CAS 987-78-0|Citicoline
Introduction：Basic information about CAS 987-78-0|Citicoline, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Citicoline | ||
|---|---|---|---|
| CAS Number | 987-78-0 | Molecular Weight | 488.324 |
| Density | / | Boiling Point | 851.4ºC at 760 mmHg |
| Molecular Formula | C14H26N4O11P2 | Melting Point | / |
| MSDS | / | Flash Point | / |
Names
| Name | CDP-choline |
|---|---|
| Synonym | More Synonyms |
Citicoline BiologicalActivity
| Description | Citicoline is an intermediate in the synthesis of phosphatidylcholine, a component of cell membranes. Citicoline exerts neuroprotective effects. |
|---|---|
| Related Catalog | Signaling Pathways >>Others >>OthersResearch 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. |
Chemical & Physical Properties
| Boiling Point | 851.4ºC at 760 mmHg |
|---|---|
| Molecular Formula | C14H26N4O11P2 |
| Molecular Weight | 488.324 |
| Exact Mass | 488.107330 |
| PSA | 235.34000 |
| LogP | -7.07 |
| InChIKey | RZZPDXZPRHQOCG-OJAKKHQRSA-N |
| SMILES | C[N+](C)(C)CCOP(=O)([O-])OP(=O)([O-])OCC1OC(n2ccc(N)nc2=O)C(O)C1O.[H+] |
| Storage condition | -20℃ |
Toxicological Information
CHEMICAL IDENTIFICATION |
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
Safety Information
| Hazard Codes | Xi |
|---|---|
| HS Code | 2942000000 |
Customs
| HS Code | 2942000000 |
|---|
Synonyms
| 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 |
