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胞磷胆碱

胞磷胆碱用途

Citicoline 是一种合成细胞膜组分磷脂酰胆碱的中间体。发挥神经保护作用。

胞磷胆碱名称

[ CAS 号 ]:
987-78-0

[ 中文名 ]:
胞二磷胆碱

[ 英文名 ]:
Citicoline

[中文别名 ]:

[英文别名 ]:

cytidinediphosphocholine
recofnan
CDP-choline
Citicoline
colite
nicolin
MFCD00868097
nicholin
cereb
Reagin

胞磷胆碱生物活性

[ 描述 ]:

Citicoline 是一种合成细胞膜组分磷脂酰胆碱的中间体。发挥神经保护作用。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 神经疾病

[体外研究]

为了确定胞二磷胆碱和Homotaurine的潜在神经保护活性,用增加浓度的胞二磷胆碱或Homotaurine处理处理的视网膜细胞24小时。使用1μM,10μM和100μM的胞二磷胆碱或Homotaurine来研究是否可能导致视网膜细胞中细胞活力降低。在胞二磷胆碱或Homotaurine处理的培养物中,视网膜细胞保存完好,没有毒性证据或治疗后存活率显着降低。 100μM胞二磷胆碱在体外对视网膜神经胶质细胞无害,100μM的Homotaurine是增强实验性青光眼模型中神经保护作用的有效浓度。因此,该浓度的胞二磷胆碱和Homotaurine用于所有后续实验。为了评估与胞二磷胆碱和Homotaurine的共处理是否能够诱导针对谷氨酸兴奋毒性的协同神经保护作用,在谷氨酸处理前24小时,将视网膜细胞培养物暴露于100μM胞磷胆碱,100μMHomotaurine和100μM胞磷胆碱+ Homotaurine。在100μM胞二磷胆碱的存在下,观察到细胞活力的显着增加[1]。

[体内研究]

以1000mg/kg的剂量施用胞磷胆碱产生更明显的阵挛性发作阈值和具有致死结果的癫痫发作的强直期(与对照相比分别为18.54和50.08％)。以1000mg/kg的剂量注射胞二磷胆碱后,抗惊厥作用最明显[2]。

[细胞实验]

用于评估视网膜细胞中细胞活力的测定法是MTT还原测定法。为了评估胞二磷胆碱和Homotaurine对细胞存活的影响，将细胞细分为三组，并用1μM，10μM和100μM的胞二磷胆碱和1μM，10μM和100μM的Homotaurine处理24小时。为了评价胞二磷胆碱和Homotaurine的神经保护作用，在谷氨酸处理前24小时和高糖（HG）处理前30分钟，用100μM胞磷胆碱，100μMHomotaurine或100μM胞二磷胆碱+ Homotaurine处理细胞。将MTT以0.5mg / mL的终浓度加入孔中，在37℃下保持1小时。此后，除去培养基，通过向每个孔中加入100μLDMSO使还原的MTT（蓝色甲product产物）溶解。在搅拌板15分钟后，使用具有570nm测试波长和690nm参考波长的自动酶标仪测量每个孔中溶解的甲product产物的光密度[1]。

[动物实验]

小鼠[1]在体重23-27g的雄性C57Bl / 6小鼠（n = 69）上进行实验。该研究分两个系列进行。在系列I中，评估了胞二磷胆碱对小鼠癫痫发作阈值的剂量依赖性作用。在给予胞二磷胆碱后1小时进行测量。腹膜内注射剂量为500和1000mg / kg（每20g体重0.04mL）的胞二磷胆碱。对照动物在相似条件下接受等体积的生理盐水。在系列II中，在单次腹膜内注射胞二磷胆碱后3和6小时估计胞二磷胆碱效应的持续时间。

[参考文献]

[1]. Davinelli S, et al. Cytoprotective Effects of Citicoline and Homotaurine against Glutamate and High Glucose Neurotoxicity in Primary Cultured Retinal Cells. Oxid Med Cell Longev. 2017;2017:2825703.

[2]. Karpova MN, et al. Increase of the seizure threshold in C57BL/6 mice after citicoline administration. Bull Exp Biol Med. 2015 Jan;158(3):315-7.

[相关活性小分子]

胞磷胆碱物理化学性质

[ 沸点 ]:
851.4ºC at 760 mmHg

[ 分子式 ]:
C₁₄H₂₆N₄O₁₁P₂

[ 分子量 ]:
488.324

[ 精确质量 ]:
488.107330

[ PSA ]:
235.34000

[ LogP ]:
-7.07

[ 外观性状 ]:
白色结晶粉末

[ 储存条件 ]:
-20℃

胞磷胆碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: GA4027000

CHEMICAL NAME :: Choline, hydroxide, 5'-ester with cytidine 5'-(trihydrogen pyrophosphate), inner salt

CAS REGISTRY NUMBER :: 987-78-0

LAST UPDATED :: 199806

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C14-H26-N4-O11-P2

MOLECULAR WEIGHT :: 488.38

WISWESSER LINE NOTATION :: T6NVNJ DZ A- BT5OTJ CQ DQ E1OPQO&OPWO2K1&1&1 &39/36

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18501 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,109,1980

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5344 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - antipsychotic Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,109,1980

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 8218 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - antipsychotic Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,109,1980

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2973 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - antipsychotic Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,109,1980

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3750 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,531,1995

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 27142 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,109,1980

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 5393 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - antipsychotic Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,109,1980

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 6485 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,109,1980

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4150 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,531,1995

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4472 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - antipsychotic Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,109,1980

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1950 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,322,1982

胞磷胆碱安全信息

[ 危害码 (欧洲) ]:
Xi

[ 海关编码 ]:
2942000000

胞磷胆碱合成路线

详细合成路线

胞磷胆碱上下游产品

胞磷胆碱上游产品

胞磷胆碱下游产品

胞磷胆碱制备

【方法一】
可从肝或酵母提取，也可通过化学合成。合成法以胞嘧啶-5'-二磷酸与乙烯亚胺反应生成胞嘧啶-5'-二磷酸氨基乙酯，然后用碘甲烷甲基化即得。也可将胞嘧啶-5'-磷酸酰胺与磷酸胆碱酯直接缩合而得。

胞磷胆碱海关

[ 海关编码 ]: 2942000000