Nisoldipine (Sular) is a calcium channel blocker. It works by affecting the movement of calcium into the cells of the heart and blood vessels. As a result, it relaxes blood vessels and increases the supply of blood and oxygen to the heart while reducing its workload . [1, 2]
Cell Experiment | |
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Cell lines | Ventricular myocytes |
Preparation method | Bathing the myocytes in normal Tyrode's solution, held at -80 mV, and depolarised after 200-ms prepulses (-40mV) to more positive potentials for 500 ms at 0.1 Hz, recording tail currents on repolarisations to -40mV. Exposing the myocytes to 10-100 mM Nisoldipine for 8-10 minutes. Then using an EPC-7 amplifier to record the whole-cell membrane currents. |
Concentrations | Dissolved in DMSO, final concentration 10-100 μM |
Incubation time | 8-10 minutes |
Animal Experiment | |
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Animal models | Male Wistar rats with chronic intragastric ethanol exposure |
Formulation | Dissolved in DMSO and diluted in saline |
Dosages | 10 mg/kg |
Administration | Oral every day |
Molecular Weight | 388.41 |
Formula | C20H24N2O6 |
CAS Number | 63675-72-9 |
Solubility (25°C) | DMSO 70 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] R Heinig. Clinical pharmacokinetics of nisoldipine coat-core
[3] J Langan, et al. Nisoldipine CC: clinical experience in hypertension
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