Centrophenoxine – An Overview
Centrophenoxine (sold as Lucidril, Centrophenoxin, Cerutil, Helfergin, or meclofenoxate) is a nootropic that is used as a prescription drug in some European countries as well as Japan.
It may have nootropic benefits for:
- Memory and learning
- Cerebral blood flow
Centrophenoxine is a potent nootropic agent that acts as an antioxidant, stimulates glucose uptake, oxygen consumption, and increases energy metabolism in the brain.1Zs-Nagy I. A survey of the available data on a new nootropic drug, BCE-001 Ann N Y Acad Sci. 1994
It is actually a combination of DMAE (dimethylethanolamine) and pCPA (parachlorphenoxyacetic acid), two individual nootropic compounds that have a synergistic effect.
What Does Centrophenoxine Do?
There is some evidence, mostly from animal studies, that centrophenoxine can prevent age-related damage to the brain.
It does this by acting as an antioxidant, clearing out products of cellular waste that can build up as we age.
Centrophenoxine can lower neuronal lipofuscin, which is a marker of cellular aging.
Lipofuscin builds up due to oxidation of “cellular garbage” that must be flushed out in order for the cell to work correctly.
Lipofuscin can mean oxidative stress and mitochondrial damage, and it is one of the major markers of aging.2Ohtani R, Kawashima S. Reduction of lipofuscin by centrophenoxine and chlorpromazine in the neurons of rat cerebral hemisphere in primary culture Exp Gerontol. 1983
Luckily, centrophenoxine helps get rid of this cellular garbage. Animal studies saw that this nootropic lowered levels of lipofuscin in the cerebral cortex, hippocampus, thalamus, basal ganglia, midbrain, medulla oblongata and spinal cord.
Ultimately, this should mean that there is less damage to the mitochondria in nerve cells, meaning they stay functionally “younger”.3Tani F, Miyoshi K. Neuronal lipofuscin in centrophenoxine treated rats, Folia Psychiatr Neurol Jpn. 1977 4Terman A, Gustafsson B, Brunk UT. The lysosomal-mitochondrial axis theory of postmitotic aging and cell death Chem Biol Interact. 2006
There is also evidence that centrophenoxine increases the rates mRNA synthesis in the brain cortex of old rats.
It seems to scavenge free-radicals, leading to RNA synthesis rates similar to that seen in rats half the age of the old rats.5Zs-Nagy I, Semsei I. 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 Gerontol. 1984
Centrophenoxines anti-aging properties could also be due to increasing glutathione production, which is a powerful antioxidant.6Roy D, Pathak DN, Singh R. Effect of centrophenoxine on the antioxidative enzymes in various regions of the aging rat brain, Exp Gerontol. 1983
There is some data that this benefit could extent to humans as well. Centrophenoxine treatment may be useful in dementia in older groups of patients.
One double blind study showed more improvement in treatment group than placebo.7Pék G, Fülöp T, Zs-Nagy I. Gerontopsychological studies using NAI (‘Nürnberger Alters-Inventar’) on patients with organic psychosyndrome (DSM III, Category 1) treated with centrophenoxine in a double blind, comparative, randomized clinical trial Arch Gerontol Geriatr. 1989
Memory and Learning
Centrophenexone can potentially improve cognitive function. Some of the same mechanisms that help it prevent aging can also enhance mental abilities like memory and learning.
It can increase the flow of acetylcholine, which is critical for memory tasks.
Centrophenoxine-treated animals learned tasks with significantly fewer trials, possibly due to decreased lipofuscin in the neurons of the cerebral cortex and the hippocampus.8Nandy K. Centrophenoxine: effects on aging mammalian brain J Am Geriatr Soc. 1978
Centrophenoxine was able to improve the altered short-term memory and cognitive performance resulting from aluminum exposure in rats.9Nehru B, Bhalla P, Garg A. Evidence for centrophenoxine as a protective drug in aluminium induced behavioral and biochemical alteration in rat brain Mol Cell Biochem. 2006
There’s also preliminary from human trials that it could improve aspects of cognition.
According to a study on elderly subjects, this nootropic appears to increase the consolidation of new information into long-term memory.
Researchers also found that significantly more of the subjects receiving centrophenoxine reported an increased level of mental alertness.10Marcer D, Hopkins SM. The differential effects of meclofenoxate on memory loss in the elderly Age Ageing. 1977
Centrophenoxine can prevent and possibly reverse cognitive damage in come cases.
It has the ability to inhibit MAO-B, which is the enzyme responsible for breaking down the neurotransmitter dopamine.
This ultimately raises the levels of dopamine in the brain.
This means it may be useful for treating conditions like Parkinson’s, which is characterized by low dopamine levels.
It’s antioxidant properties may also be useful in countering this disease.11Stancheva SL, Alova LG. Effect of centrophenoxine, piracetam and aniracetam on the monoamine oxidase activity in different brain structures of rats, Farmakol Toksikol. 1988 12Verma R, Nehru B. Effect of centrophenoxine against rotenone-induced oxidative stress in an animal model of Parkinson’s disease Neurochem Int. 2009
One study found that it could alleviate symptoms of Tardive’s Dyskinesia. This disease is marked by low levels of cholinergic activity, which centrophenoxine may be able to improve.13Izumi K, et al. Meclofenoxate therapy in tardive dyskinesia: a preliminary report Biol Psychiatry. 1986
Centrophenoxine may be beneficial in recovery from brain injuries.14FOSSATI P, et al. Centrophenoxine in the resuscitation of cranium-injured patients Lille Med. 1962
According to one study, centrophenoxine may be beneficial in the treatment of chronic alcoholism, although more study is needed.15Kulisiewicz TA. Evaluation of the effect of Lucidril (ANP 235, centrophenoxine) “Bracco” in some organic nervous diseases and in chronic alcoholism Pol Tyg Lek. 1965
Centrophenoxine can be a non-toxic herbicide used in cereal crops.16Ismagul A, Iskakova G, Harris JC, Eliby S. Biolistic transformation of wheat with centrophenoxine as a synthetic auxin Methods Mol Biol. 2014
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How Centrophenoxine Works In The Brain
Centrophenoxine is actually the synthesis of two separate nootropic substances, DMAE and pCPA.
DMAE increases acetylcholine flow, acts as an antioxidant, gets converted to phosphatidyl, a crucial building block of neural membranes. This can improve overall neural plasticity.
DMAE may also increase acetylcholine production, which is a critical neurotransmitter for memory and learning.17Bhalla P, Nehru B. Modulatory effects of centrophenoxine on different regions of ageing rat brain Exp Gerontol. 2005
However, DMAE has poor oral bioavailability. Luckily pCPA is a synthetic compound that can help it cross the blood-brain barrier and start taking effect.
Centrophenoxine can also increase glutathione. Glutathione is a powerful antioxidant that can decompose free radicals.18Chance B, Sies H, Boveris A. Hydroperoxide metabolism in mammalian organs Physiol Rev. 1979
One of the major ways centrophenoxine can improve mental function is by reducing lipofuscin in neurons. This has been found to stimulate brain metabolism, increase life span, and improve learning capacity.19Nandy K. Lipofuscinogenesis in mice early treated with centrophenoxine Mech Ageing Dev. 1978
This effect h on lipofuscin as also been shown to produce beneficial effects in some human pathological states such as cerebral atrophy, brain injury, and chronic alcoholism.20Gustafson L, et al. Effects of piracetam on regional cerebral blood flow and mental functions in patients with organic dementia Psychopharmacology (Berl). 1978
How Much Centrophenoxine Should I Take?
Standard dosing is 400-1000mg per day.
Many of the human trials looked at doses of 500mg in the morning and 500mg in the afternoon.
You should not take centrophenoxine later than 4PM due to its potential to interfere with sleep. Centrophenoxine Potential Side Effects
Some users do report stomach issues, anxiety, irritation, and drowsiness, so pay attention to how you are feeling if you decide to take it.
Centrophenoxine is not advised for pregnant women due to DMAE content.
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