Animal Pharmacology of Nebivolol

Janssens, W. J.; Xhonneux, R.; Janßen, Paul

doi:10.1007/bf03258258

Cited by 16 publications

(12 citation statements)

References 27 publications

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“…Previous studies have shown remarkable vasodilating effects with minimal alterations of the metabolic profile. 22,23 However, there is little information available on its pharmacological effects in physically active hypertensive patients.…”

Section: Discussionmentioning

confidence: 99%

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Integrated effects of the vasodilating beta-blocker nebivolol on exercise performance, energy metabolism, cardiovascular and neurohormonal parameters in physically active patients with arterial hypertension

Mainka

Schillings

et al. 2001

J Hum Hypertens

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Objective: The present study was designed to investigate the integrated effects of the beta-1-selective blocker with vasodilator properties, nebivolol, on systemic haemodynamics, neurohormones and energy metabolism as well as oxygen uptake and exercise performance in physically active patients with moderate essential hypertension (EH). Design and methods: Eighteen physically active patients with moderate EH were included: age: 46.9 ؎ 2.38 years, weight: 83.9 ؎ 2.81 kg, blood pressure (BP): 155.8 ؎ 3.90/102.5 ؎ 1.86 mm Hg, heart rate: 73.6 ؎ 2.98 min −1 . After a 14-day wash-out period a bicycle spiroergometry until exhaustion (WHO) was performed followed by a 45-min submaximal exercise test on the 2.5 mmol/l lactate-level 48 h later. Before, during and directly after exercise testing blood samples were taken. An identical protocol was repeated after a 6-week treatment period with 5 mg nebivolol/day. Results: Nebivolol treatment resulted in a significant (P Ͻ 0.01) decrease in systolic and diastolic BP and heart

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Section: Discussionmentioning

confidence: 99%

“…22,23 A number of experimental and human pharmacological studies suggest that the vasodilatation is triggered via the endothelial nitrogen oxide system. The pharmacological profile is characterised by the significant antihypertensive effects as well as a lowering of cardiac pre-and after-load.…”

Section: Journal Of Human Hypertension (2001) 15 715-721mentioning

confidence: 99%

Integrated effects of the vasodilating beta-blocker nebivolol on exercise performance, energy metabolism, cardiovascular and neurohormonal parameters in physically active patients with arterial hypertension

Mainka

Schillings

et al. 2001

J Hum Hypertens

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“…Numerous biologically active natural products contain the butyrolactone ring system (77). Similarly, methyl α-aryl-α-ketoacetates (97) have been reduced to methyl (R)- (98) or (S)-mandelates, useful intermediates in the synthesis of, among other compounds, optically active 4-aryl-2-hydroxytetronic acids (99) (78). These acidic compounds are aci-reductones which possess a low redox potential and numerous biological activities including reactive radical scavenging, cyclooxygenase inhibition, and antilipidemic properties.…”

Section: Asymmetric Induction Methodologiesmentioning

confidence: 99%

“…The hemodynamic effects cannot be explained by β 1adrenergic antagonism of the (+ )-isomer and this effect is not shared by other β-blockers. The mechanism of the observed synergy between the two enantiomers is not known (98).…”

Section: Antihypertensive Agentsmentioning

confidence: 99%

Pharmaceuticals, Chiral

Witiak¹,

Hopper²

2000

Kirk-Othmer Encyclopedia of Chemical Technology

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Stereospecific structure-activity relationships are of sufficient complexity to warrant a clear understanding of the terms involved. Prior to discussing these relationships the following definitions are offered. Stereoisomers are compounds which have the same molecular formula but differ in the arrangement of their atoms in space. Chiral compounds are compounds which have nonsuperimposable mirror images. Enantiomers are pairs of stereoisomers which are nonsuperimposable mirror images; they possess identical physical and chemical properties within an achiral environment. Stereoisomers other than enantiomers, ie, diastereomers, are identified by distinct physical and chemical properties including melting points, spectral characteristics, and rates of reaction with both chiral and achiral reactants. Enantiomers, however, are only distinguished when in the presence of a homochiral environment such as polarized light, chiral solvents, chiral reagents, or chiral molecules such as biomolecules, eg, nucleic acids (qv), proteins (qv), and carbohydrates (qv). The two molecules in a pair of enantiomers rotate a plane of polarized light with equal intensities, but in opposite directions. The dextrorotatory isomer (+ or d) rotates the plane of polarized light clockwise; the levorotatory isomer (− or l) rotates the plane of polarized light counterclockwise. An equal mixture of (+ ) and (−)-enantiomers is a racemic mixture or racemic compound and does not rotate a plane of polarized light. Optical rotation, an intrinsic property of the substance, has no bearing on drug-macromolecule interactions. It is the absolute configuration of the homochiral compound that is important for its interaction with biomolecules.Absorption, metabolism, and biological activities of organic compounds are influenced by molecular interactions with asymmetric biomolecules. These interactions, which involve hydrophobic, electrostatic, inductive, dipole-dipole, hydrogen bonding, van der Waals forces, steric hindrance, and inclusion complex formation give rise to enantioselective differentiation (1, 2). Within a series of similar structures, substantial differences in biological effects, molecular mechanism of action, distribution, or metabolic events may be observed. For example, (R)-carvone [6485-40-1] (1) has the odor of spearmint whereas (S)-carvone [2244-16-8] (2) has the odor of caraway (3, 4).

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“…Nebivolol is cardioselective, demonstrating very high affinity for the β 1 receptor and a 50-fold lower affinity for β 2 receptors [8]. The drug is a racemic mixture of two enantiomers, dand l-nebivolol [9]. The β 1 blocking activity of the agent resides in d-nebivolol, which shows a more than 100-fold greater affinity for β 1 receptors compared to l-nebivolol.…”

Section: Nebivololmentioning

confidence: 98%

New drugs for hypertension: What do they offer?

Gradman

Vivas²

2006

Current Science Inc

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A new drug might make a positive contribution to existing therapies for hypertension by: 1) reducing blood pressure (BP) via a novel pharmacologic mechanism; 2) possessing pharmacologic or pharmacokinetic properties that make it superior to other members of its class; or 3) facilitating BP control in refractory patients. In this paper, we review four experimental agents that promise to advance therapeutics by one of these mechanisms. Aliskiren is the first in a new class of potent, orally effective renin inhibitors. Aliskiren produces dose-dependent BP reduction with few side effects and constitutes a novel pharmacologic approach to renin-angiotensin-aldosterone inhibition. Nebivolol is a third-generation, cardioselective beta-blocker that produces vasodilation and improves endothelial function via the l-arginine/nitric oxide pathway. Clevidipine is an ultra-short-acting, vascular-selective, dihydropyridine calcium antagonist that is being developed for intravenous use in acute hospitalized patients. Darusentan is an endothelin(A) selective endothelin receptor antagonist that is effective in achieving BP control in a significant percentage of patients who remain uncontrolled despite treatment with three or more antihypertensive drugs.

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Animal Pharmacology of Nebivolol

Cited by 16 publications

References 27 publications

Integrated effects of the vasodilating beta-blocker nebivolol on exercise performance, energy metabolism, cardiovascular and neurohormonal parameters in physically active patients with arterial hypertension

Integrated effects of the vasodilating beta-blocker nebivolol on exercise performance, energy metabolism, cardiovascular and neurohormonal parameters in physically active patients with arterial hypertension

Pharmaceuticals, Chiral

New drugs for hypertension: What do they offer?

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