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 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 models||Male Sprague Dawley rat myocardial infarction (MI) model|
|Formulation||Dissolved in DMSO and diluted in saline|
|Administration||Gastric gavage once daily|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 80 mg/mL|
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