CDP-Choline, Citicholine, Cytidine-5'-diphosphocholine
CDP-choline (cytidine-5'-diphosphocholine) is a unique form of choline that readily passes through the blood-brain barrier. CDP-choline is a rate-limiting intermediate in the biosynthesis of phosphatidylcholine, an important component of the neural cell membrane.
Choline and pantothenic acid (vitamin B5) are used to produce acetylcholine, the major neurotransmitter that transmits nerve impulses between neurons. Choline is also needed for cell membrane integrity, and to move fats in and out of cells. Choline is, therefore, essential for proper brain function as the brain contains millions of nerve cells and is composed almost entirely of fats.
CDP-choline is also known by its drug name, Citicholine, which approved as a drug in Europe and Japan for use in stroke, head trauma, and other neurological disorders. It is presently being evaluated in phase II/III stroke trials in the United States. (D'Orlando and Sandage 1995)
Several mechanisms of action have been proposed for the neuroprotective effects of CDP-choline: (Conant and Schauss 2004)
CDP-choline increases the synthesis of phosphatidylcholine, which is used to repair neuronal membranes.
CDP-choline may prevent the catabolism of phospholipids from neuronal membranes when the demand for acetylcholine is increased or choline stores are low, which may occure after injury.
CDP-choline may reduce central nervous system ischemic injury by stabilizing cell membranes and reducing free radical generation.
CDP-choline inhibits the release of arachadonic acid, which may prevent the activation of phospholipase A1.
CDP-choline is an intermediate in the synthesis of sphingomyelin, an important component of the neural membrane. Sphingomyelin is hydrolyzed by sphingomyelinase, which is stimulated by tumor necrosis factor released during ischemia.
CDP-choline may counteract the deposition of beta-amyloid, a neurotoxic protein that is increased in patients with Alzheimer disease.
CDP-choline increases levels of neurotransmitters, including norepinephrine, dopamine and serotonin.
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