Angiotensin II acetate salt

Names

[ Name ]:
Angiotensin II acetate salt

[Synonym ]:
Phenylalanine, α-aspartyl-N-(diaminomethylene)ornithylvalyltyrosylisoleucylhistidylprolyl-
α-Aspartylarginylvalyltyrosylisoleucylhistidylprolylphenylalanine
phenylalanine, α-aspartylarginylvalyltyrosylisoleucylhistidylprolyl-
α-aspartyl-N-(diaminomethylidene)ornithylvalyltyrosylisoleucylhistidylprolylphenylalanine
α-Aspartyl-N-(diaminomethylene)ornithylvalyltyrosylisoleucylhistidylprolylphenylalanine
Angiotensin II
ASP-ARG-VAL-TYR-ILE-HIS-PRO-PHE
Angiotensin II human

Biological Activity

[Description]:

Angiotensin II human is a vasoconstrictor that acts on the AT1 and the AT2 receptor.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Angiotensin Receptor

Research Areas >> Cardiovascular Disease

Natural Products >> Others

Peptides

[Target]

Angiotensin receptor (AT receptor)[1]

[In Vitro]

Most of the known actions of Angiotensin II (Ang II) are mediated by AT1 receptors, the AT2 receptor contributes to the regulation of blood pressure and renal function[1]. Angiotensin II raises blood pressure (BP) by a number of actions, the most important ones being vasoconstriction, sympathetic nervous stimulation, increased aldosterone biosynthesis and renal actions. Other Angiotensin II actions include induction of growth, cell migration, and mitosis of vascular smooth muscle cells, increased synthesis of collagen type I and III in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. These actions are mediated by type 1 Ang II receptors (AT1)[2]. At the cellular level, responsiveness to Angiotensin II is conferred by the expression of the two classes of angiotensin receptors (AT1 and AT2). The effects of Angiotensin II to increase blood pressure are mediated by AT1 receptors[3].

[In Vivo]

To distinguish the AT1 receptor population that is critical for the pathogenesis of hypertension, osmotic minipumps are implanted s.c. into each animal to infuse Angiotensin II (1,000 ng/kg/min) continuously for 4 weeks. Angiotensin II causes hypertension by activating AT1 receptors in the kidney promoting sodium reabsorption[3].

[Animal admin]

Mice[3] (129×C57BL/6) F1 mice lacking AT1A receptors for Angiotensin II are used. The mice are fed 10 gm/day gelled 0.25% NaCl diet that contains all nutrients and water. After 1 week of baseline collections, the animals are implanted with osmotic minipumps infusing Angiotensin II and are returned to the metabolic cage for 5 more days. Urinary sodium content is determined by using an IL943 Automatic Flame photometer. After 28 days of Angiotensin II infusion, hearts are harvested, weighed, fixed in formalin, sectioned, and stained with Masson trichrome. All of the tissues are examined by a pathologist (P.R.) without knowledge of genotypes.

[References]

[1]. de Gasparo M, et al. International union of pharmacology. XXIII. The angiotensin II receptors. Pharmacol Rev. 2000 Sep;52(3):415-72.

[2]. Fyhrquist F, et al. Role of angiotensin II in blood pressure regulation and in the pathophysiology of cardiovascular disorders. J Hum Hypertens. 1995 Nov;9 Suppl 5:S19-24.

[3]. Crowley SD, et al. Angiotensin II causes hypertension and cardiac hypertrophy through its receptors in the kidney. Proc Natl Acad Sci U S A. 2006 Nov 21;103(47):17985-90.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
809.08°C (rough estimate)

[ Molecular Formula ]:
C₅₀H₇₁N₁₃O₁₂

[ Molecular Weight ]:
1046.179

[ Exact Mass ]:
1045.534546

[ PSA ]:
406.34000

[ LogP ]:
2.34

[ Index of Refraction ]:
1.664

[ Storage condition ]:
-20°C

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: BW2165000

CHEMICAL NAME :: Angiotensin II, 5-L-isoleucine-

CAS REGISTRY NUMBER :: 4474-91-3

LAST UPDATED :: 199712

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C50-H71-N13-O12

MOLECULAR WEIGHT :: 1046.34

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 17400 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 24,6079,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 30800 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 24,6079,1990 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 119 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 24,6109,1990

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

[ RTECS ]:
BW2165000

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

Trimethylamine-N-oxide: a carnitine-derived metabolite that prolongs the hypertensive effect of angiotensin II in rats.

Can. J. Cardiol. 30(12) , 1700-5, (2014)

Recent evidence suggests that an elevated plasma trimethylamine N-oxide (TMAO) level is associated with an increased risk of adverse cardiovascular events in humans; however, the mechanism is not clea...

IGF-1 deficiency impairs cerebral myogenic autoregulation in hypertensive mice.

J. Cereb. Blood Flow Metab. 34(12) , 1887-97, (2014)

Aging impairs autoregulatory protection in the brain, exacerbating hypertension-induced cerebromicrovascular injury, neuroinflammation, and development of vascular cognitive impairment. Despite the im...

Effects of a domain-selective ACE inhibitor in a mouse model of chronic angiotensin II-dependent hypertension.

Clin. Sci. 127(1) , 57-63, (2014)

The somatic isozyme of ACE (angiotensin I-converting enzyme) comprises two distinct zinc-dependent catalytic domains with different substrate specificities for angiotensin I (cleaved selectively by th...

Related Compounds

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