Nebivolol (Bystolic) is a β1 receptor blocker with an IC50 of 4.5 µM. It has nitric oxide-potentiating vasodilatory effect used in treatment of hypertension. Nebivolol was compared with DETA-NO and S-nitroso-N-acetylpenicillamine (SNAP), two nitric oxide (NO) donor agents, and alpha-difluoromethylornithine (DFMO), a known inhibitor of ornithine decarboxylase (ODC). All four test agents inhibited RASMC proliferation in a concentration-dependent manner, with nebivolol being the most potent (IC (50) = 4.5 microM), whereas atenolol, another relatively selective beta (1)-blocker, was inactive.
| Cell Experiment | |
|---|---|
| Cell lines | Human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs) |
| Preparation method | Exposing cells to different concentrations of Nebivolol (10-7~10-5 M) for 1, 2, 4, 7 and 14 days. Using bromodeoxyuridine (BrdU) incorporation to analyze cell proliferation , and PI or annexin V staining to detect cell apoptosis . |
| Concentrations | Dissolved in 100% methanol and diluted with three volumes of growth medium to obtain a stock solution of 10-3 M, final concentration 10-7~10-5 M |
| Incubation time | 1, 2, 4, 7 and 14 days |
| Animal Experiment | |
|---|---|
| Animal models | Male Sprague Dawley rat myocardial infarction (MI) model |
| Formulation | Dissolved in DMSO and diluted in saline |
| Dosages | 2.0 mg/kg |
| Administration | Gastric gavage once daily |
| Molecular Weight | 441.9 |
| Formula | C22H25F2NO4.HCl |
| CAS Number | 152520-56-4 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Sarah J Wang, et al. Nebivolol/valsartan combination for the treatment of hypertension: a review
[2] Nasima Olawi, et al. Nebivolol in the treatment of arterial hypertension
[3] Dawn Battise, et al. Nebivolol/Valsartan: A Novel Antihypertensive Fixed-Dose Combination Tablet
[4] Justin Fongemie, et al. A Review of Nebivolol Pharmacology and Clinical Evidence
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