It sounds like acetylcholine is another natural chemical produced in the body and the brain. But is it an important chemical? What functions does it have in the body and brain? Let’s see a little bit of history for it first.
Acetylcholine is a chemical that functions naturally in the brain and the body in many types of animals, including humans. It acts as a neurotransmitter that sends signals from one cell to other cells. It does have an important role in the sense that it is a cellular transmitter. The name is derived from a chemical: it is an ester acetic acid and choline hence the name acetylcholine. Parts of the body that are influenced by acetylcholine are labeled as cholinergic and substances that interfere with cholinergic activities are called anticholinergics. Acetylcholine is used at the neuromuscular junction (no it is not a four way stop sign in the brain) which means it is a chemical motor neurons release in the nervous system to activate muscles. This chemical has other functions in regard to the nervous system. It acts as neurotransmitter in the autonomic nervous system and as a final product released by the parasympathetic nervous system.
Unfortunately, there are drugs that can affect cholinergic systems in a very unhealthy way which could lead to health issues ranging from paralysis to convulsions. Other dangerous effects are caused by Numerous venoms and toxins produced by plants, animals, and bacteria, as well as chemical nerve agents such as Sarin, cause harm by inactivating or hyperactivating muscles via their influences on the neuromuscular junction. Let’s discuss some supplements of this natural chemical.
Acetylcholine has a few other roles as it pertains to the human body. It controls some brain and bodily functions including mood, cognition, and digestion. It is an antagonist for the fight or flight response which means it could block it. But it has many beneficial effects and can treat some serious health issues. Such as decrease heart rate and help digestion. It is noted that acetylcholine along with the powerful herbal supplement Huperzine A are supposed to enhance cognitive abilities this was confirmed in studies conducted on healthy volunteers.. It is well-documented that acetylcholine helps with cognitive function. Many drugs used to treat alzheimer’s disease increase acetylcholine levels at the synapse. (a junction between two nerve cells, consisting of a minute gap across which impulses pass by diffusion of a neurotransmitter.) One negative side effect of acetylcholine is that too much of it will cause depression. Now, the actual descriptions of some acetylcholine supplements.
Choline Bitartrate is one of the most basic and cheapest forms of choline and it is sold as a generic supplement on Amazon and at the GNC store. It sounds like it is very easy to acquire. I also make be a weak form choline. Supplementation with choline bitartrate increases the steady-state about 7 micromolar to ~11.5 micromolar in healthy women. As the process unfolds in the body. Choline is converted into acetylcholine once in the body by the enzyme choline acetyltransferase (ChAT).
CDP-Choline (also known as citicoline or cytidine diphosphate-choline) is a nootropic compound and nutritional supplement. It it is the star of many popular stacks. CDP-Choline is a potent blood brain barrier-permeable prodrug for uridine and choline. Choline is a substrate used to synthesize acetylcholine. Studies on humans say that:
- CDP-choline moderately improves attention
- promotes memory consolidation
- may aid in the prevention of cognitive decline.
CDP-Choline is comparably old compound originally developed and produced in Japan. CDP-Choline is changed into uridine and choline (which is acetylated to acetylcholine) in vivo. CDP-Choline could enhance the re-myelination of axons. (Remyelination is the process of propagating oligodendrocyte precursor cells to form oligodendrocytes to create new myelin sheaths on demyelinated axons in the CNS. This is a process naturally regulated in the body and tends to be very efficient in a healthy CNS. The process creates a thinner myelin sheath than normal, but it helps to protect the axon from further damage, from overall degeneration, and proves to increase conductance once again.) The myelin sheath surrounds and insulates projections called axons; the result is increased speeds of signals in the brain.
CDP-Choline was originally used in the treatment of acute cerebrovascular disorders in Japan. Then it was introduced in Europe, CDP-Choline was used as an adjunct to levodopa in the treatment of Parkinson’s disease. Some studies have also evaluated the use of CDP-Choline in the treatment of neurodegenerative disease and mild cognitive impairment.
Alpha-GPC is a choline-containing compound that may pharmacologically active when taken in higher doses. It is naturally present in small amounts in foods that contain choline. Alpha-GPC reduces the effect of cognitive function in elderly patients could be the most effective prodrug of choline. (A prodrug is just a precursor that is converted to the active agent in the body). Athletes are interested in Alpha-GPC because it increases the actions of the human growth hormone. Alpha-GPC is useful for nootropics purposes, most of its results were compiled from studies conducted on rodents. Studies conducted on humans may tell quite a different story; Alpha-GPC was only mildly to moderately effective of treating Alzheimer’s disease.
Huperzine A comes from the plant families known as Huperzia ceae and within 15 minutes of ingestion it supposedly Huperzine A appears in the cerebrospinal fluid which means it could easily penetrate the blood brain barrier. Is this good? Huperzine A is best-known for its inhibition of acetylcholinesterases, which increases acetylcholine at the synapse. It is a high-affinity inhibitor which has a slow dissociation constant. Huperzine A is also a NMDA-type glutamate receptor blocker (antagonist) like Magnesium and the Alzheimer’s drug Memantine. Huperzine A is able to promote neurogenesis (the creation of new neurons) in adult mice. But currently its effects on human brains just isn’t known. No studies have been conducted on humans. Watch out because Huperzine A is extremely potent; the typical advised dose is is 50-200 mcg daily. The LD50 (lethal dose that will kill 50% of the population) for Huperzine A was reported to be 2-4 mg/kg. This is a very small amount for lethal dose.
The LD50 for humans is lower than for rodent maybe because of the difference in surface areas between humans and rodents. Which really doesn’t make a lot of sense because the surface area in humans is much larger than in rodents. You would think the dosage would be higher for humans.
Quite frankly nicotine having any health benefits is hard to believe. Nicotine which is found in abundance in cigarettes is one hardest addictions to break. It can’t have any health benefits. But it is claimed nicotine is a parasympathomimetic alkaloid naturally abundant in tobacco. It is suggested that nicotine may improve working memory by activating nicotinic acetylcholine receptors in the brain. This doesn’t seem likely. Nicotine is not supplied in the traditional sense but it is sold as an over-the -counter gum called nicotine gum. Nicotine is an agonist at nicotinic acetylcholine receptors.
One researcher claims that nicotine is the only substance that reliably enhances the memory in healthy human beings. Here is the quote “To my knowledge, nicotine is the most reliable cognitive enhancer that we currently have, bizarrely,” said Jennifer Rusted, professor of experimental psychology at Sussex University in Britain when we spoke. “The cognitive-enhancing effects of nicotine in a normal population are more robust than you get with any other agent. With Provigil, for instance, the evidence for cognitive benefits is nowhere near as strong as it is for nicotine.” Whether this is a true statement remains to be seen. It is not conceivable that nicotine can improve memory in a healthy human being. If anything it would be a threat to a human being’s health. Whether nicotine gum or nicotine patches present any health risks remains to be seen.
It is said that citicoline is naturally produced in every cell of the body and in especially high levels in the brain. It is also a choline precursor increases acetylcholine This supplement had its beginning in treating strokes later it was used for treating cognitive diseases such as dementia and Alzheimer’s disease. Currently, it is supposed to enhance the functions of the brain. It may increase the flow of blood to the brain and encourages the production of new brain cells. It could improve memory, focus and attention. It has another name which is CDP-choline (which we talked about earlier as well) and it also has the name Cognizin which is a widely available bioavailable form of citicoline has been tested in humans. A daily dosage of this supplement is 1,000 to 2,000 mg for cognitive enhancement.
Warning Avoid these Acetylcholine Supplements
- If you buy a supplement that simply states “choline” on the label, it will almost certainly be choline bitartrate.
- But there is no evidence that this inexpensive form of choline reliably enters the brain or enhances cognitive functions.
- DMAE (dimethylaminoethanol) is another precursor to choline that’s found in some brain supplements.
- You may be familiar with it as a popular active ingredient in skin care products.
- While it does increase acetylcholine, studies have failed to show that it improves cognition.
- And since it’s been linked to neural tube defects, it’s not advised for use by women during their childbearing years.
- For these reasons, neither choline bitartrate nor DMAE are recommended choline-based compounds for raising acetylcholine levels.
Bacopa (Bacopa monnieri) has supposedly been used for thousands of years in Chinese and Indian medicinal traditions as a brain tonic. Bacopa is considered an adaptogen. Adaptogens are herbs that are neither sedate or stimulate but bring the body into a state of balance called homeostasis. One way bacopa does this by balancing of neurotransmitters including acetylcholine, dopamine, and serotonin. It may offset memory loss caused by anticholinergic drugs. In a head-to-head competition with the popular smart drug Modafinil, bacopa worked better to enhance memory, accuracy, and processing speed.
It is known to help those who battle a lot of stress or experience insomnia or anxiety. It is considered be so safe to use it can be administered to children. A typical daily dose of bacopa is 50 to 100 mg three times per day. If you want to experience maximum absorption take it at meals. You need to be patient because bacopa may take a few months to produce the most effective results.
American ginseng (Panax quinquefolius) is not as universally popular as its Asian cousin (Panax ginseng), but that may be about to change.So it is claimed. American ginseng is highly regarded because it is a higher quality supplement and is said to be a much more effective cognitive enhancer. For the best results for the brain look for supplements containing Cereboost, a patent-pending American ginseng extract that increases acetylcholine levels. In clinical tests, a single dose of cereboost rapidly improved memory, mental clarity, and sharpness within hours after ingestion. A typical dose of American ginseng or Cereboost is 100 to 200 mg daily. You can also take American ginseng as a tea or add dried slices to cooked foods.
This sounds like a brand of coke doesn’t it? Gotu kola (Centella asiatica) is in the same plant family as parsley and carrots and has been consumed as a food in Asia for thousands of years. Historically, it’s used to treat disorders of the mind including memory loss, mental fatigue, anxiety, and depression. Its Chinese name means “fountain of youth” because it is believed to give humans longevity. It is a highly respected brain supplement. According, to studies it it increased alertness by 100% and reduced anxiety and depression by 50%.
What makes Gotu Kola so unique is are compounds called triterpenes. (any of a group of terpenes found in plant gums and resins, having unsaturated molecules based on a unit with the formula C30H48.) These steroid precursors work somewhat like the drug Aricept to break down acetylcholine. They reduce the formation of amyloid plaques that accumulate in the brains of Alzheimer’s patients. It is claimed that because of the “Kola” in the name Gotu westerns think that gotu kola contains caffeine. Is there any recorded evidence for this perception? There probably is not. Actually, Gotu Kola contains no caffeine and is a relaxant and not a stimulant. The recommended gotu kola dosage for cognitive enhancement is 2,000 to 4,000 mg daily.
Galantamine (Galanthus caucasicus) is another acetylcholine-promoting herbal supplement that should be certainly be taken with caution. In the United States, it has been approved to treat Alzheimer’s disease and is available as a prescription and an over-the-counter remedy. Yet is advised to be taken with caution. It’s used to memory, reduce mental confusion, and slow the progression of Alzheimer’s. Its side effects are similar to huperzine A and unfortunately this supplement reacts negatively with hundreds of other medications. This could be the reason why you need to take it with caution. Before you try Galantamine talk with your doctor because you make be taking one of those medications it reacts badly with. Other supplements you can take:
While the above supplements are the most potent cholinergics, there are many other herbal remedies that exhibit some ability to increase acetylcholine:
ashwagandha (Withania somnifera)
holy basil (Ocimum sanctum)
ginger (Zingiber officinale)
cinnamon (Cinnamomum cassia)
arctic root (Rhodiola rosea)
turmeric (Curcuma longa)
saffron (Crocus sativus)
Vitamin B5 (pantothenic acid) is one of the B complex vitamins. “Pantothenic” means “from everywhere” because it’s found in so many food sources. While all vitamin B’s are essential for healthy brain function, vitamin B5 is critical cofactor needed to change choline to acetylcholine. This is amazing how the human body can change choline into the neurotransmitter acetylcholine. This could be why you may find vitamin B5 added to to alpha GPC, citicoline, and other brain supplements. Unlike many other vitamins vitamin B5 there is no RDA (Recommended Dietary Allowance) for vitamin B5. But the advised recommended daily allowance is 5 mg. (Recommended Dietary Allowance) If you take a good multivitamin, it very likely will meet or exceed this amount.
Acetyl-l-carnitine (ALC or ALCAR) is an amino acid and is well-documented for its ability to improve alertness, focus, mental clarity, and mood. This amino acid is a precursor to acetylcholine and has a similar structure, so it binds with and stimulates acetylcholine receptors in the brain. It also has fast-acting antidepressant properties making it a wise choice if you have memory loss and depression. If you shop for this ALCAR supplement don’t purchase the expensive version-l-carnitine because it will not enter the brain.
You know have a list of acetylcholine supplements that may help your brain functions noticeably and a lot of these supplements are used to treat Alzheimer’s disease. They help produce acetylcholine which are neurotransmitters produced in the brain. They can enhance the functions of the brain that studies have confirmed. It is highly advisable you talk to your doctor before you try any of these supplements. Especially with galantamine which needs to be taken with caution anyway. It reacts (as was discussed before) adversely with hundreds of other medications.