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128-62-1

中文名稱 那可汀
英文名稱 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 2024/12/03 15:40:32
128-62-1 結(jié)構(gòu)式 128-62-1 結(jié)構(gòu)式

基本信息

中文別名
那可汀
納可丁
諾司卡品
那可汀[鹼]
(S,R)-那可汀
(S,R)-諾司卡品
英文別名
Opian
Capval
Lyobex
Vadebe
Ecasil
Terial
Nipaxon
nsc5366
Opianin
Vadebex

物理化學(xué)性質(zhì)

外觀性狀無色結(jié)晶性粉末或有光澤的棱柱狀或片狀結(jié)晶;無臭,無味。幾乎不溶于水,微溶于乙醇與乙醚,溶于氯仿。
熔點174-176 °C(lit.)
比旋光度-200 º (c=1 in chloroform)
沸點532.6°C (rough estimate)
密度1.395
折射率1.5614 (estimate)
儲存條件-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.
酸度系數(shù)(pKa)7.8(at 25℃)
形態(tài)neat
顏色正交棱鏡或粗針
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化學(xué)物質(zhì)信息Narcotine alkaloid(128-62-1)

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H336
防范說明P301+P312+P330
危險品標(biāo)志Xn
危險類別碼22
安全說明24/25
危險品運(yùn)輸編號1544
WGK Germany3
RTECS號RD2625000
危險等級6.1(b)
包裝類別III
海關(guān)編碼29329990
毒害物質(zhì)數(shù)據(jù)128-62-1(Hazardous Substances Data)
毒性cyt-ham:lng 100 mg/L ATSUDG (4),41,80

應(yīng)用領(lǐng)域

用途1
支氣管解痙性鎮(zhèn)咳藥。

常見問題列表

生物活性
Noscapine ((S,R)-Noscapine) 是一種具有口服活性的苯酞異喹啉生物堿,具有強(qiáng)效鎮(zhèn)咳作用。Noscapine 通過激活 sigma 阿片類受體 (sigma opioid receptors) 發(fā)揮鎮(zhèn)咳作用,是一種非競爭性 Bradykinin 抑制劑。Noscapine 破壞微管動力學(xué),誘導(dǎo)細(xì)胞有絲分裂停滯和凋亡 (apoptosis) 以及活性。Noscapine 具有抗癌,神經(jīng)保護(hù),抗炎活性,并且可以穿越血腦屏障。
靶點

Sigma opioid receptors Bradykinin Apoptosis

體外研究

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.
體內(nèi)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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