Isradipine

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Chemical Structure| 75695-93-1 同义名 : 伊拉地平 ;PN 200-110
CAS号 : 75695-93-1
货号 : A782133
分子式 : C19H21N3O5
纯度 : 98%
分子量 : 371.387
MDL号 : MFCD00153820
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

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

DMSO: 105 mg/mL(282.72 mM)，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 sradipine is a calcium antagonist with marked vascular selectivity and, in practical terms, is devoid of cardiac effects. Both when used as single drug treatment and in combination with other agents, particularly beta-blockers, isradipine is well tolerated, does not cause metabolic disturbances and, apart from the typical dihydropyridine-type vascular adverse effects, e.g. flushing and ankle oedema, it does not cause any specific side effect[3]. The confirmation of its antihypertensive efficacy, along with its favourable haemodynamic profile and reversal of left ventricular hypertrophy, minimal effect on glucose and lipid metabolism, preservation of quality of life and good tolerability, makes isradipine a suitable drug for the treatment of most patients with mild to moderate hypertension[4]. Isradipine-induced acceleration of the Ca(v)1.2 current decay reflects enhanced fast voltage-dependent inactivation and not open channel block[2]. Isradipine in vitro attenuates beta amyloid oligomer toxicity by suppressing calcium influx into cytoplasm and by suppressing Ca(v)1.2 expression. Isradipine became bioavailable, lowered tau burden, and improved autophagy function in the brain[5]. Chronic isradipine treatment remodeled SNc DA neurons in a way that should not only diminish their vulnerability to mitochondrial challenges, but to autophagic stress as well[6].
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
NCT03538262 - Enrolling by invitation January 31, 2023 United States, New York ... 展开 >> CHeT Telemedicine (Site 363) Rochester, New York, United States, 14642 收起 <<
NCT00684489 Hypertension Not Applicable Completed - -
NCT01587742 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.46mL

2.69mL

1.35mL

26.93mL

5.39mL

2.69mL
参考文献

[1]Tran PH, Tran TT, et al. Physical properties and in vivo bioavailability in human volunteers of isradipine using controlled release matrix tablet containing self-emulsifying solid dispersion. Int J Pharm. 2013 Jun 25;450(1-2):79-86.

[2]Berjukow S, Hering S. Voltage-dependent acceleration of Ca(v)1.2 channel current decay by (+)- and (-)-isradipine. Br J Pharmacol. 2001; 133(7):959‐966

[3]Hansson L. Isradipine in hypertension. Drugs. 1990; 40 Suppl 2:10‐14

[4]Brogden RN, Sorkin EM. Isradipine. An update of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in the treatment of mild to moderate hypertension. Drugs. 1995; 49(4):618‐649

[5]Anekonda TS, Quinn JF. Calcium channel blocking as a therapeutic strategy for Alzheimer's disease: the case for isradipine. Biochim Biophys Acta. 2011; 1812(12):1584‐1590

[6]Guzman JN, Ilijic E, Yang B, et al. Systemic isradipine treatment diminishes calcium-dependent mitochondrial oxidant stress. J Clin Invest. 2018; 128(6):2266‐2280