source		3.1510
eprosartan
eprosartan: angiotensin II receptor antagonist. eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure.		3.1510dicarboxylic acid;
imidazoles;
thiophenes		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
pratosartan
pratosartan: angiotensin II type 1 receptor blocker		3.1510biphenylyltetrazoleantihypertensive agent
losartan potassium
Erythropoietin: Glycoprotein hormone, secreted chiefly by the KIDNEY in the adult and the LIVER in the FETUS, that acts on erythroid stem cells of the BONE MARROW to stimulate proliferation and differentiation.		1.9810
azilsartan
azilsartan: an angiotensin type 1 receptor blocker; receptor blocker. azilsartan : A benzimidazolecarboxylic acid that is benzimidazole-7-carboxylic acid substituted at position 2 by a methoxy group and at position 1 by a 2'-[(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl group. Used (as the prodrug, azilsartan medoxomil) for treatment of hypertension.		3.52201,2,4-oxadiazole;
aromatic ether;
benzimidazolecarboxylic acid		angiotensin receptor antagonist;
antihypertensive agent
ConditionIndicatedRelationship StrengthStudiesTrials
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		01.9810
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