Centrophenoxine, also commonly referred to as meclofenoxate, is considered by many to be an invaluable addition to their nootropic stack. It is a potent and well-respected cholinergic nootropic supplement that can improve memory, mood, and mental performance, slow down and reverse signs of cognitive aging and protect brain health. This amazing nootropic has scientific research backing of more than 50 years as an excellent choline source and for use with combination with other nootropics.
Centrophenoxine is derived from Dimethylaminoethanol (DMAE) then specifically modified to increase its potency and intensify its ability to cross the blood-brain barrier (BBB). (1) Therefore, centrophenoxine carries the same benefits of DMAE but is more effective as a therapeutic agent. For this reason, centrophenoxine has been widely adopted by most nootropic users.
Centrophenoxine mainly works by delivering and enhancing the actions of choline. Choline is the precursor of acetylcholine, an essential and limitless neurotransmitter that is strongly associated with cognitive acuity, plasticity, and memory. It is not clear how exactly centrophenoxine increases the levels of choline and acetylcholine, but it is thought that it either naturally breaks down to choline or it converts to an intermediary phospholipid that is then used to produce acetylcholine. (2) Regardless of the pathway, it is the cholinergic capability that makes centrophenoxine such a powerful potentiator nootropic in its own right.
In addition to upregulation of acetylcholine production, centrophenoxine is also known to be a powerful neuro energizer that stimulates overall brain activity by improving glucose absorption and increasing oxygen uptake. (3)By doing so, centrophenoxine makes the brain function more efficiently, thus improving focus, concentration, and clarity of thoughts, getting rid of the so-called brain fog. As a potent antioxidant, it scavenges free radicals, flushes out toxins and participates in the repair of damaged cells. (4) Lastly, it reverses cognitive aging by reducing or even eliminating the build-up of metabolic waste products that are considered to be “wear and tear pigments.” (5)
A much sought-after benefit of centrophenoxine is for protection of the brain from age-related cognitive decline. Studies have shown that centrophenoxine can decrease accumulation of age-related pigments including lipofuscin, beta-amyloid, and potassium while at the same time increasing helpful materials such as RNA and protein synthesis. (6)
Lipofuscin is one of the most striking of these pigments as it occupies more than 30% of the volume of aging cells. (7) Lipofuscin accumulates with age, especially within the skeletal, neuron and heart tissues. (8, 9). When the levels get to a critical volume, the cells become less functional, and they end up dying. In the brain specifically, the cells disrupt the transmission of nerve impulses to other organs.
Prolonged administration of centrophenoxine leads to significant reduction of lipofuscin. (10) Multiple studies have shown that it eliminates nearly half of the accumulation of brain lipofuscin in just 6 to 8 weeks. In an article (11) published in the Brain Research Journal, researchers were able to show the lipofuscin-lytic activity of centrophenoxine. They were able to demonstrate a reduction not only in the brain but also retina, spinal cord and Purkinje cells of the heart.
Centrophenoxine also prevents cognitive aging by reversing the accumulation of potassium in the brain. Potassium is critical in synaptic transmission and proper signaling, but when it accumulates beyond its physiological ranges, it contributes to poor cognitive functioning. (12) Centrophenoxine has the ability to increase intake of glucose while promoting removal of both carbon dioxide, potassium and dissolving the lipofuscin pigments.
Another exciting thing about centrophenoxine is that it increases neuronal RNA, which is used by neurons to make proteins for encoding memory and mending damaged brain cells. (13) An even more exciting bit is that it increases the capacity of the brain to reorganize itself by forming new neural connections, to compensate for injury, age-decline, and disease. This action is both by increasing RNA for repair of cells and indirectly through acetylcholine neuromodulation. (14)
All the actions mentioned above not only prevent but also halt and reverse signs of cognitive aging. For this reason, centrophenoxine is not just a dietary supplement but also a drug licensed for the treatment of symptoms of senile dementia and Alzheimer’s disease.
One of the most damaging molecules present in the brain are free radicals. (15) The brain is prone to the damage of these free radicals or reactive oxygen species partly due to the high energy requirements, high oxygen consumption, high brain tissue concentration of iron and low levels of antioxidants. In the brain, free radicals attach themselves to molecules of fat in nerve cell membranes, upsetting the delicate function of the membrane and consequently leading to failure in the regulation of substances coming in and out of the cells.
These free radical damaging actions have been implicated in strokes and degenerative disorders of the brain. Antioxidants are helpful in defending brain cells against free radicals by breaking them into harmless substances or by binding to them and inhibiting them from attacking healthy cells. Since the brain does not have many antioxidants, it needs an external supplementing source to ameliorate the effects of oxidative stress- this is where centrophenoxine comes in. (16)
When centrophenoxine crosses the BBB, some of it is incorporated into the nerve cell membranes, where it persists for more than 24 hours. It decreases the concentration of lipid peroxidation products (lipid peroxidation is the oxidative degradation of lipids, a process by which free radicals obtain electrons from fats in cell membranes). (17) In addition, centrophenoxine also increases the effect of other antioxidants including glutathione, the mother of all antioxidants. It also activates catalase and superoxide dismutase, both of which are enzymes that play a role in breaking down potentially harmful oxygen molecules.
Beyond neuroprotection and reversing signs of cognitive aging, centrophenoxine also acts as a mild but noticeable anti-depressant. (18) It can make a huge difference in both physical and mental performance by maintaining healthy and positive moods thus enhancing the capability of productivity. For people who experience temporary mood problems, centrophenoxine goes a long way in restoring good feelings. However, this benefit of mood management is not only for those with some degree of mood disorder- it can be used to provide an overall mood boost, especially when taken in the morning.
So, how exactly does centrophenoxine improve mood?
First, by enhancing absorption of glucose and oxygen to the brain, centrophenoxine increases chemical activity that improves focus and motivation. It leaves you feeling energized as opposed to feeling tired and easily drained. Second, by potentiating the actions of choline, it helps increase the levels of GABA to help combat the overwhelming symptoms of depression and anxiety.
Low levels of choline are associated with not only poor mood but also a lack of energy and memory loss. Evidence suggests that upregulation of choline is excitatory. (19) It alters brain excitability, influences synaptic transmission, and coordinates firing of groups of neurons through acetylcholine. Also, stimulation of the cholinergic centers of the brain affects the wake-sleep cycle. As you well know, sleep and mood are closely connected- lack of refreshing sleep can cause irritability and stress, while adequate quality sleep enhances well-being.
The generally recommended dosage of centrophenoxine is between 200mg and 1 gram per day. However, doses of centrophenoxine vary with one’s desired effect, age, and the body’s sensitivity levels. For nootropic benefits, smaller doses spread throughout the day are preferred, to ensure that the brain gets a constant supply at all times. To reverse the signs of brain aging, higher doses may be needed for a month. (20)
Being a fat-soluble compound that is metabolized in the liver, it is best taken with a meal to achieve better absorption and metabolism. If taken as a single dose, it is advisable to take centrophenoxine in the morning, to experience increased energy for the better part of the day. If taking two doses, the second one should be taken early in the afternoon. If taken late in the afternoon, it can interfere with sleep patterns, by making it difficult to fall and stay asleep.
Centrophenoxine is generally well tolerated by most users, but some people may experience side effects such as insomnia (when taken just before or at bedtime), headaches, gastrointestinal disturbance, and dizziness. Most of these effects are noted in the initial days of use, and they should subside with continued use. Also, the higher the dose, the more likely it is to experience the side effects. As it is with most other supplements, it is best to start with the lowest possible doses and gradually build up.
Pregnant women or those planning to get pregnant in the near future should not use centrophenoxine as it is known to cause congenital disabilities. The risk is highest in the first trimester when organogenesis is taking place. (21) The risk goes down in the subsequent trimesters, but it is generally prudent to avoid it altogether when pregnant.
Centrophenoxine is commonly taken with other nootropics. A wide variety of them such as Piracetam are heavily dependent on a good supply of cholinergic compounds in the brain, for them to be fully effective. Centrophenoxine may, therefore, be a substantial supplement to increase the potency of other nootropics.
As mentioned before, centrophenoxine has more than five decades of research, making it one of the earliest and vastly studied nootropics. It was developed in 1959 by a scientific team from the French National Scientific Research Center. (22) Although it is now popular for its nootropic and cognitive enhancement benefits, it was initially created for the treatment of cognitive decline diseases such as Alzheimer’s. It has been widely accepted as a dietary supplement for it is affordable, a potentiator of other supplements and for its scientific record.
Centrophenoxine is an outstanding choline source that is affordable, readily available and has a long-standing success track record. Furthermore, it works exceptionally well with other nootropics supplements. Here are the closing thoughts on this remarkable nootropic.
It is also known as meclofenoxate and is a derivative of Dimethylaminoethanol (DMAE) that is modified to enhance its bioavailability and ability to cross the blood-brain barrier.It was first developed in 1959 by scientists of the French National Scientific Research Center.Centrophenoxine works by enhancing the actions of choline and thus, is a cholinergic nootropic. It is thought that centrophenoxine increases the level of choline by either naturally breaking down to choline or to an intermediary phospholipid that is used to synthesize acetylcholine. The neurotransmitter then effects most of the nootropic benefits.It also increases brain activity by promoting uptake of oxygen and glucose in the brain cells. This neuro-energizes the brain, leading to improved focus, concentration, and mental clarity, clearing the common brain fog.As an antioxidant, it renders free radicals harmless, thus protecting neurons from oxidative damage.Centrophenoxine prevents the build-up of metabolic waste products such as lipofuscin which are responsible for cognitive aging.It boosts mood by affecting neurotransmitters such as GABA and acetylcholine, and also, by contributing to the sleep-wake cycle regulation.Recommended doses are between 200 and 1000mg. The supplement is best taken in the morning or early afternoon, with a full meal and preferably with other nootropics like Piracetam.Centrophenoxine is well-tolerated, but some people may experience side effects when on high doses or during the initial days of use.Centrophenoxine is not generally recommended for pregnant or nursing women.