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Nifedipine

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Chemical Structure| 21829-25-4 同义名 : BAY-a-1040;BAY 1040
CAS号 : 21829-25-4
货号 : A134096
分子式 : C17H18N2O6
纯度 : 98%
分子量 : 346.335
MDL号 : MFCD00057326
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(303.18 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 L-type calcium (Ca2+) channel mediates influx of calcium ions into the cytoplasm, and thereby triggers calcium release from the sarcoplasm. Calcium channel also plays an important role in excitation-contraction coupling in the heart and is required for normal heart development and normal regulation of heart rhythm. Nifedipine is a L-type calcium channel antagonist. In a [3H]-thymidine incorporation assay for rat vascular smooth muscle cells growth evaluation, treatment of nifedipine dose-dependently decreased the values of [3H]-thymidine incorporation to 63.82 ± 4.31%, 22.68 ± 1.22% and 5.45 ± 3.26% of those of the control, respectively, at the concentrations of 1 μM, 10 μM and 100 μM[3]. In an electrophysiology assay reported, the sustained inward current activated by 10 mM caffeine at -80 mV was completely inhibited by 1 μM nifedipine. In the absence of caffeine, nifedipine had no effect on the resting current[4]. In a balloon catheterization experiment in rats, nifedipine was administrated at a low dose of 0.3 mg/kg daily or at a high dose of 3 mg/kg daily. Treatment with nifedipine resulted in a distinct change in the size of intimal thickening in a dose-dependent fashion compared to that of the control[3]. According to another report, nifedipine also has anti-ulcer effects. In a HCI plus ethanol induced gastric mucosal injury model in rats, a single oral dose of nifedipine at the doses of 20 mg/kg or 40 mg/kg prevented the gastric mucosal injury[5]. In an acetic acid induced gastric ulcer model, nifedipine was given twice daily orally at the doses of 10 mg/kg, 20 mg/kg or 40 mg/kg for 14 consecutive days. The treatments of nifedipine dose dependently promoted the ulcer healing[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00000102 Congenital Adrenal Hyperplasia Phase 1 Phase 2 Completed - United States, South Carolina ... 展开 >> Medical University of South Carolina Charleston, South Carolina, United States 收起 <<
NCT01010048 Urinary Calculus Phase 4 Unknown December 2010 China, Chongqing ... 展开 >> The First Affiliated Hospital, ChongQing medical University Recruiting ChongQing, Chongqing, China, 400016 Contact: Yunfeng He, Doctor    86-23-89011121       Contact: Xiaohou Wu, Doctor    86-23-89011122 收起 <<
NCT00280462 Ocular Physiology ... 展开 >> Regional Blood Flow 收起 << Not Applicable Completed - Austria ... 展开 >> Department of Clinical Pharmacology Vienna, Austria, 1090 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.89mL

0.58mL

0.29mL

14.44mL

2.89mL

1.44mL

28.87mL

5.77mL

2.89mL
参考文献

[1]Ding Y, Vaziri ND. Nifedipine and diltiazem but not verapamil up-regulate endothelial nitric-oxide synthase expression. J Pharmacol Exp Ther. 2000 Feb;292(2):606-9.

[2]Zhang X, Anderson JW, et al. Characterization of nifedipine block of the human heart delayed rectifier, hKv1.5. J Pharmacol Exp Ther. 1997 Jun;281(3):1247-56.

[3]Hirata A, Igarashi M, Yamaguchi H, Suwabe A, Daimon M, Kato T, Tominaga M. Nifedipine suppresses neointimal thickening by its inhibitory effect on vascular smooth muscle cell growth via a MEK-ERK pathway coupling with Pyk2. Br J Pharmacol. 2000 Dec;131(8):1521-30. doi: 10.1038/sj.bjp.0703730. PMID: 11139427; PMCID: PMC1572490.

[4]Curtis TM, Scholfield CN. Nifedipine blocks Ca2+ store refilling through a pathway not involving L-type Ca2+ channels in rabbit arteriolar smooth muscle. J Physiol. 2001 May 1;532(Pt 3):609-23. doi: 10.1111/j.1469-7793.2001.0609e.x. PMID: 11313433; PMCID: PMC2278590.

[5]Suzuki Y, Ishihara M, Segami T, Ito M. Anti-ulcer effects of antioxidants, quercetin, alpha-tocopherol, nifedipine and tetracycline in rats. Jpn J Pharmacol. 1998 Dec;78(4):435-41. doi: 10.1254/jjp.78.435. PMID: 9920200.