Nebivolol

CAS# 152520-56-4

Nebivolol

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Chemical structure

Nebivolol

3D structure

Chemical Properties of Nebivolol

Cas No. 152520-56-4 SDF Download SDF
PubChem ID 11626384 Appearance Powder
Formula C22H26ClF2NO4 M.Wt 441.9
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 100 mg/mL (226.30 mM; Need ultrasonic)
Chemical Name (1S)-1-[(2R)-6-fluoro-3,4-dihydro-2H-chromen-2-yl]-2-[[(2S)-2-[(2S)-6-fluoro-3,4-dihydro-2H-chromen-2-yl]-2-hydroxyethyl]amino]ethanol;hydrochloride
SMILES C1CC2=C(C=CC(=C2)F)OC1C(CNCC(C3CCC4=C(O3)C=CC(=C4)F)O)O.Cl
Standard InChIKey JWEXHQAEWHKGCW-BIISKSHESA-N
Standard InChI InChI=1S/C22H25F2NO4.ClH/c23-15-3-7-19-13(9-15)1-5-21(28-19)17(26)11-25-12-18(27)22-6-2-14-10-16(24)4-8-20(14)29-22;/h3-4,7-10,17-18,21-22,25-27H,1-2,5-6,11-12H2;1H/t17-,18-,21-,22+;/m0./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Nebivolol

DescriptionHighly selective β1-adrenoceptor antagonist (Ki values are 0.88, 20, 44, 700, 1160, 2400 and 4000 nM at β1, 5-HT1A, β2, 5-HT2, α1, H1 and D2 receptors respectively). Induces vasodilation via a nitric oxide- and cGMP-dependent mechanism (EC50 = 11.36 μM in renal arteries) and displays antihypertensive activity in vivo. GRK/β -arrestin biased agonist at the β2 adrenoceptor.

Nebivolol Dilution Calculator

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Nebivolol Molarity Calculator

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Preparing Stock Solutions of Nebivolol

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.263 mL 11.3148 mL 22.6296 mL 45.2591 mL 56.5739 mL
5 mM 0.4526 mL 2.263 mL 4.5259 mL 9.0518 mL 11.3148 mL
10 mM 0.2263 mL 1.1315 mL 2.263 mL 4.5259 mL 5.6574 mL
50 mM 0.0453 mL 0.2263 mL 0.4526 mL 0.9052 mL 1.1315 mL
100 mM 0.0226 mL 0.1131 mL 0.2263 mL 0.4526 mL 0.5657 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Nebivolol

Nebivolol hydrochloride selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.

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References on Nebivolol

Differential Metabolic Effects of Beta-Blockers: an Updated Systematic Review of Nebivolol.[Pubmed:28283926]

Curr Hypertens Rep. 2017 Mar;19(3):22.

Blood pressure management in hypertensive patients with metabolic abnormalities is challenging, since many of the antihypertensive drugs adversely affect metabolism. Besides effective control of blood pressure in patients with hypertension, third-generation beta-blockers such as Nebivolol offer additional benefits for central hemodynamics and neutral or beneficial effects on metabolism. Emerging clinical data suggest that Nebivolol also has similar effects on metabolism in obese hypertensive and hypertensive diabetic patients. The present article will provide a systematic analysis of the pathophysiological links among hypertension, insulin resistance, and metabolic syndrome. We will also summarize the available clinical evidence regarding the metabolic effects of beta-blockers in hypertensive patients, with an emphasis on Nebivolol. Nebivolol exerts neutral or beneficial effects on insulin sensitivity and lipid metabolism in hypertensive patients, owing to its nitric oxide-mediated vasodilatory and antioxidative properties. Thus, Nebivolol could be a favorable therapeutic option for the treatment of hypertension in patients with impaired glucose and lipid metabolism.

The Comparison of the Effects of Nebivolol and Metoprolol on Erectile Dysfunction in the Cases with Coronary Artery Bypass Surgery.[Pubmed:28302931]

Ann Thorac Cardiovasc Surg. 2017 Apr 20;23(2):91-95.

PURPOSE: Beta-blocker use is common in the cases with coronary artery bypass surgery. According to the literature, beta-blockers have positive effects but may cause erectile dysfunction (ED). The most commonly used beta-blockers in ischemic cardiac disease are Nebivolol and metoprolol. In our clinic, we aimed to compare the effects of Nebivolol and metoprolol succinate on ED in the sexually active cases with coronary artery bypass surgery. METHODS: In our clinic, a total of 119 patients with coronary artery bypass surgery were included in the study. International Index of Erectile Function (IIEF-5) Test was used to evaluate whether the patients had ED and to grade the cases. RESULTS: No significant difference was found in terms of anti-ischemic efficacy between metoprolol succinate and Nebivolol in the postoperative period; however, the incidence of any grade ED was %85.96 in Group 1, %83.87 in Group 2. This difference was considered as statistically significant (p = 0.036). CONCLUSION: Beta-blocker use increases the risk of ED in cases with ischemic cardiac disease. We suggest that the complaints of ED could be less frequent with Nebivolol use in sexually active cases with ischemic cardiac disease.

Photolytic degradation of the beta-blocker nebivolol in aqueous solution.[Pubmed:28340419]

Water Res. 2017 Jun 1;116:211-219.

Nebivolol (NEB) is one of the top-sold prescription drugs belonging to the third generation of beta-blockers. However, so far, occurrence data in the environment are lacking. Within this study NEB has been found for the first time in effluent samples of wastewater treatment plants in Germany with an average concentration of 13 ng L(-1). Its photodegradation behavior in the environment and in technical processes is largely unknown. To fill this gap, three different UV treatment procedures (UV-C at 254 nm, UV-B at 312 nm and UV-A at 365 nm) were investigated in three different matrices: pure water, pure water in presence of the hydroxyl radical (OH) scavenger tert.-butanol and real wastewater. No elimination was observed during UV-A treatment. In contrast, NEB degradation during UV-B and UV-C treatment followed pseudo first order reaction kinetics, with highest removal rate during UV-C treatment in pure water (k = 7.8 x 10(-4) s(-1)). The rate constant for UV-C irradiation decreased to 2.9 x 10(-4) s(-1) in the presence of the OH scavenger and in the presence of the wastewater matrix. The rate constant for the UV-B lamp was 4.4 x 10(-4) s(-1), Three transformation products were identified after UV-B and UV-C photolytic degradation using high resolution mass spectrometry. The main photoreaction is the substitution of the fluorine atoms of NEB by hydroxyl groups. A photolytic cleavage of the CF bond can be excluded as the high bond dissociation energy of aromatic CF bonds (525 kJ mol(-1)), exceeds the energy of electromagnetic radiation applied in the present study (>/=254 nm, i.e., max. 471 kJ E(-1)). The quantum yields for NEB degradation for the UV-C lamp achieved in pure water, the OH scavenged system and wastewater matrix were Phideg = 0.53, 0.19 and 0.22, respectively. For UV-B Phideg was 0.023 +/- 0.003, noticeable differences in quantum yield were not found. The photooxidation involves reactive oxygen species such as superoxide and singlet oxygen. These oxidative species may be formed upon reaction of photo-excited NEB with oxygen.

Nebivolol attenuates cerebral vasospasm both by increasing endothelial nitric oxide and by decreasing oxidative stress in an experimental subarachnoid haemorrhage.[Pubmed:28335640]

Br J Neurosurg. 2017 Aug;31(4):439-445.

OBJECTIVE: Evidence suggests that reduction of nitric oxide (NO) bioavailability due to oxidative stress plays a central role in the pathophysiology of cerebral vasospasm after subarachnoid haemorrhage (SAH). To prevent SAH-induced cerebral vasospasm, therefore we used Nebivolol hydrochloride as a NO-mediated vasodilator and an antioxidant drug in an experimental rat model of SAH. MATERIALS AND METHODS: Forty female Wistar rats were divided into control, SAH, SAH plus placebo, and SAH plus Nebivolol groups. Starting six hours after inducing SAH, 5 mg/kg of Nebivolol hydrochloride and of pharmaceutical excipients of Nebivolol was given orally once daily for five days to SAH plus Nebivolol and SAH plus placebo groups, respectively. The lumen diameter and vessel wall thickness of the basilar artery were measured in brain sections. The serum and brain supernatant levels of nitric oxide (NO) were analysed. The brain supernatant levels of intrinsic antioxidants superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) were measured as markers of the antioxidant status. RESULTS: Nebivolol administration attenuated cerebral vasospasm both by increasing NO levels and by decreasing oxidative stress. Our study also demonstrated that Nebivolol administration reverses SAH created imbalance between SOD and GSH-Px by increasing GSH-Px activity relative to SOD. CONCLUSIONS: Nebivolol attenuates the cerebral vasospasm after SAH both increasing NO levels and decreasing oxidative stress. Therefore, it may promise to prevent SAH-induced cerebral vasospasm as an anti-spasmodic and anti-oxidant agent.

Description

Nebivolol hydrochloride selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.

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