Aranidipine (MPC1304)
(Synonyms: 阿雷地平,MPC1304) 目录号 : GC34049Aranidipine (MPC1304) (MPC1304) 是一种 Ca2+ 通道拮抗剂,具有强效和持久的抗高血压作用。
Cas No.:86780-90-7
Sample solution is provided at 25 µL, 10mM.
Aranidipine (MPC1304) is a Ca2+ channel antagonist with potent and long-lasting antihypertensive effects.
Aranidipine (MPC-1304) is a new Ca2+ 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 Bmax values for specific [3H](+)-PN 200-110 binding to myocardial membranes compared to the control values. The Bmax 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 Bmax 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 Kd values for myocardial [3H](+)-PN 200-110 binding are unaltered by oral administration of Aranidipine[1].
[1]. Nozawa Y, et al. Receptor occupation and pharmacokinetics of MPC-1304, a new Ca2+ channel antagonist, in spontaneously hypertensive rats. Eur J Pharmacol. 1995 Dec 12;287(2):191-6.
Animal experiment: |
Rats[1]Male SHR (11-15 weeks) are used. They are fasted for 16 h before the administration of drugs, and given Aranidipine (3, 10 mg/kg) orally through a gastric tube. Control animals are given the vehicle. At 1-24 h after drug administration, the SHR are killed by bleeding from the descending aorta under light anesthesia with ethyl ether, and the myocardium and brain are perfused with 0.9% saline from the aorta. Then, both tissues are removed, and blood vessels are trimmed away. Plasma from rat blood is isolated by centrifugation, and stored at -80°C until the concentration of Aranidipine is determined. |
References: [1]. Nozawa Y, et al. Receptor occupation and pharmacokinetics of MPC-1304, a new Ca2+ channel antagonist, in spontaneously hypertensive rats. Eur J Pharmacol. 1995 Dec 12;287(2):191-6. |
Cas No. | 86780-90-7 | SDF | |
别名 | 阿雷地平,MPC1304 | ||
Canonical SMILES | O=C(C1=C(C)NC(C)=C(C(OCC(C)=O)=O)C1C2=CC=CC=C2[N+]([O-])=O)OC | ||
分子式 | C19H20N2O7 | 分子量 | 388.37 |
溶解度 | DMSO : 125 mg/mL (321.86 mM) | 储存条件 | Store at -20°C,unstable in solution, ready to use. |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.5749 mL | 12.8743 mL | 25.7486 mL |
5 mM | 0.515 mL | 2.5749 mL | 5.1497 mL |
10 mM | 0.2575 mL | 1.2874 mL | 2.5749 mL |
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