Perindopril Erbumine is the stable form of perindopril, which is a long-acting ACE inhibitor used to treat high blood pressure, heart failure, or stable coronary artery disease.
CAT No: 10-101-120
CAS No:82834-16-0 (net), 107133-36-8 (erbumine)
Synonyms/Alias:S-9490-3; McN-A-2833-109; [(S)-1-Ethoxycarbonylbutyl]-Ala-Oic-OH t-butyl-amine salt; (2S,3aS,7aS)-1-[(2S)-2-[[(1S)-1-(Ethoxycarbonyl)butyl]amino]-1- oxopropyl]octahydro-1H-indole-2-carboxylic acid tert-butylammonium salt
Perindopril Erbumine, also known as perindopril tert-butylamine, is a prominent member of the angiotensin-converting enzyme (ACE) inhibitor class, widely recognized for its unique chemical structure and notable biological activity. As a synthetic derivative, Perindopril Erbumine exhibits a high degree of solubility and stability, making it an attractive choice for research applications involving enzyme modulation and cardiovascular system studies. Its molecular configuration allows for precise interaction with ACE, facilitating in-depth investigations into the regulation of vascular tone and the renin-angiotensin system. Researchers value the compound for its versatility in experimental design, as it serves as a reliable tool for elucidating the mechanisms underlying blood pressure regulation, endothelial function, and related physiological processes.
Cardiovascular Research: Perindopril Erbumine is extensively utilized in cardiovascular research to explore the modulation of blood pressure and vascular resistance. By inhibiting angiotensin-converting enzyme activity, it provides a robust model for studying the downstream effects on vasodilation, arterial compliance, and the interplay between various vasoactive peptides. Investigators leverage its properties to dissect the cellular and molecular pathways involved in hypertension, heart remodeling, and the adaptive responses of the cardiovascular system to hemodynamic stress. This research is vital for expanding the scientific understanding of cardiovascular homeostasis and the development of novel therapeutic strategies.
Renin-Angiotensin System Studies: In the context of renin-angiotensin system (RAS) studies, perindopril tert-butylamine serves as an indispensable agent for probing the complex regulatory network that governs fluid and electrolyte balance. Its ability to selectively inhibit ACE enables researchers to delineate the contributions of angiotensin II and related peptides in renal physiology and systemic vascular resistance. Experimental models employing this compound provide insights into the feedback mechanisms that maintain blood volume and pressure, as well as the pathophysiological alterations observed in conditions such as salt-sensitive hypertension and heart failure.
Endothelial Function Analysis: The use of Perindopril Erbumine in endothelial function analysis has become increasingly prominent, particularly in studies examining nitric oxide bioavailability and oxidative stress. By modulating the activity of ACE, the compound influences the production of vasoactive substances, which in turn affect endothelial cell signaling and vascular reactivity. Researchers employ it to investigate the molecular basis of endothelial dysfunction, a key factor in the progression of atherosclerosis and other vascular disorders. These studies contribute to a deeper understanding of the interplay between endothelial health and systemic vascular function.
Pharmacological Screening: In pharmacological screening assays, perindopril tert-butylamine is employed as a reference inhibitor for evaluating the potency and selectivity of novel ACE inhibitors and related compounds. Its well-characterized activity profile allows for the standardized assessment of new chemical entities, facilitating the identification of promising candidates for further development. The compound's predictable interaction with ACE provides a benchmark for comparative studies, enabling the optimization of structure-activity relationships and the refinement of lead compounds in drug discovery pipelines.
Metabolic and Biochemical Pathway Exploration: Beyond its primary role in cardiovascular and renal research, Perindopril Erbumine is used to investigate broader metabolic and biochemical pathways influenced by ACE activity. Studies involving this compound shed light on the cross-talk between the renin-angiotensin system and metabolic regulation, including glucose homeostasis, lipid metabolism, and inflammatory signaling. Researchers utilize it to unravel the systemic effects of ACE inhibition, thereby contributing to the expanding field of cardio-metabolic research and the identification of novel molecular targets.
Signal Transduction Research: The application of perindopril tert-butylamine extends to the study of intracellular signaling pathways modulated by ACE and angiotensin peptides. Its use in cell culture and animal models allows for the detailed analysis of kinase cascades, transcription factor activation, and gene expression changes triggered by alterations in the renin-angiotensin axis. These investigations are essential for understanding the molecular underpinnings of vascular remodeling, fibrosis, and cellular adaptation to chronic hemodynamic stress, ultimately advancing the frontiers of cardiovascular and metabolic research.
The methods of theoretical chemistry have been used to elucidate molecular properties of the antihypertensive, cardiovascular protective and antithrombotic perindopril ((2S,3aS,7aS)-1-[(2S)-2-[[(2S)-1-ethoxy-1-oxopentan-2-yl]amino]propanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carboxylic acid). The geometries and energies of various neutral and ionized complexes of perindopril erbumine and perindopril l-arginine have been computed using HF/6-31G(d) and Becke3LYP/6-31G(d) methods. The calculations showed that in both, the isolated state and water solution perindopril erbumine exists as a neutral complex. In the gas-phase perindopril l-arginine both neutral and ionic complexes are, at the HF level of theory, almost equally stable. The B3LYP level of theory slightly favors single proton transfer complex perindopril l-arginine (by about 14 kJ mol(-1)). In polar solvents like water, the ionized form of perindopril l-arginine becomes much more favored. According to our calculations l-arginine is bound to perindopril more strongly (by about 25 kJ mol(-1)) than erbumine.
Remko, M. (2009). Molecular structure and stability of perindopril erbumine and perindopril L-arginine complexes. European journal of medicinal chemistry, 44(1), 101-108.
Approximately 25% of US adults have high blood pressure (BP). Selection of effective and safe antihypertensive therapy for these individuals is an important health-care priority. High BP can be treated with a wide range of antihypertensive agents from a number of different classes. These drugs may differ in their suitability for administration to different subpopulations of patients. Results from both clinical trials and postmarketing surveillance indicate that the angiotensin-converting enzyme (ACE) inhibitor perindopril erbumine is safe and well tolerated in a wide range of patients with hypertension. Cough, the most common ACE inhibitor-associated side effect, is also the most common clinical adverse event reported for perindopril, but <2% of perindopril-treated patients discontinue therapy because of cough. Other adverse events often associated with ACE inhibitors, first-dose hypotension and hyperkalemia, appear to occur less often with perindopril than with other agents in this class. The favorable safety profile for perindopril extends to a wide range of patients, including the elderly and those with either heart failure or renal disease. Perindopril has no negative effects on lipids in patients with hyperlipidemia or on glycemic control in patients with type 2 diabetes mellitus, and it reduces proteinuria in patients with renal disease. Perindopril has no known clinically significant drug-drug interactions. Thus, perindopril is a safe BP-lowering agent with documented tolerability in a wide range of patients with hypertension.
Clark, L. T. (2001). Safety profile of perindopril. The American journal of cardiology, 88(7), 36-40.
The present study was performed to compare the bioavailability of two perindopril erbumine (CAS 107133-36-8) 4 mg tablet formulations (test formulation and reference formulation). This study was a randomized, single-blind, two-period, two-sequence cross-over study which included 20 healthy adult male and female subjects under fasting conditions. In this study, one subject withdrew from the study and one reserve subject did not appear at both periods. The pharmacokinetic parameters were assessed based on the concentrations of perindopril (CAS 82834-16-0) and perindoprilat (CAS 95153-31-4) because perindopril has litte pharmacologic activity until hydrolized in the liver into its active metabolite, perindoprilat.
Setiawati, E., Deniati, S. H., Yunaidi, D. A., Handayani, L. R., Santoso, I. D., Arland, J. A., ... & Lian, L. Y. (2011). Bioequivalence study of two perindopril erbumine tablet formulations in healthy volunteers. Arzneimittelforschung, 61(04), 234-238.
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