Neuroscience Research Compound · For laboratory research use only
Also known as CDP-Choline
Citicoline (cytidine 5'-diphosphocholine, CDP-choline) is an endogenous intermediate in the biosynthesis of phosphatidylcholine, a major membrane phospholipid1,2. In the body it is understood to be rapidly hydrolysed and dephosphorylated to cytidine and choline, which enter the brain separately and are used to resynthesise CDP-choline inside brain cells2.
Preclinical studies have examined citicoline in models of cerebral ischaemia, retinal ganglion cell injury and aminoglycoside damage to auditory hair cells1,3,4,5. A 2014 review concluded that there was at that time no adequate description of the mechanism or mechanisms behind its pharmacological actions2.
As described in the research literature
As described in the research literature, studies in transient cerebral ischaemia models led one group to propose that citicoline acts mainly by attenuating phospholipase A2 activation. Observations summarised in their review include preservation of cardiolipin and sphingomyelin, preservation of the arachidonic acid content of phosphatidylcholine and phosphatidylethanolamine, partial restoration of phosphatidylcholine, stimulation of glutathione synthesis and glutathione reductase activity, attenuation of lipid peroxidation and restoration of Na+/K+-ATPase activity1. The same review notes that citicoline also supplies choline for acetylcholine synthesis1.
A later critical review discussed its pharmacokinetics and biotransformation and proposed testing whether the intact molecule, or the phosphorylated intermediates of its hydrolysis (cytidine monophosphate and phosphocholine), are themselves pharmacologically active2.
What published studies have examined
Models of transient cerebral ischaemia have been used to examine membrane phospholipid metabolism, phospholipase A2 activation, lipid peroxidation and glutathione after citicoline1. A 2014 review discusses this preclinical evidence alongside open questions on biotransformation and mode of action2.
Mouse retinal explant cultures were used to quantify TUNEL-positive retinal ganglion cells and regenerating neurites3. In a rat partial optic nerve crush model, retinal ganglion cell density was measured by retrograde Fluorogold labelling and Bcl-2 immunoreactivity was examined, with citicoline alone and combined with lithium4.
HEI-OC1 hair cell-like cells and whole cochlear explants from mice were used to examine neomycin-induced hair cell loss, reactive oxygen species accumulation, mitochondrial dysfunction and apoptosis with and without citicoline co-treatment5.
Sources [5]
Citicoline: neuroprotective mechanisms in cerebral ischemia.
Adibhatla RM, Hatcher JF, Dempsey RJ Journal of Neurochemistry, 2002.
Neuroprotective properties of citicoline: facts, doubts and unresolved issues.
Grieb P CNS Drugs, 2014.
Citicoline has a protective effect on damaged retinal ganglion cells in mouse culture retina.
Oshitari T, Fujimoto N, Adachi-Usami E Neuroreport, 2002.
Citicoline and lithium rescue retinal ganglion cells following partial optic nerve crush in the rat.
Schuettauf F, Rejdak R, Thaler S, et al. Experimental Eye Research, 2006.
Citicoline Protects Auditory Hair Cells Against Neomycin-Induced Damage.
Zhong Z, Fu X, Li H, et al. Frontiers in Cell and Developmental Biology, 2020.
This page is provided for research and educational reference only. It does not constitute medical advice, dosing guidance, or a recommendation for use. All compounds are strictly for laboratory and in-vitro research purposes.