Nebivolol hydrochloride

Nebivolol Hydrochloride is a third-generation β-adrenergic receptor antagonist (β-blocker) used for the treatment of essential hypertension and chronic heart failure. Unlike conventional β-blockers, Nebivolol Hydrochloride uniquely combines highly selective β₁-adrenergic receptor antagonist properties with nitric oxide-mediated vasodilatory actions and beneficial effects on endothelial function. Nebivolol Hydrochloride is approximately 40-fold selective for β₁ versus β₂ receptors, and its vasodilatory activity is attributed to an interaction with the L-arginine/NO pathway. Nebivolol Hydrochloride also exhibits antioxidant properties and a favorable metabolic profile. In quality control contexts, Nebivolol Hydrochloride is associated with various pharmacopeial and non-pharmacopeial impurities, including Nebivolol Hydrochloride Impurity C, 4-hydroxy Nebivolol Hydrochloride, and N-nitroso Nebivolol Hydrochloride, which serve as critical reference standards for analytical method development, method validation, and ANDA submissions. The compound is supplied as a white to almost white powder to crystal with a melting point of 223.0 to 228.0 °C, and is stored at room temperature in a cool, dark place under inert gas due to its hygroscopic nature.

Product Parameters

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Parameter	Specification
Product Name	Nebivolol Hydrochloride
CAS Number	152520-56-4
CAS Number	118457-14-0
Molecular Formula	C₂₂H₂₅F₂NO₄·HCl
Molecular Weight	441.90 g/mol
Physical Form	Solid
Appearance	White to almost white powder
Melting Point	220.0–222.0 °C
Storage Condition	Room temperature

 

Bioactivity

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In rabbit lung β1-adrenergic receptor binding assays, Nebivolol HCl (R-65824) selectively blocks β1 receptors with an IC50 value of 0.8 nM.

 

In Vitro Study

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During the preparation of rabbit pleura, Nebivolol exhibits high affinity and remarkable selectivity for binding to beta1-adrenergic receptor sites (Ki value: 0.9 nM; beta2/β1 ratio: 50). Nebivolol demonstrates selective action on β1-adrenergic receptors; in the presence of CGP207.12A (300 nM, Kiβ2) or ICI118.551 (50 nM, Kiβ1), competitive assays using ³H-CGP12.1777 revealed a Ki(β2)/Ki(β1) ratio of 40.7. Nebivolol inhibits cell proliferation in coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs), with this effect being concentration-and time-dependent. Treatment of haCSMCs with Nebivolol for 7 days significantly reduced cell growth, with an IC50 of 6.1 μM; it also inhibited proliferation stimulated by growth factors PDGF-BB, bFGF, and TGFβ, with IC50 values of 6.8 μM, 6.4 μM, and 7.7 μM, respectively. Treatment of haCSMCs with 10⁻⁵ M Nebivolol for 48 hours induced moderate apoptosis (23%) and reduced the proportion of cells in the S phase from 16% to 5%.

 

In Vivo Studies

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Nebivolol (administered via intravenous injection for the initial 10 minutes followed by oral administration) treated rats with myocardial infarction (MI), reducing myocardial apoptosis through NO-mediated regulation. NebivChemicalbookolol significantly inhibited left ventricular (LV) pressure fluctuations and decreased both total and localized apoptotic myocardial cells. Treatment with nebolol in MI rats slightly reduced mean blood pressure (MBP).

 

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