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Cytidine 5′-Diphosphocholine: Definition, Synthesis, Uses, Benefits, Side Effects

Cytidine 5′-diphosphocholine, a precursor for lecithin biosynthesis, has received widespread attention because it is mainly used to treat declining brain function. So, in this article, Natural Micron would like to introduce the compound cytidine 5′-diphosphocholine in detail, including its definition, synthesis, uses, benefits, side effects, etc.

Now, let’s get started!

What is cytidine 5′-diphosphocholine?

Cytidine 5′-diphosphocholine is a nucleoside derivative composed of cytidine, diphosphate, and choline linkages. Compounds that can play a crucial role in cell membrane formation and repair.

Cytidine 5′-diphosphocholine may also be called CDP-choline or citicoline. Appearance: white or off-white powder, odorless and hygroscopic. In terms of solubility, cytidine 5′-diphosphocholine is easily soluble in water but insoluble in ethanol, acetone, and chloroform.

Other physicochemical properties of cytidine 5′-diphosphocholine include:

Melting point: >185°C (dec.)
Specific rotation: D25 +19.0° (c = 0.86 in H2O)
Acidity coefficient (pKa): 4.4 (at 25℃)
Stability: Moisture Sensitive

For more information, you can view this page.

Cytidine 5′-Diphosphocholine (CAS: 987-78-0)

Now, let’s move on to the synthesis of cytidine 5′-diphosphocholine

Cytidine 5′-diphosphocholine Synthesis

There are many methods for synthesizing cytidine 5′-diphosphocholine, which are mainly divided into three pathways:

  1. Microbial fermentation. This method has problems such as low product concentration and unstable yield.
  2. Organic Chemistry Synthesis Methods. This method has problems such as difficulty in separating the product from the condensing agent, not suitable for medicinal use, low reaction conversion rate, many by-products, high cost, and serious environmental pollution.
  3. Enzymatic synthesis. For example, microorganisms such as beer yeast mud are used for biosynthesis. It is enzymatically synthesized using free beer yeast mud cells, which has a simple process, high conversion rate and low cost. The production process of synthesizing sodium citicoline through enzymatic synthesis can be divided into two parts: enzymatic synthesis process and extraction and purification process.

There are two specific options here


The synthesis method involves the reaction of cytosine-5′-diphosphate and ethyleneimine to generate cytosine-5′-diphosphate aminoethyl ester, which is then methylated with iodine. It can also be obtained by direct condensation of cytosine-5′-phosphate amide and phosphocholine ester.


It is synthesized from the raw materials cytidine, choline and diphosphoryl chloride. The cytidine molecule is activated to react with diphosphoryl chloride to form the cytidine diphosphate intermediate. The activated cytidine is then coupled to choline to form a CDP-choline molecule. Finally, the final product is obtained through removal of protecting groups, crystallization, purification, etc.

Cytidine 5′-diphosphocholine Uses

Cytidine 5′-diphosphocholine is also widely used. In addition to targeted treatment of brain functional problems, it also has positive significance for many other diseases. Here are the details:

  • Cytidine 5′-diphosphocholine is used to treat metabolic disorders, disturbances of consciousness, paresis vitiligo, neurological deafness, and tinnitus following acute traumatic brain injury and brain surgery.
  • It is also effective for cerebral thrombosis and hemiplegia, multiple cerebral embolisms, stroke sequelae, insufficient cerebral blood supply caused by cerebral arteriosclerosis, hypnotics and carbon monoxide poisoning, Parkinson’s syndrome and various organic encephalopathy.
  • It can improve the state of consciousness and electroencephalogram of consciousness disorders after head trauma or brain surgery. Promoting the recovery of upper limb motor functions in stroke and hemiplegic patients has a certain effect on promoting brain function recovery and promoting awakening.
  • Promote lecithin biosynthesis and resist phospholipase A. Combined with proteolytic enzyme inhibitors, it can protect and repair brain tissue.
  • Cytidine 5′-diphosphocholine promotes recovery and awakening of brain function. It is also used for disorders of consciousness caused by acute injury to the central nervous system.
  • Cytidine 5′-diphosphocholine is used to treat glaucoma. Because it may help protect optic nerve cells.
  • Crop athlete’s supplement to improve focus, coordination and endurance.

What are cytidine 5′-diphosphocholine benefits?

In addition to its use in treating various types of brain injuries and diseases, cytidine 5′-diphosphocholine has many additional benefits. for example:

  • Strong memory, concentration and overall cognitive function.
  • Enhances neurotransmitter production and promotes nerve membrane repair.
  • Cytidine 5′-diphosphocholine has the effect of changing the physiological function of the meninges. It can also improve cerebral blood vessel tension, increase cerebral blood flow and oxygen consumption, and have a wake-up effect.
  • Cytidine 5′-diphosphocholine can stabilize cell membranes, improve neural plasticity in non-damaged areas, repair nerve cell membranes, and promote functional recovery.
  • Reduce the production of toxic oxygenation metabolites and free radicals.
  • It can increase the levels of vasopressin and plasma norepinephrine, and stimulate the release of growth hormone, thyrotropin and luteinizing hormone.
  • Cytidine 5′-diphosphocholine can reduce the release of free fatty acids and restore the activity of mitochondrial ATPase and cell membrane Na+/K+ATPase, thus alleviating brain damage.

Cytidine 5′-diphosphocholine side effects

Common side effects of cytidine 5′-diphosphocholine are as follows:

  • Cytidine 5′-diphosphocholine may irritate the gastrointestinal tract, resulting in symptoms such as nausea and vomiting.
  • If you are allergic to the ingredients in the medicine, you may experience symptoms such as skin itching and rash.
  • If used in large amounts for a long time, it may increase the burden on the liver, resulting in an increase in alanine aminotransferase and aspartate aminotransferase.
  • Arrhythmias may occur, and may even be accompanied by symptoms such as chest tightness and shortness of breath.
  • It may cause damage to the nervous system, resulting in dizziness, headache, insomnia, memory loss, drowsiness and other symptoms.
  • Sometimes it causes changes in blood pressure.
  • High doses of cytidine 5′-diphosphocholine may trigger manic or hypomanic episodes.

In the end

Cytidine 5′-diphosphocholine has many benefits and uses. But it also has many side effects. Therefore, we should always pay attention to its side effects when using it to ensure our own health. Natural Micron provides high quality and purity of Cytidine 5′-Diphosphocholine and can provide free samples for your testing. Contact us now for the best quote!

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