Citicoline

Modify Date: 2024-01-02 14:28:10

Citicoline structure	Common Name	Citicoline
	CAS Number	987-78-0	Molecular Weight	488.324
	Density	N/A	Boiling Point	851.4ºC at 760 mmHg
	Molecular Formula	C₁₄H₂₆N₄O₁₁P₂	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Citicoline

Citicoline is an intermediate in the synthesis of phosphatidylcholine, a component of cell membranes. Citicoline exerts neuroprotective effects.

Name	CDP-choline
Synonym	More Synonyms

Description	Citicoline is an intermediate in the synthesis of phosphatidylcholine, a component of cell membranes. Citicoline exerts neuroprotective effects.
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Neurological Disease
In Vitro	To determine the potential neuroprotective activity of Citicoline and Homotaurine, treated retinal cells are treated with increasing concentrations of Citicoline or Homotaurine for 24 hours. 1 μM, 10 μM and 100 μM of Citicoline or Homotaurine are used to investigate whether may contribute to a reduced cell viability in retinal cells. Retinal cells are well preserved in Citicoline- or Homotaurine-treated cultures, with no evidence of toxicity or significant loss of viability after treatments. 100 μM of Citicoline is not harmful to retinal neuroglial cells in vitro and 100 μM of Homotaurine is an effective concentration to enhance neuroprotection in a model of experimental glaucoma. Therefore, this concentration of Citicoline and Homotaurine is used for all subsequent experiments. To evaluate whether cotreatment with Citicoline and Homotaurine is able to induce a synergistic neuroprotective effect against glutamate excitotoxicity, retinal cell cultures are exposed to Citicoline 100 μM, Homotaurine 100 μM, and Citicoline+Homotaurine 100 μM, 24 hours before glutamate treatment. In the presence of 100 μM Citicoline, a significant increase in cell viability is observed[1].
In Vivo	Administration of Citicoline in a dose of 1000 mg/kg produces more pronounced increase in the threshold of clonic seizures and tonic phase of seizures with lethal outcome (by 18.54 and 50.08% respectively, in comparison with the control). The anticonvulsant effect is most pronounced after injection of Citicoline in a dose of 1000 mg/kg[2].
Cell Assay	The assay used to assess cell viability in retinal cells was the MTT reduction assay. To evaluate the effect of Citicoline and Homotaurine on cell survival, the cells are subdivided into three groups and treated for 24 hours with 1 μM, 10 μM, and 100 μM of Citicoline and with 1 μM, 10 μM and 100 μM of Homotaurine. To evaluate the neuroprotective effects of Citicoline and Homotaurine, cells are treated with Citicoline 100 μM, Homotaurine 100 μM, or Citicoline+Homotaurine 100 μM, 24 hours before glutamate treatment and 30 min before high glucose (HG) treatment. MTT is added to wells at a final concentration of 0.5 mg/mL for 1 hour at 37°C. After this time, the medium is removed and reduced MTT (blue formazan product) is solubilized by adding 100 μL DMSO to each well. After agitation of plates for 15 min, the optical density of the solubilized formazan product in each well is measured using an automatic microplate reader with a 570 nm test wavelength and a 690 nm reference wavelength[1].
Animal Admin	Mice[1] Experiments are performed on male C57Bl/6 mice (n=69) weighing 23-27 g. The study is performed in two series. In series I, the dose-dependent effect of Citicoline on the seizure threshold in mice is evaluated. The measurements are performed 1 h after Citicoline administration. Citicoline in doses of 500 and 1000 mg/kg (0.04 mL per 20 g body weight) is injected intraperitoneally. The control animals receive an equivalent volume of physiological saline under similar conditions. In series II, the duration of Citicoline effect is estimated in 3 and 6 h after single intraperitoneal injection of Citicoline.
References	[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.

Boiling Point	851.4ºC at 760 mmHg
Molecular Formula	C₁₄H₂₆N₄O₁₁P₂
Molecular Weight	488.324
Exact Mass	488.107330
PSA	235.34000
LogP	-7.07
Storage condition	-20℃

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

Hazard Codes	Xi
HS Code	2942000000

dextrose

CAS#:492-62-6

Choline chloride

CAS#:67-48-1

Orotic acid

CAS#:65-86-1

Citicoline

CAS#:987-78-0

Literature: EP1939210 A1, ; Page/Page column 15-18 ;

Precursor 3
CAS#:492-62-6 dextrose CAS#:67-48-1 Choline chloride CAS#:65-86-1 Orotic acid
DownStream 0

HS Code	2942000000

cytidinediphosphocholine

recofnan

CDP-choline

Citicoline

colite

nicolin

MFCD00868097

nicholin

cereb

5'-O-[Hydroxy({[2-(trimethylammonio)ethoxy]phosphinato}oxy)phosphoryl]cytidine

Reagin

Audes

Cytidine, 5'-O-[hydroxy[[hydroxy[2-(trimethylammonio)ethoxy]phosphinyl]oxy]phosphinyl]-, inner salt

cytidine diphosphate choline

EINECS 213-580-7

Rexort

CYTIDINE 5'-DIPHOSPHOCHOLINE

ensign

cytidine-5'-diphosphocholine

Citifar

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Citicoline
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Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: Citicoline
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Purity: 98.0%
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Henan Tianfu Chemical Co., Ltd.
China
Product Name: cdp choline
Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
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Taiwan Oyi peptide Co. Ltd
China
Product Name: Citicoline
Price: $Inquiry/1mg $Inquiry/100kg
Purity: 98.0%
Delivery: 1 Day
Contact: Vinnie
Email: Jamie@api-made.com

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Citicoline

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