Citicoline
(Synonyms: 胞磷胆碱; Cytidine diphosphate-choline; CDP-Choline; Cytidine 5'-diphosphocholine) 目录号 : GC35703
An intermediate in the synthesis of phosphatidylcholine
Cas No.:987-78-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Cell experiment: |
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 0.5mg/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]. |
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Animal experiment: |
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. |
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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. |
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Citicoline is an endogenous intermediate in the synthesis of phosphatidylcholine, the major phospholipid in eukaryotic cells.1 It also serves as a choline donor in the biosynthesis of the neurotransmitter acetylcholine. Citicholine demonstrates protective effects in cerebral ischemia, traumatic brain injury, and memory disorders.2 Exogenous administration of citicholine to rodents (500 mg/kg i.p. immediately after ischemia and at 3-
1.McMaster, C.R., and Bell, R.M.Phosphatidylcholine biosynthesis via the CDP-choline pathway in Saccharomyces cerevisiaeJ. Biol. Chem.269(20)14776-14783(1994) 2.Dávalos, A., and Secades, J.Citicoline preclinical and clinical update 2009-2010Stroke42(1)36-39(2011) 3.Rao, M., Hatcher, J.F., and Dempsey, R.J.Lipid alterations in transient forebrain ischemia: Possible new mechanisms of CDP-choline neuroprotectionJ. Neurochem.75(6)2528-2535(2000)
| Cas No. | 987-78-0 | SDF | |
| 别名 | 胞磷胆碱; Cytidine diphosphate-choline; CDP-Choline; Cytidine 5'-diphosphocholine | ||
| Canonical SMILES | O[C@@H]([C@H]([C@H](N1C(N=C(C=C1)N)=O)O2)O)[C@H]2COP(OCC[N+](C)(C)C)(OP([O-])(O)=O)=O | ||
| 分子式 | C14H26N4O11P2 | 分子量 | 488.32 |
| 溶解度 | Water : 300 mg/mL (586.73 mM); DMSO: < 1 mg/mL (insoluble or slightly soluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0478 mL | 10.2392 mL | 20.4784 mL |
| 5 mM | 0.4096 mL | 2.0478 mL | 4.0957 mL |
| 10 mM | 0.2048 mL | 1.0239 mL | 2.0478 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Application of Citicoline in Neurological Disorders: A Systematic Review
Nutrients 2020 Oct 12;12(10):3113.PMID:33053828DOI:10.3390/nu12103113.
Citicoline is a chemical compound involved in the synthesis of cell membranes. It also has other, not yet explained functions. Research on the use of Citicoline is conducted in neurology, ophthalmology, and psychiatry. Citicoline is widely available as a dietary supplement. It is often used to enhance cognitive functions. In our article, accessible databases were searched for articles regarding Citicoline use in neurological diseases. This article has a systemic review form. After rejecting non-eligible reports, 47 remaining articles were reviewed. The review found that Citicoline has been proven to be a useful compound in preventing dementia progression. It also enhances cognitive functions among healthy individuals and improves prognosis after stroke. In an animal model of nerve damage and neuropathy, Citicoline stimulated regeneration and lessened pain. Among patients who underwent brain trauma, Citicoline has an unclear clinical effect. Citicoline has a wide range of effects and could be an essential substance in the treatment of many neurological diseases. Its positive impact on learning and cognitive functions among the healthy population is also worth noting.
Citicoline: pharmacological and clinical review, 2022 update
Rev Neurol 2022 Nov 30;75(s05):S1-S89.PMID:36544369DOI:10.33588/rn.75s05.2022311.
This review is based on the previous one published in 2016 (Secades JJ. Citicoline: pharmacological and clinical review, 2016 update. Rev Neurol 2016; 63 (Supl 3): S1-S73), incorporating 176 new references, having all the information available in the same document to facilitate the access to the information in one document. This review is focused on the main indications of the drug, as acute stroke and its sequelae, including the cognitive impairment, and traumatic brain injury and its sequelae. There are retrieved the most important experimental and clinical data in both indications.
Citicoline for treating people with acute ischemic stroke
Cochrane Database Syst Rev 2020 Aug 29;8(8):CD013066.PMID:32860632DOI:10.1002/14651858.CD013066.pub2.
Background: Stroke is one of the leading causes of long-lasting disability and mortality and its global burden has increased in the past two decades. Several therapies have been proposed for the recovery from, and treatment of, ischemic stroke. One of them is Citicoline. This review assessed the benefits and harms of Citicoline for treating patients with acute ischemic stroke. Objectives: To assess the clinical benefits and harms of Citicoline compared with placebo or any other control for treating people with acute ischemic stroke. Search methods: We searched in the Cochrane Stroke Group Trials Register, CENTRAL, MEDLINE Ovid, Embase Ovid, LILACS until 29 January 2020. We searched the World Health Organization Clinical Trials Search Portal and ClinicalTrials.gov. Additionally, we also reviewed reference lists of the retrieved publications and review articles, and searched the websites of the US Food and Drug Administration (FDA) and European Medicines Agency (EMA). Selection criteria: We included randomized controlled trials (RCTs) in any setting including participants with acute ischemic stroke. Trials were eligible for inclusion if they compared Citicoline versus placebo or no intervention. Data collection and analysis: We selected RCTs, assessed the risk of bias in seven domains, and extracted data by duplicate. Our primary outcomes of interest were all-cause mortality and the degree of disability or dependence in daily activities at 90 days. We estimated risk ratios (RRs) for dichotomous outcomes. We measured statistical heterogeneity using the I² statistic. We conducted our analyses using the fixed-effect and random-effects model meta-analyses. We assessed the overall quality of evidence for six pre-specified outcomes using the GRADE approach. Main results: We identified 10 RCTs including 4281 participants. In all these trials, Citicoline was given either orally, intravenously, or a combination of both compared with placebo or standard care therapy. Citicoline doses ranged between 500 mg and 2000 mg per day. We assessed all the included trials as having high risk of bias. Drug companies sponsored six trials. A pooled analysis of eight trials indicates there may be little or no difference in all-cause mortality comparing Citicoline with placebo (17.3% versus 18.5%; RR 0.94, 95% CI 0.83 to 1.07; I² = 0%; low-quality evidence due to risk of bias). Four trials found no difference in the proportion of patients with disability or dependence in daily activities according to the Rankin scale comparing Citicoline with placebo (21.72% versus 19.23%; RR 1.11, 95% CI 0.97 to 1.26; I² = 1%; low-quality evidence due to risk of bias). Meta-analysis of three trials indicates there may be little or no difference in serious cardiovascular adverse events comparing Citicoline with placebo (8.83% versus 7.77%; RR 1.04, 95% CI 0.84 to 1.29; I² = 0%; low-quality evidence due to risk of bias). Overall, either serious or non-serious adverse events - central nervous system, gastrointestinal, musculoskeletal, etc. - were poorly reported and harms may have been underestimated. Four trials assessing functional recovery with the Barthel Index at a cut-off point of 95 points or more did not find differences comparing Citicoline with placebo (32.78% versus 30.70%; RR 1.03, 95% CI 0.94 to 1.13; I² = 24%; low-quality evidence due to risk of bias). There were no differences in neurological function (National Institutes of Health Stroke Scale at a cut-off point of ≤ 1 points) comparing Citicoline with placebo according to five trials (24.31% versus 22.44%; RR 1.08, 95% CI 0.96 to 1.21; I² = 27%, low-quality evidence due to risk of bias). A pre-planned Trial Sequential Analysis suggested that no more trials may be needed for the primary outcomes but no trial provided information on quality of life. Authors' conclusions: This review assessed the clinical benefits and harms of Citicoline compared with placebo or any other standard treatment for people with acute ischemic stroke. The findings of the review suggest there may be little to no difference between Citicoline and its controls regarding all-cause mortality, disability or dependence in daily activities, severe adverse events, functional recovery and the assessment of the neurological function, based on low-certainty evidence. None of the included trials assessed quality of life and the safety profile of Citicoline remains unknown. The available evidence is of low quality due to either limitations in the design or execution of the trials.
Citicoline in acute ischemic stroke: A randomized controlled trial
PLoS One 2022 May 31;17(5):e0269224.PMID:35639720DOI:10.1371/journal.pone.0269224.
Introduction: Two pharmacological possibilities exist for an acute ischemic stroke (AIS): recanalization of the occluded artery and neuroprotection from ischaemic injury, the latter's efficacy being debatable. We sought to determine whether administration of Citicoline immediately after recanalization therapy for AIS would improve clinical and radiological outcome at three months compared to standard treatment alone. Patients and methods: CAISR was a single centre, randomized, placebo-controlled, parallel-group trial with blinded endpoint assessment. It was approved by the All India Institute of Medical Sciences Institutional ethics committee and registered at the Clinical Trial Registry of India (CTRI/2018/011900). We recruited participants with AIS undergoing recanalization therapy and randomly assigned them to receive either Citicoline or placebo in 1:1 ratio. Citicoline arm patients received Citicoline 1gm BD intravenously for three days, followed by oral Citicoline 1gm BD for 39 days. Placebo arm patients received 100ml intravenous normal saline for three days, followed by multivitamin tablet BD for 39 days. All patients received standard of care. Outcome: Blinded assessors did the follow-up assessment at six weeks (MRI Brain-stroke volume) and three months (NIHSS 0-2, mRS 0-2 and Barthel index> = 95). Results: The infarct volume decreased from week 1 to week 6 by 2.6 cm3 on placebo versus 4.2 cm3 on Citicoline (p-0.483). The OR for achieving NIHSS 0-2, mRS 0-2 and Barthel index> = 95 with Citicoline was found to be 0.96(95%CI 0.39-2.40), 0.92(95%CI 0.40-2.05) and 0.87(95%CI 0.22-2.98) respectively. Conclusion: CAISR was the first to evaluate the role of Citicoline, when used immediately after recanalization therapy, when the penumbral tissue is the most susceptible either to be protected from injury or become ischemic. We did not find any significant difference between the Citicoline or placebo arms with respect to either our primary or secondary outcomes.
Citicoline and Memory Function in Healthy Older Adults: A Randomized, Double-Blind, Placebo-Controlled Clinical Trial
J Nutr 2021 Aug 7;151(8):2153-2160.PMID:33978188DOI:10.1093/jn/nxab119.
Background: Supplementation of Citicoline (CDP-choline), a naturally occurring mononucleotide, has shown beneficial effects on memory function and behavior in populations with a wide range of impairments. However, few studies have investigated its effect in healthy older populations. Objective: The objective of this study was to investigate the effects of Citicoline (Cognizin®), on memory in healthy elderly populations with age-associated memory impairment (AAMI). Methods: A total of 100 healthy men and women aged between 50 and 85 y with AAMI participated in this randomized, double-blind, placebo-controlled trial. Participants were randomized to receive placebo (n = 51) or Citicoline (n = 49; 500 mg/d) for 12 wk. Memory function was assessed at baseline and end of the intervention (12 wk) using computerized tests (Cambridge Brain Sciences, Ontario, Canada). Safety measurements included adverse events query, body weight, blood pressure, and hematology and metabolic panel. Intent-to-treat analysis was conducted using ANCOVA for the primary and secondary outcome variables with Bonferroni correction for multiple comparisons. Results: A total of 99 out of 100 participants completed the study in its entirety. After the 12-wk intervention, participants supplemented with Citicoline showed significantly greater improvements in secondary outcomes of episodic memory (assessed by the Paired Associate test), compared with those on placebo (mean: 0.15 vs. 0.06, respectively, P = 0.0025). Composite memory (secondary outcome), calculated using the scores of 4 memory tests, also significantly improved to a greater extent following Citicoline supplementation (mean: 3.78) compared with placebo (mean: 0.72, P = 0.0052). Conclusions: Dietary supplementation of Citicoline for 12 wk improved overall memory performance, especially episodic memory, in healthy older males and females with AAMI. The findings suggest that regular consumption of Citicoline may be safe and potentially beneficial against memory loss due to aging. This trial was registered at clinicaltrials.gov as NCT03369925.