Manidipine (Manyper) is a lipophilic, third-generation, highly vasoselective dihydropyridine calcium antagonist with an IC50 of 2.6 nM. It causes systemic vasodilation by inhibiting the voltage-dependent calcium inward currents in smooth muscle cells. It is used clinically as an antihypertensive. At a holding potential of −37 mV, manidipine decreased the Ca2+ current at concentrations above 0.1 nM, and abolished it at 100 nM. The voltage-dependent effect of manidipine on the Ca2+ current may explain the weak negative inotropism of manidipine in ventricular muscles, and provide an electrophysiological basis for its vascular selectivity.
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Source | Acta Pharmacol Sin (2007). Figure 5. Manidipine |
| Method | Immunohistochemical staining | |
| Cell Lines | 8-OHdG | |
| Concentrations | 50 μm | |
| Incubation Time | ||
| Results | Manidipine treatment also provided moderate relief of oxidative stress-related DNA injury |
 |
Source | Acta Pharmacol Sin (2007). Figure 3. Manidipine |
| Method | insulin staining | |
| Cell Lines | β-cell | |
| Concentrations | 50 μm | |
| Incubation Time | 6 weeks | |
| Results | β-cell mass was quite low in the db/db control group, and it was rescued greatly after 6 weeks’ treatment by both candesartan 1 mg/kg and 10 mg/kg |
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | stroke-prone spontaneously hypertensive rat |
| Formulation | |
| Dosages | 20 mg/kg |
| Administration | oral |
| Molecular Weight | 610.7 |
| Formula | C35H38N4O6 |
| CAS Number | 89226-50-6 |
| Solubility (25°C) | DMSO 100 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.
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