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Centrophenoxine

Centrophenoxine Overview

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Broadly speaking, centrophenoxine is best thought of as a brain-bioavailable form of DMAE that is capable of crossing the blood brain barrier with greater efficacy than DMAE alone. DMAE is a well established nootropic and it would appear centrophenxoine is similar.  A cholinergic compound,  centrophenoxine increases acetylcholine and thus can be thought to be mildly stimulating in higher doses.

Mixed research supports centropheoxine’s ability to attenuate lipofuscin buildup, a cellular wear and tear pigment associated with aging which is thought to reduce the ability of lysosomes to effectively clear cellular waste.

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Other names

Lucidril, Meclofenoxate

Centrophenoxine Background

Centrophenoxine, developed in 1959 at the French Scientific Research Center is one of the earliest nootropics discovered.  Centrophenoxine is a DMAE ester which allows for it to be transported into the brain with greater efficiency than DMAE alone. Centrophenoxine has been well studied for many years and has been found to act as a neural enhancer and also reverse some of the signs of aging by cleaning up waste products in the brain (4).

Centrophenoxine’s Method of Action

Increasing Acetylcholine

Acetylcholine

Acetylcholine

Although there have been much research performed, centrophenoxine’s method of action still isn’t completely transparent. What is known, is that centrophenoxine increases the amount of acetylcholine, a neurotransmitter that resides in the synaptic vesicles.  The specific pathways centrophenoxine uses are unknown. The two theories surrounding this are that it converts into an intermediary phospholipid which is then used to make acetylcholine or it breaks down into choline in the brain and naturally leads to the conversion of acetylcholine. Regardless, one thing we know is that centrophenoxine is a net cholinergic and may possibly be used as an alternative to other sources of choline.

Cholinergic Activity

Centrophenoxine’s cholinergic activity is believed to be responsible for improving memory formation and other associated cognitive benefits.  Centrophenoxine also helps increases the brains blood flow and oxygen uptake, which can support the brain’s energy demands and boosts mental energy levels (5)(6). This energy increase may be responsible for the increase in attention span users notice, making it easier to have longer study sessions without experiencing mental fatigue as much. In addition, centrophenoxine works to increase chemical activities and functions in the brain by enhancing glucose intake (1)(3).

DMAE Prodrug

The other way centrophenoxine works stems from the fact that it’s a source of DMAE. It is a biosynthetic version of DMAE that has better capabilities of crossing the blood-brain barrier and making it into the central nervous system.  Centrophenoxine also acts as a powerful anti-oxidant by playing a role in increasing the amount of acetylcholine. It has the ability to counter radicals and other products out of the brain that could damage it which helps the brain maintain good health by supporting brain cells and neurons.

Centrophenoxine Benefits

Lipofuscin Regression

Lipofuscin - A yellow "wear and tear" pigment.

Lipofuscin – A yellow “wear and tear” pigment.

According to a study that focused on changes in lipofuscin concentration, multiple unit activity in the CA3 region and lipid peroxidation in the hippocampus of male rats, centrophenoxine is capable of reversing lipofuscin and beta-amyloid pigmentation build up in aged brains (2)(4). The increase of RNA synthesis, glucose uptake, and protein synthesis in neurons and glial cells are dependent upon the reductions of lipofuscin build-up, and reportedly has no affect younger brains with no lipofuscin build-up (2).

There is going debate as to whether DMAE attenuates lipofuscin buildup in humans. Further research is required in this area.

Cognitive Enhancement

Centrophenoxine has been proven to be effective in treating dementia by showing an increase in skills on cognition testing after several weeks of a 2g daily dose. (7).

Dosing Centrophenoxine

For the aged 3-6 doses of 250mg is generally recommended for therapeutic usage in lowering levels of lipofuscin. In younger individuals who seek neuronal protection and neurological enhancement, 1-3 doses of 250mg has been touted as effective.

Centrophenoxine Safety

A clinical trial in which the mean age of the subjects was 64 revealed that over a 12 month time period, an extremely high daily dosage of 3 grams showed no harmful changes on the function of bone marrow and hepatic function (3).

Given DMAE’s theoretical teratogenic effects during early pregnancy through disruptions in choline metabolism, it would be prudent to avoid DMAE if trying to conceive (8).

References:

  1. http://www.ncbi.nlm.nih.gov/pubmed/1098982
  2. http://www.ncbi.nlm.nih.gov/pubmed/8367013
  3. http://www.ncbi.nlm.nih.gov/pubmed/35024
  4. http://www.ncbi.nlm.nih.gov/pubmed/1106435
  5. http://www.ncbi.nlm.nih.gov/pubmed/6799848
  6. http://www.ncbi.nlm.nih.gov/pubmed/6405547
  7. http://www.ncbi.nlm.nih.gov/pubmed/15374499
  8. http://www.ncbi.nlm.nih.gov/pubmed/15374499