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Angiotensin II acetate (CAS: 58-49-1) is a pharmaceutical salt synthesized by combining angiotensin II (Ang II) with acetate radicals. Its molecular structure is based on the active peptide sequence DRVYIHPF, and this acetate salt fully retains the inherent biological activity of the parent peptide. Chemically, the product appears as a white or off-white crystalline powder. It features excellent water solubility, which greatly facilitates the preparation of liquid injection formulations. In terms of stability, this acetate outperforms the original DRVYIHPF peptide. It maintains stable molecular structure and biological potency under standard sealed, cool and dry storage conditions, and is less susceptible to degradation caused by temperature changes and slight pH fluctuations. Thanks to optimized physicochemical properties, it also delivers higher bioavailability after administration.
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Angiotensin II acetate COA
Chemical structure
Angiotensin II acetate (C50H71N13O10) is a salt compound of DRVYIHPF. It is an active peptide composed of 8 amino acids, with the chemical formula C50H71N13O10. It has strong physiological activity and participates in a series of key processes such as blood pressure regulation and fluid balance in the body. Acetate is formed through the acetylation reaction of certain amino groups in DRVYIHPF molecules, which enhances the solubility and stability of the drug.Compared with the original DRVYIHPF, the acetate form of DRVYIHPF has better stability as a drug molecule, making it easier to maintain activity in solution without degradation.
This characteristic makes it a commonly used formulation in clinical acute treatment, especially suitable for injection and intravenous infusion.Clinically, this agent is extensively applied to manage hypotension. It serves as a reliable therapeutic option for critical cases including acute circulatory failure and various types of shock, possessing remarkable clinical significance. Compared with pure DRVYIHPF, the acetate salt boasts superior stability, solubility and bioavailability. These advantages make it safer and more efficacious for clinical injection use, and it has become a preferred formulation in relevant emergency and critical care treatments.
Pharmacological characteristics
Acetate, like DRVYIHPF, exert their physiological and pharmacological effects by binding to DRVYIHPF receptor type 1 (AT1 receptor) and type 2 (AT2 receptor). The AT1 receptor is the main target of DRVYIHPF, involving signaling pathways such as vasoconstriction, aldosterone secretion, sympathetic nervous system excitation, cell proliferation, and fibrosis..
Acetate, due to its chemical stability and biological activity, is widely used in the treatment of critically ill patients, especially in cases of shock, acute hypotension, etc., to restore hemodynamic stability by rapidly raising blood pressure in a short period of time. Compared with direct injection of the original form of DRVYIHPF, the acetate form has better stability in solution, which helps reduce dose uncertainty and the risk of drug inactivation.
DRVYIHPF, abbreviated as DRVYIHPF, is a widely used drug in clinical practice. It is a key hormone in the renin angiotensin aldosterone system (RAAS), widely involved in regulating important physiological processes such as blood pressure, fluid balance, and vasoconstriction. Similar to the mechanism of action of DRVYIHPF, it mainly stimulates AT1 and AT2 receptors to exert physiological effects on systems such as blood vessels, heart, and kidneys, thereby effectively treating conditions such as hypotension and shock.By acting on the AT1 receptor, the G protein coupled receptor signaling pathway is activated, promoting an increase in intracellular calcium ions, which in turn causes the contraction of vascular smooth muscle.
clinical application
1. Used for the treatment of acute hypotension and shock
One of the main clinical applications of angiotensin II acetate is in the treatment of acute hypotension and shock. Shock is a common clinical emergency involving inadequate circulation and perfusion of blood, resulting in insufficient oxygen supply to tissues and organs. There are various types of shock, including septic shock, traumatic shock, low volume shock, etc., and most of these types are accompanied by vasodilation, leading to a sharp drop in blood pressure.
In these cases, its strong vasoconstrictive effect helps to rapidly increase the patient's blood pressure.
Thereby increasing peripheral vascular resistance and raising blood pressure. In addition, DRVYIHPF can help restore fluid balance by promoting the secretion of aldosterone and enhancing sodium reabsorption.
Typical application: Patients with multiple organ failure
In patients with multiple organ failure (MODS), especially those with severe infections or trauma, simple blood volume supplementation often cannot effectively restore blood flow perfusion due to the persistent presence of vasodilation and hypotension. At this point, the use can quickly correct hypotension and improve organ perfusion, avoiding irreversible damage caused by organ hypoxia.
2. Application in renal disease
Its application is not limited to the treatment of acute hypotension, but also plays an important role in the management of kidney disease. Long term hypotension or hypoperfusion can cause renal tubular failure, and in severe cases, may lead to irreversible damage to renal function. By utilizing its vasoconstrictive effect, it can effectively increase the perfusion pressure of the kidneys and maintain the glomerular filtration rate (GFR).
In some patients with chronic kidney disease, especially those with a tendency towards low blood pressure, using it can also help improve kidney function and prevent further deterioration.
3. Adjuvant therapy for cardiovascular diseases
It has also been applied in the acute management of cardiovascular diseases. For example, in patients with acute heart failure, increasing the preload and afterload of the heart through vasoconstriction can help increase the hemodynamic effects of the heart and improve its pumping function.
In the treatment process of restarting the heart after cardiac arrest, as a vasopressor drug, it can effectively increase blood pressure, ensure the perfusion of important organs such as the heart and brain, and reduce complications after cardiopulmonary resuscitation.
4. Combined use with other drugs
It is often used in combination with other drugs, especially in the treatment of critically ill patients, and is often used in combination with vasopressors such as norepinephrine and dopamine to achieve comprehensive hemodynamic support. This combination therapy can maximize the recovery of blood pressure and maintain blood flow perfusion in multiple organs, especially in organs such as the heart, brain, and kidneys that require high blood supply.
Mechanism of action in clinical practice
The core mechanism applied in clinical practice is its therapeutic effect on acute hypotension and shock. It helps critically ill patients restore hemodynamic stability by rapidly increasing blood pressure, especially in the following clinical situations where it has important applications:
1. Acute hypotension and shock
In various types of shock, especially septic shock, hemorrhagic shock, etc., its strong vasoconstrictive effect helps restore peripheral vascular resistance, rapidly increase blood pressure, and restore organ perfusion. This is because shock is usually accompanied by large-scale vasodilation and blood pressure drop. Through direct vasoconstriction, this hypotensive state can be quickly corrected, improving the perfusion of important organs.
2. Acute heart failure
When applied for the management of acute heart failure, this agent helps strengthen the heart's pumping function by elevating blood pressure and boosting cardiac preload. It acts by activating AT1 receptors, which intensifies myocardial contractility and improves venous blood return. Consequently, the overall pressure burden on the heart is effectively alleviated.
3. Hemodynamic support for high-risk patients
Commonly used for high-risk patients who require strong hemodynamic support, such as critically ill patients after surgery, patients with multiple organ failure, etc. By rapidly increasing blood pressure, angiotensin II acetate can help these patients maintain stable vital signs and prevent organ hypoperfusion.
Clinical advantages and indications
Has demonstrated unique advantages in the following aspects:
Due to its high stability and water solubility, blood vessels are suitable for long-term intravenous infusion, especially when patients require continuous blood pressure regulation. In contrast, traditional DRVYIHPF, due to its short half-life, is difficult to maintain long-lasting efficacy and requires more frequent dose adjustments.
In conditions such as acute hypotension and shock, it can quickly take effect and maintain hemodynamic stability continuously.
This is particularly important in severe hypotensive conditions such as septic shock and hemorrhagic shock, as it can help doctors quickly restore blood pressure and ensure organ perfusion.
Due to its stronger stability, more precise dosage adjustment, and more controllable patient response to medication, this helps to avoid the risk of excessive hypertension or insufficient medication.
Reference
1. Galletti, F., et al. (2020). *DRVYIHPFI: A key regulator of cardiovascular function*. Journal of Hypertension, 38(5), 783-792.
2. Joffe, S. P., & Singh, A. K. (2018). *DRVYIHPF in acute circulatory shock and sepsis*. Journal of Critical Care, 44, 153-160.
3. Fletcher, R. L., et al. (2017). *Pharmacokinetics and pharmacodynamics of DRVYIHPF in patients with shock*. Journal of Clinical Pharmacology, 57(12), 1549-1557.
4. Mendoza, A. S., et al. (2019). *The role of DRVYIHPF in the pathophysiology of hypertension and cardiovascular disease*. Journal of Clinical Hypertension, 21(9), 1281-1289.
5. Giapreza, INN-angiotensin2 acetate(https://www.ema.europa.eu/en/documents/product-information/giapreza-epar-product-information_en.pdf)
6. AngiotensinII Acetate(https://evsexplore.semantics.cancer.gov/evsexplore/concept/ncit/C142924)
FAQ
AngiotensinII Acetate is the acetate salt derivative of angiotensinII peptide, featuring the amino acid sequence DRVYIHPF. Once administered, it binds to specific receptors within the human body to exert a potent vasoconstrictive effect and elevate systemic blood pressure. This salt form fully preserves the intact biological activity of the original angiotensinII peptide. Clinically, it is widely applied for the intervention of hypotension, acute circulatory failure, as well as various categories of shock accompanied by unstable hemodynamic conditions.
Compared with pure DRVYIHPF peptide, AngiotensinII Acetate shows better water solubility, which simplifies the preparation of injection solutions. It also has improved chemical stability and higher bioavailability after administration. These superior physicochemical properties reduce the risk of activity degradation during use and storage, making it safer and more suitable for clinical injection.
This product is commercially available in the form of fine crystalline powder. For proper preservation, it needs to be placed inside a tightly sealed container and stored in a cool, dry and dark environment. Direct exposure to high temperatures, intense light and extreme humidity must be strictly avoided, since such unfavorable conditions are likely to destroy its inherent molecular structure and gradually diminish its pharmacological activity. Strict compliance with standardized storage guidelines can effectively maintain stable product quality and preserve its original performance throughout the entire shelf life.
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