Angiotensin (1-7) (; Molecular weight = 899.02 g/mol; H- Asp- Arg- Val- Tyr-

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-OH) is an active heptapeptide of the

renin–angiotensin system The renin–angiotensin system (RAS), or renin–angiotensin–aldosterone system (RAAS), is a hormone system that regulates blood pressure, fluid, and electrolyte balance, and systemic vascular resistance. When renal blood flow is reduced, ...

(RAS). It also known by the generic name talfirastide (development name TXA127). In 1988, Santos ''et al'' demonstrated that angiotensin (1-7) was a main product of the incubation of angiotensin I with brain micropunch biopsies and Schiavone ''et al'' reported the first biological effect of this heptapeptide. Benter et al were the first to report that Ang-(1-7) behaves in a way opposite to that of Ang II and that intavenous administration of Ang-(1-7) produces blood pressure lowering effects by activating its own receptor Angiotensin (1-7) is a vasodilator agent affecting cardiovascular organs, such as heart, blood vessels and kidneys, with functions frequently opposed to those attributed to the major effector component of the RAS, angiotensin II (Ang II).

Synthesis

The polypeptide Ang I can be converted into Ang (1-7) by the actions of

neprilysin Neprilysin (; also known as membrane metallo-endopeptidase (MME), neutral endopeptidase (NEP), cluster of differentiation 10 (CD10) and common acute lymphoblastic leukemia antigen (CALLA)) is an enzyme that in humans is encoded by the ''MME'' ge ...

(NEP) and thimet oligopeptidase (TOP) enzymes. Also, Ang II can be

hydrolyzed Hydrolysis (; ) is any chemical reaction in which a molecule of water breaks one or more chemical bonds. The term is used broadly for substitution, elimination, and solvation reactions in which water is the nucleophile. Biological hydrolysi ...

into Ang (1-7) through the actions of

angiotensin-converting enzyme 2 Angiotensin-converting enzyme 2 (ACE2) is an enzyme that can be found either attached to the membrane of cells (mACE2) in the intestines, kidney, testis, gallbladder, and heart or in a soluble form (sACE2). Both membrane bound and soluble ACE2 ...

(ACE2). Ang (1-7) binds and activates the

G-protein coupled receptor G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large protein family, group of evoluti ...

Mas receptor leading to opposite effects of those of Ang II.

Possible pathways

* Action of

on angiotensin I or angiotensin II. * Action of

prolyl endopeptidase Prolyl endopeptidase (PE) also known as prolyl oligopeptidase or post-proline cleaving enzyme is an enzyme that in humans is encoded by the ''PREP'' gene. Function Prolyl endopeptidase is a large cytosolic enzyme that belongs to a distinct cl ...

angiotensin I Angiotensin is a peptide hormone that causes vasoconstriction and an increase in blood pressure. It is part of the renin–angiotensin system, which regulates blood pressure. Angiotensin also stimulates the release of aldosterone from the adren ...

. * Action of ACE on angiotensin 1-9. * Action of

on angiotensin 1-9. * Action of ACE2 on

angiotensin II Angiotensin is a peptide hormone that causes vasoconstriction and an increase in blood pressure. It is part of the renin–angiotensin system, which regulates blood pressure. Angiotensin also stimulates the release of aldosterone from the ...

Effects

Ang (1-7) has been shown to have anti-oxidant and anti-inflammatory effects. It helps protect cardiomyocytes of spontaneously hypertensive rats by increasing the expression of endothelial and neuronal nitric oxide synthase enzymes, augmenting production of nitric oxide.

Pharmacological interactions

Ang (1-7) contributes to the beneficial effects of ACE inhibitors and angiotensin II receptor type 1 antagonists.

Clinical trials

Talfirastide has been tested in people with

COVID-19 Coronavirus disease 2019 (COVID-19) is a contagious disease caused by the coronavirus SARS-CoV-2. In January 2020, the disease spread worldwide, resulting in the COVID-19 pandemic. The symptoms of COVID‑19 can vary but often include fever ...

and stroke.

References

{{Reflist Peptides Angiology Endocrinology Hypertension