Nebivolol
(Synonyms: Bystolic,R 065824) 目录号 : GC25663Nebivolol (Bystolic,R 065824) is a β1 receptor blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and also for left ventricular failure.
Cas No.:118457-14-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Nebivolol (Bystolic,R 065824) is a β1 receptor blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and also for left ventricular failure.
| Cas No. | 118457-14-0 | SDF | Download SDF |
| 别名 | Bystolic,R 065824 | ||
| 分子式 | C22H25F2NO4 | 分子量 | 405.43 |
| 溶解度 | DMSO: 88 mg/mL (217.05 mM);; | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4665 mL | 12.3326 mL | 24.6652 mL |
| 5 mM | 0.4933 mL | 2.4665 mL | 4.933 mL |
| 10 mM | 0.2467 mL | 1.2333 mL | 2.4665 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Nebivolol in the treatment of arterial hypertension
Basic Clin Pharmacol Toxicol 2019 Sep;125(3):189-201.PMID:31066991DOI:10.1111/bcpt.13248.
This MiniReview reports the current knowledge about the treatment of arterial hypertension with the third-generation beta-adrenoceptor antagonist (BAA) Nebivolol. Furthermore, it reviews the advantages of Nebivolol compared to the earlier generation of BAAs with respect to their different pharmacological properties. Beta-adrenoceptor antagonists are a class of drugs applied for several different conditions, including hypertension and heart failure. They differ significantly in their pharmacological properties, including varying β1 /β2 -selectivity and/or exertion of additive effects on the heart and circulation. Although these drugs have been a part of hypertensive therapy for about 40 years, the outcome of large clinical trials has put the role of BAAs into question. However, most of these results were based on first- and second-generation BAAs and cannot be translated directly into third-generation drugs. The third-generation BAA Nebivolol has the highest β1 -selectivity seen so far, together with additional vasodilating and anti-oxidative properties. It is currently applied in the treatment of hypertension and congestive heart failure. Nebivolol has a unique pharmacological profile, despite showing similar blood pressure-lowering effects, and has certain advantages in the treatment of hypertension compared to the previous generations of BAAs. This includes significant improvements in endothelial dysfunction, central haemodynamics and the degree of erectile dysfunction in men, a neutral/beneficial metabolic profile and lastly a more favourable side effect profile. It is widely beneficial for, for example, sexually active men and patients with comorbidities such as type II diabetes mellitus, metabolic syndrome and chronic obstructive lung disorders. Whether the advantages translate to an improved long-term clinical outcome remains to be clarified, and ongoing prospective studies will show this in the future.
Nebivolol/valsartan combination for the treatment of hypertension: a review
Future Cardiol 2021 Jul;17(4):573-583.PMID:33064027DOI:10.2217/fca-2020-0079.
Nebivolol (N) is a β1-adrenoreceptor antagonist that is approved for treatment of hypertension in the USA. Effective treatment of hypertension is becoming an increasingly difficult process that often requires multiple drug combinations to meet target guidelines. This has resulted in the increasing introduction of multidrug single-pill combinations (SPCs) to facilitate cost and compliance issues. Some of the SPCs have added valsartan (V), an angiotensin receptor blocker, which is an increasingly advocated antihypertensive class. Pharmacological profiles of N and V, alone and combined, are well characterized. In 2007, the SPC of N and V, 5 and 80 mg, respectively, was approved by the US FDA for treatment of hypertension. This paper will summarize and update key issues in pharmacology, clinical use and benefit.
A Review of Nebivolol Pharmacology and Clinical Evidence
Drugs 2015 Aug;75(12):1349-71.PMID:26177892DOI:10.1007/s40265-015-0435-5.
Nebivolol is a highly selective β1-adrenergic receptor antagonist with a pharmacologic profile that differs from those of other drugs in its class. In addition to cardioselectivity mediated via β1 receptor blockade, Nebivolol induces nitric oxide-mediated vasodilation by stimulating endothelial nitric oxide synthase via β3 agonism. This vasodilatory mechanism is distinct from those of other vasodilatory β-blockers (carvedilol, labetalol), which are mediated via α-adrenergic receptor blockade. Nebivolol is approved for the treatment of hypertension in the US, and for hypertension and heart failure in Europe. While β-blockers are not recommended within the current US guidelines as first-line therapy for treatment of essential hypertension, Nebivolol has shown comparable efficacy to currently recommended therapies in lowering peripheral blood pressure in adults with hypertension with a very low rate of side effects. Nebivolol also has beneficial effects on central blood pressure compared with other β-blockers. Clinical data also suggest that Nebivolol may be useful in patients who have experienced erectile dysfunction while on other β-blockers. Here we review the pharmacological profile of Nebivolol, the clinical evidence supporting its use in hypertension as monotherapy, add-on, and combination therapy, and the data demonstrating its positive effects on heart failure and endothelial dysfunction.
Nebivolol/Valsartan: A Novel Antihypertensive Fixed-Dose Combination Tablet
Ann Pharmacother 2019 Apr;53(4):402-412.PMID:30449127DOI:10.1177/1060028018813575.
Data sources: A PubMed (1966 to October 2018) search was conducted using the following keywords: Nebivolol, valsartan, and hypertension (HTN). Additional sources were identified by references. Study selection and data extraction: Articles written in English were included if they evaluated the pharmacology, pharmacokinetics, efficacy, safety, or place in therapy of Nebivolol/valsartan in human subjects. Data synthesis: Most patients with HTN require combination therapy; however, β-adrenergic antagonists and AII type 1 receptor blockers have been considered less effective because of overlapping mechanisms of action. A phase III, randomized trial demonstrated that Nebivolol/valsartan produced statistically significant blood pressure (BP) lowering as compared with monotherapy with the individual components or placebo. Substudy analyses confirmed this among subgroups and demonstrated that Nebivolol/valsartan decreased plasma renin and aldosterone levels. One trial reported continued BP lowering at 52 weeks. Another study showed that Nebivolol/valsartan had similar additivity scores as compared with other antihypertensive combinations. Relevance to Patient Care and Clinical Practice: This review discusses drug information, efficacy, and safety of Nebivolol/valsartan and discusses its clinical relevance as a novel combination product in managing patients with HTN. Conclusion: Nebivolol/valsartan combination may offer a benefit to patients with an indication for both classes who desire to decrease pill burden. Although BP lowering was statistically significant in comparison to the individual components as monotherapy, the combination does not offer clinically significant benefits that would elevate its place in HTN management.
Randomized trial to determine the effect of Nebivolol on mortality and cardiovascular hospital admission in elderly patients with heart failure (SENIORS)
Eur Heart J 2005 Feb;26(3):215-25.PMID:15642700DOI:10.1093/eurheartj/ehi115.
Aims: Large randomized trials have shown that beta-blockers reduce mortality and hospital admissions in patients with heart failure. The effects of beta-blockers in elderly patients with a broad range of left ventricular ejection fraction are uncertain. The SENIORS study was performed to assess effects of the beta-blocker, Nebivolol, in patients >/=70 years, regardless of ejection fraction. Methods and results: We randomly assigned 2128 patients aged >/=70 years with a history of heart failure (hospital admission for heart failure within the previous year or known ejection fraction Nebivolol (titrated from 1.25 mg once daily to 10 mg once daily), and 1061 to placebo. The primary outcome was a composite of all cause mortality or cardiovascular hospital admission (time to first event). Analysis was by intention to treat. Mean duration of follow-up was 21 months. Mean age was 76 years (SD 4.7), 37% were female, mean ejection fraction was 36% (with 35% having ejection fraction >35%), and 68% had a prior history of coronary heart disease. The mean maintenance dose of Nebivolol was 7.7 mg and of placebo 8.5 mg. The primary outcome occurred in 332 patients (31.1%) on Nebivolol compared with 375 (35.3%) on placebo [hazard ratio (HR) 0.86, 95% CI 0.74-0.99; P=0.039]. There was no significant influence of age, gender, or ejection fraction on the effect of Nebivolol on the primary outcome. Death (all causes) occurred in 169 (15.8%) on Nebivolol and 192 (18.1%) on placebo (HR 0.88, 95% CI 0.71-1.08; P=0.21). Conclusion: Nebivolol, a beta-blocker with vasodilating properties, is an effective and well-tolerated treatment for heart failure in the elderly.