Page last updated: 2024-12-07

forasartan

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

Description

forasartan: structure given in first source; an angiotensin AT(1) receptor antagonist; angiotensin II receptor antagonist; used in treatment of congestive heart failure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

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. [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]

Cross-References

ID SourceID
PubMed CID132706
CHEMBL ID315021
CHEBI ID141552
SCHEMBL ID489497
MeSH IDM0225561

Synonyms (33)

Synonym
CHEMBL315021 ,
5-(3,5-dibutyl-[1,2,4]triazol-1-ylmethyl)-2-[2-(1h-tetrazol-5-yl)-phenyl]-pyridine
bdbm50049209
5-(3,5-dibutyl-[1,2,4]triazol-1-ylmethyl)-2-[2-(2h-tetrazol-5-yl)-phenyl]-pyridine
5-((3,5-dibutyl-1h-1,2,4-triazol-1-yl)methyl)-2-(2-(1h-tetrazol-5-ylphenyl))pyridine
pyridine, 5-((3,5-dibutyl-1h-1,2,4-triazol-1-yl)methyl)-2-(2-(1h-tetrazol-5-yl)phenyl)-
unii-065f7wpt0b
5-((3,5-dibutyl-1h-1,2,4-triazol-1-yl)methyl)-2-(o-1h-tetrazol-5-ylphenyl)pyridine
065f7wpt0b ,
forasartan [usan:inn]
145216-43-9
D04243
forasartan (usan/inn)
forasartan
DB01342
L007541
sc 52458
forasartanum
5-[(3,5-dibutyl-1h-1,2,4-triazol-1-yl)methyl]-2-[2-(1h-tetrazol-5-yl)phenyl]pyridine
CHEBI:141552
sc-52458 ,
5-[(3,5-dibutyl-1,2,4-triazol-1-yl)methyl]-2-[2-(2h-tetrazol-5-yl)phenyl]pyridine
gtpl6896
5-[(3,5-dibutyl-1h-1,2,4-triazol-1-yl)methyl]-2-(o-1h-tetrazol-5-ylphenyl)pyridine
forasartan [inn]
forasartan [usan]
forasartan [who-dd]
SCHEMBL489497
DTXSID70162942
5-[(dibutyl-1h-1,2,4-triazol-1-yl)methyl]-2-[2-(2h-1,2,3,4-tetrazol-5-yl)phenyl]pyridine
sc 52458;pyridine, 5-[(3,5-dibutyl-1h-1,2,4-triazol-1-yl)methyl]-2-[2-(1h-tetrazol-5-yl)phenyl]-
Q8564451
AKOS040751844
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
angiotensin receptor antagonistA hormone antagonist that blocks angiotensin receptors.
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
[role 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]

Drug Classes (4)

ClassDescription
tetrazolesAn azole in which the five-membered heterocyclic aromatic skeleton contains four N atoms and one C atom.
pyridinesAny organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives.
triazolesAn azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.
benzenesAny benzenoid aromatic compound consisting of the benzene skeleton and its substituted derivatives.
[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]

Pathways (1)

PathwayProteinsCompounds
Forasartan Action Pathway43

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Type-1B angiotensin II receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00690.00040.13343.8000AID37687
Type-1 angiotensin II receptorHomo sapiens (human)IC50 (µMol)0.00690.00020.09323.6000AID568897
[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)
Type-1 angiotensin II receptorHomo sapiens (human)Kd0.00630.00200.00390.0063AID568789
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (28)

Processvia Protein(s)Taxonomy
regulation of cell growthType-1 angiotensin II receptorHomo sapiens (human)
kidney developmentType-1 angiotensin II receptorHomo sapiens (human)
renin-angiotensin regulation of aldosterone productionType-1 angiotensin II receptorHomo sapiens (human)
maintenance of blood vessel diameter homeostasis by renin-angiotensinType-1 angiotensin II receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensinType-1 angiotensin II receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationType-1 angiotensin II receptorHomo sapiens (human)
Rho protein signal transductionType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationType-1 angiotensin II receptorHomo sapiens (human)
regulation of vasoconstrictionType-1 angiotensin II receptorHomo sapiens (human)
calcium-mediated signalingType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of phospholipase A2 activityType-1 angiotensin II receptorHomo sapiens (human)
low-density lipoprotein particle remodelingType-1 angiotensin II receptorHomo sapiens (human)
regulation of renal sodium excretionType-1 angiotensin II receptorHomo sapiens (human)
angiotensin-activated signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
regulation of cell population proliferationType-1 angiotensin II receptorHomo sapiens (human)
symbiont entry into host cellType-1 angiotensin II receptorHomo sapiens (human)
regulation of inflammatory responseType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of inflammatory responseType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of protein metabolic processType-1 angiotensin II receptorHomo sapiens (human)
cell chemotaxisType-1 angiotensin II receptorHomo sapiens (human)
phospholipase C-activating angiotensin-activated signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
blood vessel diameter maintenanceType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of blood vessel endothelial cell proliferation involved in sprouting angiogenesisType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of CoA-transferase activityType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processType-1 angiotensin II receptorHomo sapiens (human)
inflammatory responseType-1 angiotensin II receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
angiotensin type I receptor activityType-1 angiotensin II receptorHomo sapiens (human)
angiotensin type II receptor activityType-1 angiotensin II receptorHomo sapiens (human)
protein bindingType-1 angiotensin II receptorHomo sapiens (human)
bradykinin receptor bindingType-1 angiotensin II receptorHomo sapiens (human)
protein heterodimerization activityType-1 angiotensin II receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
plasma membraneType-1 angiotensin II receptorHomo sapiens (human)
membraneType-1 angiotensin II receptorHomo sapiens (human)
plasma membraneType-1 angiotensin II receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID60208Compound at an oral dose of 30 mg/Kg was tested for the inhibition of Ang-II induced pressor responses in conscious dog1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID568897Binding affinity to angiotensin AT1 receptor2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID568789Antagonist activity at angiotensin AT1 receptor2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID37687Binding affinity for rat angiotensin II receptor, type 12004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
Design, synthesis, structural studies, biological evaluation, and computational simulations of novel potent AT(1) angiotensin II receptor antagonists based on the 4-phenylquinoline structure.
AID568906Antihypertensive activity in conscious dog assessed as inhibition of angiotensin 2-induced response at 30 mg/kg, po up to 2 hrs2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID568787Displacement of [125I]-Sar1Ile8-angiotensin 2 from angiotensin AT1 receptor in rat adrenal cortical membranes2010Bioorganic & 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.
AID37828In vitro antagonistic potency against Angiotensin II receptor, type 1 in rat adrenal cortex1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's9 (60.00)18.2507
2000's5 (33.33)29.6817
2010's1 (6.67)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: 16.64

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 Index16.64 (24.57)
Research Supply Index2.83 (2.92)
Research Growth Index4.29 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.64)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (6.67%)5.53%
Reviews3 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (73.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]