Amlodipine

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Chemical Structure| 88150-42-9 同义名 : Intervask;UK-48340;Pelmec
CAS号 : 88150-42-9
货号 : A367713
分子式 : C20H25ClN2O5
纯度 : 99%
分子量 : 408.88
MDL号 : MFCD00864687
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(73.37 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Calcium Channel
描述 Amlodipine, a third-generation dihydropyridine calcium antagonist, has a mode of action and pharmacodynamic profile which are comparable to those of conventional compounds in this series, such as nifedipine[3]. Among combinations of hypertension medications, a β-blocker such as bisoprolol with a calcium channel blocker such as amlodipine is an effective combination therapy for hypertension, with distinct and complimentary modes of action[4]. Black triangle In the comparison with amlodipine monotherapy, >70% of olmesartan medoxomil/amlodipine recipients, some requiring upwards dosage adjustment, met BP goals. Peripheral oedema was significantly less common in olmesartan medoxomil/amlodipine 40 mg/10 mg per day than amlodipine monotherapy 10 mg/day recipients[5]. Maximal amlodipine concentrations in mothers ranged from 4.4 to 14.7 ng/mL in plasma, and 6.5 to 19.7 ng/mL in milk (Average milk/plasma ratio: 1.4). RID was 3.4% of the maternal weight-adjusted dose. All plasma concentrations in infants were under the quantitation limit (0.4 ng/mL). Infant exposure to amlodipine in breast milk appears very small, suggesting that amlodipine can be used with little influence on infants during breastfeeding[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.24mL

12.23mL

2.45mL

1.22mL

24.46mL

4.89mL

2.45mL
参考文献

[1]Mason RP, Walter MF, et al. Membrane antioxidant effects of the charged dihydropyridine calcium antagonist amlodipine. J Mol Cell Cardiol. 1999 Jan;31(1):275-81.

[2]Zhang X, Hintze TH. Amlodipine releases nitric oxide from canine coronary microvessels: an unexpected mechanism of action of a calcium channel-blocking agent. Circulation. 1998 Feb 17;97(6):576-80.

[3]van Zwieten PA. Amlodipine: an overview of its pharmacodynamic and pharmacokinetic properties. Clin Cardiol. 1994;17(9 Suppl 3):III3‐III6

[4]Gottwald-Hostalek U, Sun N, Barho C, Hildemann S. Management of Hypertension With a Fixed-Dose (Single-Pill) Combination of Bisoprolol and Amlodipine. Clin Pharmacol Drug Dev. 2017;6(1):9‐18

[5]Sanford M, Keam SJ. Olmesartan medoxomil/amlodipine. Drugs. 2009;69(6):717‐729

[6]Aoki H, Ito N, Kaniwa N, et al. Low Levels of Amlodipine in Breast Milk and Plasma. Breastfeed Med. 2018;13(9):622‐626