(+)-Nebivolol - CAS 118457-15-1
Catalog number: 118457-15-1
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C22H25F2NO4
Molecular Weight:
405.44
COA:
Inquire
Targets:
Adrenergic Receptor
Description:
This active molecular is a β-adrenergic receptor antagonist. Dexnebivolol is an enantiomer of Nebivolol which is a β1 receptor blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and left ventricular failure in Europe. It is highly cardioselective under certain circumstances. In Apr 2015, US FDA approved an ANDA for nebivolol submitted by Amerigen. In Jan 2016, Forest Laboratories and the University of Chicago withdrew a phase II/III trial for Hypertension in patients with chronic obstructive pulmonary disease in USA .
Purity:
98%
Appearance:
Off-White Solid
Synonyms:
R67138; R-67138; R 67138; Dexnebivolol. (αR,α'R,2R,2'S)-α,α'-[Iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol]; [2R-[2R*[R*[R*(S*)]]]]-α,α'-[Iminobis(methylene)]bis[6-fluoro-3,4- dihydro-2H-1-benzopyran-2-methanol; (S,R,R,R)-Nebivolol; Dexnebivolol; R 67138; d-Nebivolol; '
Solubility:
Chloroform, DMSO, Methanol
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
treatment of hypertension and left ventricular failure
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Boiling Point:
No Data Available
Melting Point:
130-133°C
Density:
1.309g/cm3
InChIKey:
KOHIRBRYDXPAMZ-YHBROIRLSA-N
InChI:
InChI=1S/C22H25F2NO4/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/t17-,18-,21-,22+/m1/s1
Canonical SMILES:
C1CC2=C(C=CC(=C2)F)OC1C(CNCC(C3CCC4=C(O3)C=CC(=C4)F)O)O
Current Developer:
Duncan; Forest Laboratories; Janssen; Menarini
1.Chronic Nebivolol Treatment Suppresses Endothelin-1-Mediated Vasoconstrictor Tone in Adults With Elevated Blood Pressure.
Diehl KJ1, Stauffer BL1, Dow CA1, Bammert TD1, Brunjes DL1, Greiner JJ1, DeSouza CA2. Hypertension. 2016 Apr 25. pii: HYPERTENSIONAHA.115.06979. [Epub ahead of print]
Endothelin-1 (ET-1) plays a major role in the pathophysiology of hypertension and its associated cardiovascular risk. We tested the hypothesis that chronic nebivolol treatment reduces ET-1-mediated vasoconstrictor tone in adult humans with elevated blood pressure (BP). Furthermore, reducing ET-1 vasoconstrictor activity contributes to the improvement in endothelial vasodilator function associated with nebivolol treatment. Forty-two middle-aged adults with elevated BP (systolic BP ≥130 mm Hg or diastolic BP ≥85 mm Hg) completed a 3-month, double-blind, randomized, placebo controlled trial: 14 received nebivolol (8 men/6 women; 5 mg per day); 14 received metoprolol succinate (9 men/5 women; 100 mg per day); and 14 received placebo (9 men/5 women). Forearm blood flow (plethysmography) responses to selective (BQ-123: 100 nmol/min; 60 minutes) and nonselective (BQ-123+BQ-788 [50 nmol/min]; 60 minutes) ET-1 receptor blockade, as well as acetylcholine (4.
2.Effects of Carvedilol Compared to Nebivolol on Insulin Resistance and Lipid Profile in Patients With Essential Hypertension.
Ozyıldız AG1, Eroglu S2, Bal U1, Atar I1, Okyay K1, Muderrisoglu H1. J Cardiovasc Pharmacol Ther. 2016 Apr 18. pii: 1074248416644987. [Epub ahead of print]
BACKGROUND AND AIM: Beta-blockers have unfavorable effects on metabolic parameters in hypertensive treatment. New generation beta-blockers with vasodilatory capabilities are superior to traditional beta-blockers, but studies examining their effects on metabolic parameters are still lacking. This study aimed to compare the effects of 2 new generation beta-blockers, carvedilol and nebivolol, on insulin resistance (IR) and lipid profiles in patients with essential hypertension.
3.Fixed-dose combination therapy of nebivolol and valsartan for the treatment of hypertension.
Sander GE1, Fernandez C1, Giles TD1. Expert Rev Cardiovasc Ther. 2016 May;14(5):563-72. doi: 10.1586/14779072.2016.1167598. Epub 2016 Apr 7.
Recent large clinical trials have refuted earlier suggestions from the Joint National Committee 8 committee that less aggressive targets for blood pressure control were all that could be justified in most hypertensive patients. It now does appear that in fact "lower is better," with blood pressure targets < 120/80 mm Hg appropriate for many hypertensive patients. Two drug combinations are often indicated as initial therapy if a 20/10 mm Hg or greater blood pressure reduction is necessary to reach target. Combinations consisting of β-blockers and renin-angiotensin-aldosterone system inhibitors have previously been deemed "less effective," based on partially overlapping mechanisms of action and limited clinical trial evidence. Nebivolol is a vasodilating β1-selective blocker and β3- adrenoceptor agonist; β3-adrenoceptor activation increases nitric oxide concentrations and thus explains the vasodilatory effect. A recent 8-week randomized trial (N=4,161) in individuals with stage 1-2 hypertension demonstrated that single-pill fixed dose combinations (FDC) of nebivolol and valsartan, an angiotensin II subtype 1 receptor blocker, were more effective in reducing blood pressure than the corresponding monotherapies, with comparable tolerability.
4.Recent advances in the treatment of renal diseases with nebivolol: A literature review.
Shamekhi Amiri F1. Nephrol Ther. 2016 Apr 21. pii: S1769-7255(16)00046-8. doi: 10.1016/j.nephro.2016.01.011. [Epub ahead of print]
Reactive oxygen species play an important role in both acute and chronic kidney diseases. Chronic kidney disease is associated with various consequences to the cardiovascular system and metabolic profiles. Nebivolol, a highly cardioselective third-generation β-blocker, has nitric oxide (NO) induced vasodilation and antioxidant properties. Nebivolol affects the endothelial NO pathway in two complementary ways: it increases endothelial mediated NO expression and has antioxidant action, which leads to a decrease in degradation. Central blood pressure can be effectively lowered by nebivolol in the prehypertension phase. Clinically nebivolol's ability to modulate endothelial dysfunction may offer additional vascular protection in treating hypertension. As well, pre-treatment with 5mg nebivolol every 24 hours for 4 days is protective against nephrotoxic effects of contrast media. The aim of this study is to review the current literature on the efficacy and safety of nebivolol in the treatment of various states of renal diseases.
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Chemical Structure

CAS 118457-15-1 (+)-Nebivolol

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