Name | Nebivolol hydrochloride |
Synonyms | Nebilet R-67555 Nebilox Lobivon Narbivolol Nebivolol hcl Nebivolol hydrochloride RAC NEBIVOLOL, HYDROCHLORIDE NEBIVOLOLHYDROCHLORIDE(SUBJECTTOPATENTFREE) a,a(Iminodimethylene)bis[6-fluoro-2-chromanmethanol] Hydrochloride 2,2'-iminobis[1-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)ethanol] hydrochloride a,a'-[Iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol hydrochloride rel-(aR,a′R,2R,2′S)-a,a′-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] hydrochloride |
CAS | 152520-56-4 169293-50-9 |
EINECS | 1806241-263-5 |
InChI | InChI=1/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 |
Molecular Formula | C22H26ClF2NO4 |
Molar Mass | 441.8959464 |
Melting Point | 220-222°C |
Boling Point | 600.5°C at 760 mmHg |
Flash Point | 316.9°C |
Solubility | DMSO: ≥20mg/mL |
Vapor Presure | 2.88E-15mmHg at 25°C |
Appearance | White to off-white powder |
Color | white to off-white |
Merck | 14,6432 |
Storage Condition | room temp |
In vitro study | In the preparation of rabbit lung membranes, Nebivolol acts on beta 1-adrenoceptor sites with high affinity and high selectivity. (K I value of 0.9 nM,beta 2/beta 1 ratio of 50). Nebivolol acts selectively on β1-adrenoceptors in the presence of CGP 207.12 A (300 nM, K I β2) or ICI 118.551 (50 nM, K I β1), the value of K I (β2)/K I (β1) was 40.7 by 3H-CGP 12.1777 competition experiment. Nebivolol acts on coronary artery smooth muscle cells (haCSMCs) and endothelial cells (haECs) to reduce cell proliferation in a concentration-and time-dependent manner. Nebivolol treatment of hacsmcs for 7 days resulted in a significant decrease in cell growth, with an IC50 of 6.1 μm, and inhibited the accelerated haCSMC proliferation stimulated by growth factors PDGF-BB, bFGF, and TGFβ, the IC50 was 6.8 μm, 6.4 μm and 7.7 μm, respectively. 10-5 M Nebivolol treatment of haCSMCs for 48 hours induced moderate apoptosis, apoptosis reached 23%, and reduced the number of S-phase cells from 16% to 5%. |
In vivo study | Treatment of rats with myocardial infarction (MI) with Nebivolol (I. V. For the first 10 min, followed by oral treatment) decreased myocardial apoptosis, which could be regulated by NO. Nebivolol significantly blocked left ventricular (LV) pressure changes and reduced total and local apoptotic cardiomyocytes. Nebivolol treatment of rats with myocardial infarction slightly reduced mean blood pressure (MBP). |
Risk Codes | R22 - Harmful if swallowed R50/53 - Very toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment. |
Safety Description | S60 - This material and its container must be disposed of as hazardous waste. S61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
UN IDs | 3077 |
WGK Germany | 3 |
HS Code | 29322090 |