Molecular Formula | C19H20N2O7 |
Molar Mass | 388.37 |
Density | 1.284±0.06 g/cm3(Predicted) |
Melting Point | 155° |
Boling Point | 530.0±50.0 °C(Predicted) |
pKa | 2.56±0.70(Predicted) |
Storage Condition | 2-8°C |
Physical and Chemical Properties | Yellow prismatic crystals are obtained from ethyl acetate-hexane with a melting point of 155 ℃. Acute toxicity LD50 male and female mice, male and female rats (mg/kg):143,193,1982,1459 oral administration. Acute toxicity LD50 male and female mice (mg/kg):7.3,9.1 intraperitoneal injection. |
In vivo study | Aranidipine (MPC-1304) is a new Ca 2+ channel antagonist in spontaneously hypertensive rats. Following oral administration of Aranidipine at doses of 3 and 10 mg/kg to spontaneously hypertensive rats (SHR), there are significant decreases in B max values for specific [ 3 H](+)-PN 200-110 binding to myocardial membranes compared to the control values. The B max values at 1 h (3 mg/kg), 1 and 6 h (10 mg/kg) are significantly decreased (47.7, 48.9 and 25.8%, respectively) compared to the control values. The effect is greatest at 1 h and decreases with time. The B max values at 6 h (3 mg/kg) and 12 or 24 h (10 mg/kg) after the oral administration of Aranidipine are not significantly different from the control values, suggesting the disappearance of the effect of Aranidipine. The K d values for myocardial [ 3 H](+)-PN 200-110 binding are unaltered by oral administration of Aranidipine. |
Toxicity | LD50 in male, female mice, rats (mg/kg): 143, 193, 1982, 1459 orally; LD50 in male, female mice (mg/kg): 7.3, 9.1 i.p. (Nakano) |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.575 ml | 12.874 ml | 25.749 ml |
5 mM | 0.515 ml | 2.575 ml | 5.15 ml |
10 mM | 0.257 ml | 1.287 ml | 2.575 ml |
5 mM | 0.051 ml | 0.257 ml | 0.515 ml |