Page last updated: 2024-11-07

up 269-6

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

Description

UP 269-6: structure given in first source; angiotensin receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID132840
CHEMBL ID312104
SCHEMBL ID12465608
SCHEMBL ID489673
MeSH IDM0234926

Synonyms (23)

Synonym
CHEMBL312104 ,
ripisartan
5-methyl-7-propyl-8-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-[1,2,4]triazolo[1,5-c]pyrimidin-2-ol
bdbm50039342
5-methyl-7-propyl-8-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-[1,2,4]triazolo[1,5-c]pyrimidin-2-ol
ripisartan [inn]
unii-7lq7oqp653
148504-51-2
7lq7oqp653 ,
(1,2,4)triazolo(1,5-c)pyrimidin-2(3h)-one, 5-methyl-7-propyl-8-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-
5-methyl-7-propyl-8-(p-(o-1h-tetrazol-5-ylphenyl)benzyl)-s-triazolo(1,5-c)pyrimidin-2(3h)-one
up-269-6
5-methyl-7-propyl-8-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-(1,2,4)triazolo(1,5-c)pyrimidin-2(3h)-one
5-methyl-7-n-propyl-8-((2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl)-(1,2,4)-triazolo(1,5-c)pyrimidin-2(3h)-one
up 269-6
L001457
5-methyl-7-propyl-8-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]-3h-[1,2,4]triazolo[1,5-c]pyrimidin-2-one
SCHEMBL12465608
ripisartan [who-dd]
SCHEMBL489673
DTXSID10164001
Q27268532
AKOS040749300

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Urinary electrolytes and aldosterone were measured for the 24 h before dosing and for 24 h after dosing."( Comparison of the oral angiotensin II receptor antagonist UP 269-6 or enalapril 20 mg on blood pressure and neurohormonal effects in salt-deplete man.
Brunner, HR; Insuasty, J; MacFadyen, RJ; McIntyre, M; Menard, J; Meredith, PA; Reid, JL, 1995
)
0.54
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Type-1A angiotensin II receptor Rattus norvegicus (Norway rat)Ki0.02400.00020.10251.7000AID37982
Type-1B angiotensin II receptorRattus norvegicus (Norway rat)Ki0.02400.00020.05211.1000AID37982; AID39511
Type-1 angiotensin II receptorHomo sapiens (human)Ki0.02400.00020.18374.7000AID568897
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)Ki79.20000.00010.01470.0316AID39638
[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 (7)

Assay IDTitleYearJournalArticle
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.
AID167369Compound was tested for its antagonistic activity against angiotensin II-induced contractions in rabbit aorta1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID39638In vitro binding affinity against angiotensin-2 (AT-2) receptor in rat adrenal1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Synthesis and SAR studies of novel triazolopyrimidine derivatives as potent, orally active angiotensin II receptor antagonists.
AID224825Compound at a dose of 10 mg/kg was administered orally and evaluated for change in systolic arterial blood pressure in renal artery ligated hypertensive rats1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Synthesis and SAR studies of novel triazolopyrimidine derivatives as potent, orally active angiotensin II receptor antagonists.
AID224824Compound at a dose of 1 mg/kg was administered orally and evaluated for change in mean arterial blood pressure in renal artery ligated hypertensive rats1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Synthesis and SAR studies of novel triazolopyrimidine derivatives as potent, orally active angiotensin II receptor antagonists.
AID39511Displacement of [125I]-Sar1-Ile8-A II from rat adrenal Angiotensin-1 (AT-1) receptor1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Synthesis and SAR studies of novel triazolopyrimidine derivatives as potent, orally active angiotensin II receptor antagonists.
AID37982Binding affinity was evaluated towards Angiotensin II receptor, type 1 in rat adrenal membrane1996Journal 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's10 (66.67)18.2507
2000's4 (26.67)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: 11.20

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 Index11.20 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index4.20 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.20)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (26.67%)5.53%
Reviews2 (13.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (60.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]