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伊拉地平

伊拉地平用途

Isradipine(Dynacirc)是钙离子通道阻断剂，IC50为34μM。

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伊拉地平名称

[ CAS 号 ]:
75695-93-1

[ 中文名 ]:
伊拉地平

[ 英文名 ]:
Isradipine

[中文别名 ]:

[英文别名 ]:

Rebriden
DynaCirc
Esradin
Isrodipine
Presca
Dynacrine
MFCD00153820
Rebfiden
Iomir
Clivoten

伊拉地平生物活性

[ 描述 ]:

Isradipine(Dynacirc)是钙离子通道阻断剂,IC50为34μM。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

研究领域 >> 心血管疾病

[参考文献]

[1]. Berjukow, S. and S. Hering, Voltage-dependent acceleration of Ca(v)1.2 channel current decay by (+)- and (-)-isradipine. Br J Pharmacol, 2001. 133(7): p. 959-66.

[2]. Tran, P.H., 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. 450(1-2): p. 79-86.

[相关活性小分子]

伊拉地平物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
501.9±60.0 °C at 760 mmHg

[ 熔点 ]:
166-168°C

[ 分子式 ]:
C₁₉H₂₁N₃O₅

[ 分子量 ]:
371.387

[ 闪点 ]:
257.4±32.9 °C

[ 精确质量 ]:
371.148132

[ PSA ]:
103.55000

[ LogP ]:
3.59

[ 外观性状 ]:
黄色固体

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.566

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMSO: ~26 mg/mL

伊拉地平MSDS

详细MSDS(安全技术说明书)

伊拉地平安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

伊拉地平合成路线

详细合成路线

伊拉地平制备

苯并呋咱-4-甲醛和3-氨基丁烯酸甲酯及乙酰乙酸异丙酯缩合，即得伊拉地平。

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伊拉地平文献

Cav1.3 channels control D2-autoreceptor responses via NCS-1 in substantia nigra dopamine neurons.

Brain 137(Pt 8) , 2287-302, (2014)

Dopamine midbrain neurons within the substantia nigra are particularly prone to degeneration in Parkinson's disease. Their selective loss causes the major motor symptoms of Parkinson's disease, but th...

Analysis of responses to the TRPV4 agonist GSK1016790A in the pulmonary vascular bed of the intact-chest rat.

Am. J. Physiol. Heart Circ. Physiol. 306(1) , H33-40, (2014)

The transient receptor potential vanilloid 4 (TRPV4) channel is a nonselective cation channel expressed on many cell types, including the vascular endothelium and smooth muscle cells. TRPV4 channels p...

L-type calcium channel blockade alleviates molecular and reversal spatial learning and memory alterations induced by entorhinal amyloid pathology in rats.

Behav. Brain Res. 237 , 190-9, (2013)

The entorhinal cortex (EC) is one of the most vulnerable brain regions that is affected by beta amyloid (Aβ) in the early phases of Alzheimer's disease (AD). Calcium dyshomeostasis is one reason of Aβ...

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