What is Centrophenoxine?
Centrophenoxine, or CPH, is an ester of 2 other molecules: dimethylethanolamine (DMAE), which is a natural byproduct of choline that is also found in fish and parachlorophenoxyacetic acid (pCPA), a synthetic compound that is structurally similar to a family of plant growth hormones called auxins. It was first synthesized at the French National Scientific Center in 1959. It is also called meclofenoxate, and has been marketed under a number of different names, including Analux, Brenal, Cerebon, Luicidril, and Teluxidone.
How does it work?
Centrophenoxine is a fantastic source of choline. Other supplements have poor bioavailability, but esterifying DMAE and CPH make for an excellent delivery system. The chemical combination of the 2 molecules is believed to facilitate the entrance of centrophenoxine through the blood-brain barrier; more DMAE is able to access the brain when it is joined with pCPA. Once it makes its way past the barrier and into neurons, centrophenoxine is incorporated into the cell membrane, where it acts as an antioxidant and protects the membrane (which is composed of a double layer of lipids that are easily oxidized) from free radicals, which modify cellular proteins and cause them to clump together. This cross-linking of proteins prevents them from performing their normal functions.
Dr. Zs-Nagy, a well-known professor in Hungary, has performed extensive research into centrophenoxine’s mechanisms and feels that its antioxidant capabilities are primarily responsible for the observed effects. In addition to its role in the cell membrane, centrophenoxine is the only treatment that reduces the accumulation of a substance called lipofuscin in aged neurons. Because neurons are post-mitotic (non-dividing), they are decades old and tend to accumulate proteins that are damaged or no longer useful. Lipofuscin is one such harmful protein that increases with age but is decreased with centrophenoxine treatment, presumably via its antioxidant properties.
This compound is also thought to stimulate glucose and oxygen uptake and enhance neuronal resistance to various insults, such as low oxygen levels. Other studies have indicated that it increases acetylcholine neurotransmission. Research in rats demonstrated that it enhances neuronal firing.
The effects on acetylcholine levels and transmission are believed to increase attention and focus. Anecdotally, people who use centrophenoxine also report higher energy levels and sounder sleep. A double-blind study in healthy elderly subjects found that it improved the transition from short-term to long-term memory, but did not facilitate other memory domains (e.g., verbal or procedural).
Centrophenoxine may reduce the appearance of age spots, which are composed of lipofuscin deposits in the skin.
While centrophenoxine may have some benefit in the early stages of Alzheimer’s disease, it is likely ineffective in moderate and advanced disease. Some studies suggest that it may be useful in patients that suffer from dementia due to hypoxia (commonly known as vascular dementia).
Centrophenoxine Side Effects
Centrophenoxine is considered very safe; it is non-toxic at therapeutic doses. In fact, the main components of the molecule occur naturally in the human body (albeit not combined into a single entity). Nausea and dizziness have been reported. Some people may develop sore muscles, which typically disappear following a short (~1 week) hiatus from a centrophenoxine regimen. This compound should be avoided by pregnant or nursing mothers and people with epilepsy or severe high blood pressure.
Doses used in clinical studies have ranged from 600-2000 mg/day, which is given in 2 divided doses that are taken at breakfast and lunch. Lower doses are suggested for individuals that plan to incorporate centrophenoxine into an existing cognitive-enhancing regimen. The standard amount in a capsule is 500 mg, which may be taken twice a day.
Taking centrophenoxine with other nootropics, particularly those that affect the cholinergic system, will result in a synergistic effect. Although this sounds like it would yield more noticeable results, it is more likely to cause unpleasant side effects. People who use similar compounds, particularly racetams, should take dosages in the low range and may consider dividing a 500-mg capsule in half.
Centrophenoxine should be refrigerated to prevent degradation.
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Zs-Nagy, Imre. “A Survey of the Available Data on a New Nootropic Drug, BCE-001.”Annals of the New York Academy of Sciences 717.1 (1994): 102-14. Print.
Zs-Nagy, Imre, and I. Semsei. “Centrophenoxine Increases the Rates of Total and MRNA Synthesis in the Brain Cortex of Old Rats: an Explanation of Its Action in Terms of the Membrane Hypothesis of Aging.” Exp Gerontal 19 (1984): 171-78. Print.
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