Metoprolol Tartrate

Синонимы: Metoprolol tartrate, 56392-17-7, 1-[4-(2-Methoxyethyl)phenoxy]-3-[(1-methylethyl)amino]-2-propanol tartrate, CGP 2175E, Lopressor, Seloken, Betaloc

Metoprolol tartrate is a cardioselective beta-1 adrenergic receptor blocker, structurally characterized by a phenoxypropanolamine core with a methoxyethyl side chain. This molecular configuration confers high affinity for beta-1 receptors located primarily in cardiac tissue, with minimal activity at beta-2 receptors in the lungs and vasculature. The tartrate salt enhances aqueous solubility, facilitating oral and parenteral formulation development.

As a second-generation beta-blocker, metoprolol tartrate is widely prescribed for hypertension, angina pectoris, and heart failure. It is also used in the management of arrhythmias and as an adjunct in myocardial infarction. The compound is available in immediate-release and extended-release forms, with the tartrate salt predominantly used in immediate-release tablets and injection solutions.

For pharmaceutical manufacturers, metoprolol tartrate API offers a well-established synthesis route and consistent crystalline form, ensuring reliable tableting and dissolution performance. Its compatibility with common excipients and stability under typical storage conditions make it a preferred choice for generic and branded formulations alike.

Chemical Structure & Properties

Metoprolol tartrate is a white to off-white crystalline powder with a molecular weight of 684.82 g/mol (as the tartrate salt). It is freely soluble in water and methanol, slightly soluble in ethanol, and practically insoluble in acetone. The tartrate counterion contributes to its stability and solubility profile, which is critical for injectable and oral solid dosage forms. The compound exists as a racemic mixture, with the S-enantiomer carrying the primary beta-blocking activity.

Механизм действия

• Beta-1 receptor blockade: Competitively inhibits catecholamine binding at beta-1 adrenergic receptors in the heart, reducing heart rate and cardiac output.
• Negative chronotropic and inotropic effects: Decreases sinoatrial node firing and myocardial contractility, lowering oxygen demand.
• Renin-angiotensin system modulation: Suppresses renin release from juxtaglomerular cells, contributing to blood pressure reduction.
• Membrane-stabilizing activity: At high concentrations, exhibits local anesthetic-like effects, though clinically negligible at therapeutic doses.

Quality Specifications

Supply & Documentation

• Capacity: 50 metric tons per year
• Срок выполнения заказа: 3–5 рабочих дней (товары, имеющиеся в наличии)
• Documentation: COA, MSDS, TDS, DMF available upon request
• Packaging: 25 kg fiber drum with double polyethylene liner, customized packaging available

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