Compounds > angiotensin ii, 1-sar-5-ile-8-ala-
Page last updated: 2024-11-11

angiotensin ii, 1-sar-5-ile-8-ala-

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

Cross-References

ID SourceID
PubMed CID5748380
CHEMBL ID312754
SCHEMBL ID11024001
MeSH IDM0089539

Synonyms (13)

Synonym
siaa ii
CHEMBL312754 ,
38027-95-1
1-sar-5-ile-8-ala-angiotensin ii
angiotensin ii, 1-sar-5-ile-8-ala-
1-sarcosyl-5-isoleucyl-8-alanine angiotensin ii
angiotensin ii, 1-sarcosyl-5-isoleucyl-8-alanine-
angiotensin ii, 1-(n-methylglycine)-5-l-isoleucine-8-l-alanine-
sar-arg-val-tyr-ile-his-pro-ala
(2s)-2-[[(2s)-1-[(2s)-2-[[(2s,3s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-3-(1h-imidazol-5-yl)propanoyl]py
SCHEMBL11024001
DTXSID90191436
bdbm50228894
[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)IC50 (µMol)0.00510.00040.15553.8000AID39206
Type-1B angiotensin II receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00510.00040.13343.8000AID39206
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00510.00100.39573.3000AID39206
[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-1A angiotensin II receptor Rattus norvegicus (Norway rat)EC50 (µMol)0.00570.00130.03390.2040AID1634589; AID1634591
Type-1 angiotensin II receptorHomo sapiens (human)EC50 (µMol)5.00460.00050.01350.0676AID1634585; AID1634587
[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 (23)

Assay IDTitleYearJournalArticle
AID182928In vivo antagonist activity (ANG II like) expressed as blood pressure increase (mHg) produced by 1 mg bolus iv injection of compound in rats1991Journal of medicinal chemistry, Oct, Volume: 34, Issue:10
An investigation of angiotensin II agonist and antagonist analogues with 5,5-dimethylthiazolidine-4-carboxylic acid and other constrained amino acids.
AID167207In vitro agonist activity expressed as percent activity relative to ANG II was measured in rabbit aorta strip assay1991Journal of medicinal chemistry, Oct, Volume: 34, Issue:10
An investigation of angiotensin II agonist and antagonist analogues with 5,5-dimethylthiazolidine-4-carboxylic acid and other constrained amino acids.
AID182803Dose required for the two fold increase in the dose of AII to produce the same elevation in blood pressure as in the control period.1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Effects of D-amino acid substitution on antagonist activities of angiotensin II analogues.
AID1134547Agonist activity at angiotensin 2 receptor in rabbit aorta assessed as myotropic activity up to 1 uM/L relative to angiotensin-21977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Synthesis of angiotensin II antagonists by incorporating alpha-methylalanine or O-methylthreonine residues in angiotension II analogues.
AID169065In vivo agonist activity expressed as percent activity relative to angiotensin II in rat blood pressure assay.1991Journal of medicinal chemistry, Oct, Volume: 34, Issue:10
An investigation of angiotensin II agonist and antagonist analogues with 5,5-dimethylthiazolidine-4-carboxylic acid and other constrained amino acids.
AID167344In vitro agonist activity relative to angiotensin II measured in rabbit aorta strip assay.1991Journal of medicinal chemistry, Oct, Volume: 34, Issue:10
An investigation of angiotensin II agonist and antagonist analogues with 5,5-dimethylthiazolidine-4-carboxylic acid and other constrained amino acids.
AID39205Binding affinity against Angiotensin II receptor, from rat adrenal gland1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype.
AID39206Binding affinity for rat brain Angiotensin II receptor1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype.
AID1134538In vivo non-competitive antagonist activity at angiotensin 2 receptor in ganglion-blocked vagotomized rat assessed as angiotensin-2 dose ratio at 250 ng/kg/min administered as an infusion1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Synthesis of angiotensin II antagonists by incorporating alpha-methylalanine or O-methylthreonine residues in angiotension II analogues.
AID1134548Competitive antagonist at angiotensin 2 receptor in rabbit aorta assessed as rightward shift in angiotensin-2 dose response curve for myotropic activity1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Synthesis of angiotensin II antagonists by incorporating alpha-methylalanine or O-methylthreonine residues in angiotension II analogues.
AID1134536In vivo agonist activity at angiotensin 2 receptor in ganglion-blocked vagotomized rat assessed as rise in blood pressure at 250 ng/kg/min compound infused for 30 mins1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Synthesis of angiotensin II antagonists by incorporating alpha-methylalanine or O-methylthreonine residues in angiotension II analogues.
AID167386pA2 value was determined in the range of competitive inhibition in the in vitro rabbit aorta strip assay.1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Effects of D-amino acid substitution on antagonist activities of angiotensin II analogues.
AID166813Antagonist activity pA2, was measured in the in vitro rabbit aorta strip assay1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
The role of position 4 in angiotensin II antagonism: a structure-activity study.
AID167382In vitro antagonist activity (ANG II like) expressed as percent activity relative to ANG II in rabbit aorta strip assay.1991Journal of medicinal chemistry, Oct, Volume: 34, Issue:10
An investigation of angiotensin II agonist and antagonist analogues with 5,5-dimethylthiazolidine-4-carboxylic acid and other constrained amino acids.
AID31277The compound was tested for its inhibitory activity as antagonist of AI on guinea pig ileum1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and biological activity of angiotensin II analogues containing a Val-His replacement, Val psi[CH(CONH2)NH]His.
AID167346In vitro angiotensin II-like activity, expressed as percent relative to angiotensin II, measured in the rabbit aorta strip assay1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Effects of D-amino acid substitution on antagonist activities of angiotensin II analogues.
AID1134549Non-competitive antagonist at angiotensin 2 receptor in rabbit aorta assessed as inhibition of angiotensin-2 induced myotropic activity at > 1 uM/L1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Synthesis of angiotensin II antagonists by incorporating alpha-methylalanine or O-methylthreonine residues in angiotension II analogues.
AID1134534In vivo agonist activity at angiotensin 2 receptor in ganglion-blocked vagotomized rat assessed as rise in blood pressure at 250 ng/kg/min compound infused for 10 mins1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Synthesis of angiotensin II antagonists by incorporating alpha-methylalanine or O-methylthreonine residues in angiotension II analogues.
AID1134550Antagonist at angiotensin 2 receptor in rabbit aorta assessed as duration of action at 1 uM/L treated for 5 mins after angiotensin-2 challenge1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Synthesis of angiotensin II antagonists by incorporating alpha-methylalanine or O-methylthreonine residues in angiotension II analogues.
AID172862In vivo AII-like activity, expressed as percent activity relative to AII (angiotensin II), measured in rat blood pressure assay1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Effects of D-amino acid substitution on antagonist activities of angiotensin II analogues.
AID39052Displacement of [3H]Angiotensin II (300 ng/mL) from rabbit adrenal cortex1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and biological activity of angiotensin II analogues containing a Val-His replacement, Val psi[CH(CONH2)NH]His.
AID31303Inhibitory activity as antagonist of AII on guinea pig ileum1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and biological activity of angiotensin II analogues containing a Val-His replacement, Val psi[CH(CONH2)NH]His.
AID1134532In vivo agonist activity at angiotensin 2 receptor in ganglion-blocked vagotomized rat assessed as rise in blood pressure at 250 ng/kg/min compound infused for 3 mins1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Synthesis of angiotensin II antagonists by incorporating alpha-methylalanine or O-methylthreonine residues in angiotension II analogues.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (55.56)18.7374
1990's4 (44.44)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)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: 12.11

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 Index12.11 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.41 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.11)

All Compounds (24.57)

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%
Other9 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
indomethacin
Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.		1.9510aromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole		analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite;
xenobiotic
captopril
Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug.		1.9710alkanethiol;
L-proline derivative;
N-acylpyrrolidine;
pyrrolidinemonocarboxylic acid		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
angiotensin ii, sar(1)-me-tyr(4)-
[no description available]		1.9710
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).		3.0750amino acid zwitterion;
angiotensin II		human metabolite
pd 123319
PD123319 : An imidazopyridine consisting of 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine having 4-(dimethylamino)-3-methylbenzyl, diphenylacetyl and carboxy and groups at positions 1, 5 and 6 respectively		1.9710imidazopyridineangiotensin receptor antagonist;
endothelin receptor antagonist;
vasoconstrictor agent
exp 655
[no description available]		1.9710
lisinopril
Lisinopril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure.		1.9710dipeptideEC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
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).		1.9710dicarboxylic acid monoester;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
geroprotector;
prodrug
saralasin
Saralasin: An octapeptide analog of angiotensin II (bovine) with amino acids 1 and 8 replaced with sarcosine and alanine, respectively. It is a highly specific competitive inhibitor of angiotensin II that is used in the diagnosis of HYPERTENSION.		2.8840oligopeptide
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.		02.3720
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		01.9510
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		01.9710
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.		01.9710