Compounds > a 81988
Page last updated: 2024-11-07

a 81988

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Description

A 81988: angiotensin II antagonist selective for type 1 receptors [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID132387
CHEMBL ID416477
SCHEMBL ID7048946
MeSH IDM0216587

Synonyms (23)

Synonym
3-pyridinecarboxylic acid, 2-(propyl((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)amino)-
OPREA1_714523
a 81988
CHEMBL416477 ,
a-81988
L007227
2-{propyl-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-amino}-nicotinic acid
bdbm50003154
2-{propyl-[2''-(2h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-amino}-nicotinic acid
2-[propyl-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]amino]pyridine-3-carboxylic acid
2-(n-propyl-n-((2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl)amino)pyridine-3-carboxylic acid
abbott-81988
a81988
141887-34-5
[3h]-a81988
[3h]a81988
gtpl3938
SCHEMBL7048946
DTXSID40161846
HY-U00188
CS-7281
3-pyridinecarboxylic acid, 2-[propyl[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]amino]-
AKOS040741019

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Comparison of urea 2 with a series of well-absorbed compounds using delta log P analysis suggested that 2 has an excess capacity for forming hydrogen bonds with solvent."( Azole endothelin antagonists. 3. Using delta log P as a tool to improve absorption.
Calzadilla, SV; Chiou, W; Dayton, BD; Dixon, DB; Hernandez, L; Hoffman, DJ; Kester, JA; Marsh, KC; Nellans, HN; Opgenorth, TJ; von Geldern, TW; Wu-Wong, JR, 1996)		0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Type-1A angiotensin II receptor Rattus norvegicus (Norway rat)Ki0.00060.00020.10251.7000AID39022
Type-1B angiotensin II receptorRattus norvegicus (Norway rat)Ki0.00080.00020.05211.1000AID37705
Type-2 angiotensin II receptorHomo sapiens (human)Ki0.00060.00020.56507.7790AID39022
[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)
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Kd0.00010.00012.29338.5114AID37536
Type-1 angiotensin II receptorOryctolagus cuniculus (rabbit)Kd0.00010.00010.03790.1995AID37536
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (25)

Processvia Protein(s)Taxonomy
blood vessel remodelingType-2 angiotensin II receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by circulatory renin-angiotensinType-2 angiotensin II receptorHomo sapiens (human)
angiotensin-mediated vasodilation involved in regulation of systemic arterial blood pressureType-2 angiotensin II receptorHomo sapiens (human)
brain renin-angiotensin systemType-2 angiotensin II receptorHomo sapiens (human)
cell surface receptor signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway coupled to cGMP nucleotide second messengerType-2 angiotensin II receptorHomo sapiens (human)
brain developmentType-2 angiotensin II receptorHomo sapiens (human)
regulation of blood pressureType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of heart rateType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of cell growthType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of phosphoprotein phosphatase activityType-2 angiotensin II receptorHomo sapiens (human)
regulation of metanephros sizeType-2 angiotensin II receptorHomo sapiens (human)
exploration behaviorType-2 angiotensin II receptorHomo sapiens (human)
nitric oxide-cGMP-mediated signalingType-2 angiotensin II receptorHomo sapiens (human)
angiotensin-activated signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
vasodilationType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of blood vessel endothelial cell migrationType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of neurotrophin TRK receptor signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
neuron apoptotic processType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of metanephric glomerulus developmentType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of branching involved in ureteric bud morphogenesisType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of extrinsic apoptotic signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
inflammatory responseType-2 angiotensin II receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
angiotensin type II receptor activityType-2 angiotensin II receptorHomo sapiens (human)
protein bindingType-2 angiotensin II receptorHomo sapiens (human)
receptor antagonist activityType-2 angiotensin II receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneType-2 angiotensin II receptorHomo sapiens (human)
plasma membraneType-2 angiotensin II receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (56)

Assay IDTitleYearJournalArticle
AID22405Volume of distribution of the terminal phase (= CLp+ plasma elimination rate constant) after intravenous dose of 3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID23993Half-life period of compound after intravenous dose of 1 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID22396Volume of distribution of central compartment (= dose+ plasma concentration at time zero) after intravenous dose of 1 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID174249% decrease in blood pressure after 4 hours at a dose of 1 mg/kg in male rats by using Renal artery hypertensive model1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID568881Binding affinity to angiotensin AT1 receptor in rat liver membranes2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID37542Potency to antagonize the ability of angiotensin II to contract rabbit aorta1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID23992Half-life period of compound after intravenous dose of 0.3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID37985In vitro antagonistic potency against Angiotensin II receptor, type 1 in rat liver1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID16333Delta logD (pH 6.5)1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
Azole endothelin antagonists. 3. Using delta log P as a tool to improve absorption.
AID22206Tmax value after oral dose of 3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID37536Compound was evaluated for in vitro potency against angiotensin II receptor, type 1 in isolated rabbit aorta; value ranges from 10.1-10.71992Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
Discovery of a novel class of orally active, non-peptide angiotensin II antagonists.
AID22403Volume of distribution of the terminal phase (= CLp+ plasma elimination rate constant) after intravenous dose of 0.3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID10475Area under curve after oral dose of 0.1 mg//kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID22201Tmax value after oral dose of 0.1 mg//kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID22395Volume of distribution of central compartment (= dose+ plasma concentration at time zero) after intravenous dose of 0.3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID17975Bioavailability after oral dose of 3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID15897Plasma clearance after intravenous dose of 0.3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID10477Area under curve after oral dose of 1 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID568914Oral bioavailability in cynomolgus monkey2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID22202Tmax value after oral dose of 0.3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID39022Binding affinity against angiotensin II receptor from rat liver1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID37705Compound was evaluated for binding affinity against angiotensin II receptor, type 1 in rat liver1992Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
Discovery of a novel class of orally active, non-peptide angiotensin II antagonists.
AID22404Volume of distribution of the terminal phase (= CLp+ plasma elimination rate constant) after intravenous dose of 1 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID174385% decrease in blood pressure after 4 hours in male rats at a dose of 0.03 mg/kg by using Renal artery hypertensive model1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID15480Cmax value after oral dose of 0.3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID23997Half-life period after oral dose of 0.3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID174240% decrease in blood pressure after 24 hours at a dose of 1 mg/kg in male rats by using Furosemide-treated spontaneous hypertensive model1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID174253% decrease in blood pressure after 4 hours in male rats at a dose of 0.01 mg/kg by using Renal artery hypertensive model1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID174237% decrease in blood pressure after 24 hours at a dose of 0.1 mg/kg in male rats by using Furosemide-treated spontaneous hypertensive model1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID15481Cmax value after oral dose of 1 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID15479Cmax value after oral dose of 0.1 mg//kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID174241% decrease in blood pressure after 4 hours at a dose of 0.1 mg/kg in male rats by using Furosemide-treated spontaneous hypertensive model1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID15899Plasma clearance after intravenous dose of 3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID16334Partition coefficient by standard shake-flask techniquesat 37 C, using octanol and cyclohexane1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
Azole endothelin antagonists. 3. Using delta log P as a tool to improve absorption.
AID18174Oral Bioavailability was evaluated in dog by oral administration1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID23998Half-life period after oral dose of 1 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID17970Bioavailability after oral dose of 0.1 mg//kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID18176Oral bioavailability in rat1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID174389% decrease in blood pressure after 4 hours in male rats at a dose of 0.3 mg/kg by using Renal artery hypertensive model1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID23994Half-life period of compound after intravenous dose of 3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID10476Area under curve after oral dose of 0.3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID22203Tmax value after oral dose of 1 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID15484Cmax value after oral dose of 3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID17972Bioavailability after oral dose of 1 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID568869Oral bioavailability in rat2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID167381Inhibition of angiotensin II-induced contractions in rabbit aorta in vitro.1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID18172Oral Bioavailability was evaluated in cynomolgus monkeys by oral administration1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID568783Antagonist activity at angiotensin AT1 receptor in rabbit aorta2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID23999Half-life period after oral dose of 3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID15898Plasma clearance after intravenous dose of 1 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID17971Bioavailability after oral dose of 0.3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID568913Oral bioavailability in dog2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID10480Area under curve after oral dose of 3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID22397Volume of distribution of central compartment (= dose+ plasma concentration at time zero) after intravenous dose of 3 mg/kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID174247% decrease in blood pressure after 4 hours at a dose of 1 mg/kg in male rats by using Furosemide-treated spontaneous hypertensive model1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID23996Half-life period after oral dose of 0.1 mg//kg1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (17)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's15 (88.24)18.2507
2000's1 (5.88)29.6817
2010's1 (5.88)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.26

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

MetricThis Compound (vs All)
Research Demand Index11.26 (24.57)
Research Supply Index2.89 (2.92)
Research Growth Index4.15 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.26)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (11.76%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (88.24%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
niacin
Niacin: A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties.. vitamin B3 : Any member of a group of vitamers that belong to the chemical structural class called pyridines that exhibit biological activity against vitamin B3 deficiency. Vitamin B3 deficiency causes a condition known as pellagra whose symptoms include depression, dermatitis and diarrhea. The vitamers include nicotinic acid and nicotinamide (and their ionized and salt forms).. nicotinic acid : A pyridinemonocarboxylic acid that is pyridine in which the hydrogen at position 3 is replaced by a carboxy group.		1.9810pyridine alkaloid;
pyridinemonocarboxylic acid;
vitamin B3		antidote;
antilipemic drug;
EC 3.5.1.19 (nicotinamidase) inhibitor;
Escherichia coli metabolite;
human urinary metabolite;
metabolite;
mouse metabolite;
plant metabolite;
vasodilator agent
theophylline
[no description available]		1.9910dimethylxanthineadenosine receptor antagonist;
anti-asthmatic drug;
anti-inflammatory agent;
bronchodilator agent;
drug metabolite;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
fungal metabolite;
human blood serum metabolite;
immunomodulator;
muscle relaxant;
vasodilator agent
candesartan cilexetil
candesartan cilexetil: a prodrug which is metabolized to an active form candesartan to exert its biological effects		4.0320biphenyls
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.		4.0320benzimidazolecarboxylic 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.		4.0320azaspiro 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		4.750biphenylyltetrazole;
imidazoles		angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist
arginine
Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group.		1.9810arginine;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		biomarker;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical
ng-nitroarginine methyl ester
NG-Nitroarginine Methyl Ester: A non-selective inhibitor of nitric oxide synthase. It has been used experimentally to induce hypertension.		2.3920alpha-amino acid ester;
L-arginine derivative;
methyl ester;
N-nitro compound		EC 1.14.13.39 (nitric oxide synthase) inhibitor
dup 532
DuP 532: angiotensin I receptor antagonist		4.330
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.		4.0320biphenylyltetrazole;
monocarboxylic acid amide;
monocarboxylic acid		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
tasosartan
tasosartan: angiotensin II antagonist; structure given in first source		4.0320biphenyls
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).		4.03201-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.		4.330biphenylyltetrazole;
imidazoles;
organochlorine compound		metabolite
ro 46-2005
Ro 46-2005: an orally active non-peptide antagonist of endothelin receptors; structure given in first source		1.9910
exp7711
EXP7711: to search, use E#P7711(nm); angiotensin II receptor antagonist; structure given in first source		3.0910
bibs 39
BIBS 39: structure given in first source; angiotensin II receptor antagonist		3.0910
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		4.0320
bibs 222
BIBS 222: structure given in first source; angiotensin II receptor antagonist		3.0910
ici d8731
ICI D8731: structure given in first source; an angiotensin II receptor antagonist		4.0320
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.		4.0320benzenes;
pyridines;
tetrazoles;
triazoles		angiotensin receptor antagonist;
antihypertensive agent
up 269-6
UP 269-6: structure given in first source; angiotensin receptor antagonist		4.0320
mk 996
MK 996: an AT1-selective angiotensin II receptor antagonist; structure given in first source		4.0320
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).		3.69100amino acid zwitterion;
angiotensin II		human metabolite
me 3221
ME 3221: an angiotensin II receptor antagonist; structure given in first source		4.0320
l 158809
L 158809: RN & structure given in first source; angiotensin receptor antagonist		4.330
bradykinin
[no description available]		1.9810oligopeptidehuman blood serum metabolite;
vasodilator agent
nitroarginine
Nitroarginine: An inhibitor of nitric oxide synthetase which has been shown to prevent glutamate toxicity. Nitroarginine has been experimentally tested for its ability to prevent ammonia toxicity and ammonia-induced alterations in brain energy and ammonia metabolites. (Neurochem Res 1995:200(4):451-6). N(gamma)-nitro-L-arginine : An L-arginine derivative that is L-arginine in which the terminal nitrogen of the guanidyl group is replaced by a nitro group.		1.9810guanidines;
L-arginine derivative;
N-nitro compound;
non-proteinogenic L-alpha-amino acid
cv 11194
CV 11194: structure given in first source; an angiotensin II receptor antagonist		3.1510
milfasartan
milfasartan: angiotensin I receptor antagonist; structure in first source		4.0320
dmp 811
DMP 811: angiotensin II receptor antagonist; structure given in first source		4.0320
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.		4.0320dicarboxylic acid;
imidazoles;
thiophenes		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
exp 655
[no description available]		3.0910
enalapril
Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration).		1.9810dicarboxylic acid monoester;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
geroprotector;
prodrug
l 162313
L 162313: a biphenylimidazole derivative; a non-peptide angiotensin agonist; no further information available 2/95		3.0910
pratosartan
pratosartan: angiotensin II type 1 receptor blocker		4.0320biphenylyltetrazoleantihypertensive agent
l 163491
L 163491: structure given in first source		3.0910
ema401
[no description available]		3.0910
pituitrin
Pituitrin: A substance or extract from the neurohypophysis (PITUITARY GLAND, POSTERIOR).		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.		3.15101,2,4-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
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		01.9810
Genetic Diseases
[description not available]		01.9810
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		01.9810
Blood Pressure, High
[description not available]		03.2460
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		03.2460
Genetic Diseases, Inborn
Diseases that are caused by genetic mutations present during embryo or fetal development, although they may be observed later in life. The mutations may be inherited from a parent's genome or they may be acquired in utero.		01.9810
Proteinuria
The presence of proteins in the urine, an indicator of KIDNEY DISEASES.		02.3820
Kidney Failure
A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism.		01.9810
Renal Insufficiency
Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE.		01.9810
Hypertension, Renal
Persistent high BLOOD PRESSURE due to KIDNEY DISEASES, such as those involving the renal parenchyma, the renal vasculature, or tumors that secrete RENIN.		01.9810
Left Ventricular Hypertrophy
[description not available]		0210
Cirrhosis
[description not available]		0210
Cardiac Failure
[description not available]		0210
Fibrosis
Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.		0210
Heart Failure
A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.		0210
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		0210
Hypertrophy, Left Ventricular
Enlargement of the LEFT VENTRICLE of the heart. This increase in ventricular mass is attributed to sustained abnormal pressure or volume loads and is a contributor to cardiovascular morbidity and mortality.		0210