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128-62-1

中文名称 那可汀
英文名称 Narcotine
CAS 128-62-1
分子式 C22H23NO7
分子量 413.42
MOL 文件 128-62-1.mol
更新日期 2023/11/23 17:54:46
128-62-1 结构式 128-62-1 结构式

基本信息

中文别名
那可汀
纳可丁
诺司卡品
那可汀[鹼]
(S,R)-那可汀
(S,R)-诺司卡品
英文别名
Opian
Capval
Lyobex
Vadebe
Ecasil
Terial
Nipaxon
nsc5366
Opianin
Vadebex

物理化学性质

外观性状无色结晶性粉末或有光泽的棱柱状或片状结晶;无臭,无味。几乎不溶于水,微溶于乙醇与乙醚,溶于氯仿。
熔点174-176 °C(lit.)
比旋光度-200 º (c=1 in chloroform)
沸点532.6°C (rough estimate)
密度1.395
折射率1.5614 (estimate)
储存条件-20°C Freezer, Under Inert Atmosphere
溶解度Practically insoluble in water, soluble in acetone, slightly soluble in ethanol (96 per cent). It dissolves in strong acids; on dilution of the solution with water, the base may be precipitated.
酸度系数(pKa)7.8(at 25℃)
形态neat
颜色正交棱镜或粗针
旋光性 (optical activity)[α]20/D 200°, c = 1 in chloroform
水溶解性302.9mg/L(25 ºC)
Merck13,6752
NIST化学物质信息Narcotine alkaloid(128-62-1)

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302-H336
防范说明P301+P312+P330
危险品标志Xn
危险类别码22
安全说明24/25
危险品运输编号1544
WGK Germany3
RTECS号RD2625000
危险等级6.1(b)
包装类别III
海关编码29329990
毒性cyt-ham:lng 100 mg/L ATSUDG (4),41,80

应用领域

用途1
支气管解痉性镇咳药。

常见问题列表

生物活性
Noscapine ((S,R)-Noscapine) 是一种具有口服活性的苯酞异喹啉生物碱,具有强效镇咳作用。Noscapine 通过激活 sigma 阿片类受体 (sigma opioid receptors) 发挥镇咳作用,是一种非竞争性 Bradykinin 抑制剂。Noscapine 破坏微管动力学,诱导细胞有丝分裂停滞和凋亡 (apoptosis) 以及活性。Noscapine 具有抗癌,神经保护,抗炎活性,并且可以穿越血脑屏障。
靶点

Sigma opioid receptors Bradykinin Apoptosis

体外研究

Noscapine (0-1000 μM; 0-96 hours; rat C6 glioma cells) treatment inhibits cell viability of rat C6 glioma in vitro in a dose- and time-dependent manner. Noscapine inhibits the viability of rat C6 glioma cells with an IC 50 of 250 μM at 72 hours.
Noscapine exposure causes abnormal S-phase reentry, increases mitotic arrest and results in excessive DNA accumulation.
Cylindromatosis increases the ability of noscapine to induce mitotic arrest and apoptosis. Cylindromatosis enhances the effect of noscapine on microtubule polymerization and promotes noscapine binding to microtubules.

Cell Viability Assay

Cell Line: Rat C6 glioma cells
Concentration: 0 μM, 0.1 μM, 1 μM, 2 μM, 10 μM, 50 μM, 100 μM, 1000 μM
Incubation Time: 0 hours, 12 hours, 24 hours, 48 hours, 72 hours, 96 hours
Result: Inhibited cell viability of rat C6 glioma in vitro in a dose- and time-dependent manner.
体内研究

Noscapine (300 mg/kg; oral gavage; daily; for 15 days; athymic female mice) treatment reduces tumor growth in mice.

Animal Model: Athymic female mice (nu/nu) (8-week-old) injected with rat C6 glioma cells
Dosage: 300 mg/kg
Administration: Oral gavage; daily; for 15 days
Result: Revealed a significant reduction of tumor volume.
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