Choline is neither a vitamin or mineral. It is a water-soluble “nutrient” related to the B-Vitamin group. Choline was recognized as an “essential” nutrient by the US Institute of Medicine in 1998.[i] “Essential” because your body cannot make enough choline on its own. You need to get it from food, or a supplement.
Choline is found naturally in eggs, liver, beef, salmon, cauliflower, Brussels sprouts and breast milk. Eggs are often considered “brain food” because they supply high amounts of choline.
Choline is needed by your body for liver function, normal brain function and development, nerve function, muscle movement, cellular energy and metabolism.
Choline assists in methylation involved in genetic expression and the repair of DNA, nerve signaling, and detoxification.
Your brain has a huge appetite for choline. It is critical for the synthesis of the key neurotransmitter acetylcholine. Which your brain uses to maintain clear communication between its billions of neurons.
In fact, choline is so vital to cognition and nerve function that, without it, we couldn’t move, think, sleep or remember anything.
Not enough choline and you deal with poor recall, memory loss, fatigue, brain fog, inability to learn, feeling irritable or distracted, and difficulty walking or staying balanced.
Table of Contents
Stacking Racetams with Choline
If you use any of the racetam-family of nootropics in your stack, you likely should add a choline supplement. Because the racetams all affect choline and/or acetylcholine use in your brain in some way.
- Aniracetam – releases more acetylcholine (ACh)
- Coluracetam – increases choline – ACh conversion through the High Affinity Choline Uptake (HACU) process
- Noopept – modulates ACh transmission
- Oxiracetam – enhances choline-acetyltransferase (ChAT) which is used to synthesize acetylcholine
- Piracetam – potentiates the flow of, and increases the effect of ACh
- Phenylpiracetam – increases the density of ACh receptors
- Pramiracetam – increases choline – ACh conversion through the High Affinity Choline Uptake (HACU) process
- Nefiracetam – potentiates nicotinic acetylcholine receptors
I’ll dive into more detail on how each of the racetams affect acetylcholine in your brain in the post on acetylcholine. For now, you should know that when a racetam affects ACh in some way, it usually means you need to make sure more ACh is available. Or the racetam will not be as effective.
The other primary issue facing neurohackers are racetam-headaches. These headaches are unique because they usually only happen in a part of your brain. You’ll get to recognize them for what they are with more experience.
Racetam-headaches are caused by using a racetam without enough supplemental choline. Your brain is telling you it’s starved for choline.
Who Needs Choline
Even if you’re not interested in nootropics or brain optimization, anyone over 45 years can benefit from a good choline supplement. You’ll experience more alertness, energy, faster recall and better memory.
We all need choline for clarity and mental energy. And we have several nootropic supplements to choose from to boost choline in the brain. And increase the synthesis of acetylcholine.
We’ll review the best nootropics for boosting choline in your brain next.
Best Forms of Choline Supplements
As a nootropic supplement, Alpha GPC is about 40% choline by weight.
Alpha GPC naturally occurs in your brain as a byproduct of phosphatidylcholine (PC). When your brain needs more choline, and choline floating around in your brain is running low, it breaks down PC from cell membranes. And turns it into Alpha GPC.
And like other choline supplements, Alpha GPC provides the choline needed to synthesize acetylcholine.
But Alpha GPC is unique from other forms of choline. It helps increase human growth hormone.[iii] It restores and boosts nerve growth factor receptors in the brain.[iv] And stimulates the release of dopamine.[v]
One study in particular demonstrated why Alpha GPC is a favorite among neurohackers. 32 healthy volunteers received either Alpha GPC or a placebo. Ten days later they were injected with scopolamine to induce amnesia. The researchers found Alpha GPC was able to prevent the impairment of attention and memory normally caused by scopolamine.[vi]
The researchers showed that memory function in healthy young people could be boosted simply by taking Alpha GPC as a nootropic supplement.
Choline Bitartrate is choline combined with tartaric acid to increase bioavailability. One of the least expensive forms of choline, it’s about 40% choline by weight.
Like other choline supplements, Choline Bitartrate provides the choline needed for acetylcholine synthesis. But neurohackers have found this form is not nearly as effective as other forms of choline.
However, if Choline Bitartrate is the only choline supplement you have available, we do have the science to prove it works as a nootropic.
A research team in the Netherlands gave 28 volunteers 2 grams of Choline Bitartrate or a placebo. An hour and 10 minutes after taking the supplements, they had participants attempt to hit the center of a target.
The volunteers who used the choline supplement were not only more accurate at hitting the target center than the placebo group. The also did it faster.
The researchers concluded there was a “choline-induced bias” towards precision, speed and accuracy.[vii] Now logic tells us that you’d have this positive outcome with any choline supplement. So if all you have to take is Choline Bitartrate – you’ll be OK.
Choline Citrate is choline combined with citrate which is an ester of citric acid. Citrate is involved in the transport mechanism of acetyl units from its site of synthesis in mitochondria to the site of acetylcholine synthesis.[viii]
And citrate plays another important role in the brain. Citrate is an intermediate in the Krebs cycle (also known as the TCA cycle or Tricarboxylic Acid cycle, or Citric acid cycle).
Citrate synthase catalyzes the condensation of oxaloacetate with acetyl CoA to form citrate. Citrate then acts as the substrate for aconitase and is converted in aconitic acid. This cycle ends with the regeneration of oxaloacetate.
This series of chemical reactions is the source of 2/3’s of the energy we get from food. Most of the energy made available by these steps is transferred to form NADH. Which then drives adenosine triphosphate (ATP) synthesis that fuels mitochondria and provides the energy needed for brain cells.[ix]
One of the less expensive versions of choline, Choline Citrate is about 50% choline by weight. And like other sources of choline, provides the raw material needed to synthesize acetylcholine.
Acetylcholine is the neurotransmitter needed to signal muscle movement.[x] But Choline Citrate is unique because it helps prevent fatigue, muscle aches and pain following a workout.
I have personal experience with the benefits of Choline Citrate. For years, I saw a rheumatologist who injected cortisone into my shoulder muscles to relieve excruciating pain. Once I began supplementing with 3 – 4 grams of Choline Citrate per day, the severe muscle pain in my shoulders was gone.
CDP-Choline (Cytidine Diphosphate Choline or cytidine 5′-diphosphocholine) is also known as Citicoline. This naturally occurring choline source is present in every cell in your body.
The CDP-Choline supplement is unique as a choline source. Once it’s digested it separates into cytidine and choline. When it gets to your brain it converts back to CDP-Choline.
Choline is needed for the synthesis of acetylcholine. And cytidine is a component of Ribonucleic acid (RNA). This molecule is involved in coding, decoding, regulation and the expression of genes. And once it gets into the brain, it converts to uridine.
When choline is in short supply, neuronal signaling resorts to grabbing choline molecules from phosphatidylcholine (PC) in cell membranes. This is where uridine steps in. Uridine is used to synthesize phosphatidylcholine (PC). Supplemental CDP-Choline provides the uridine needed for this synthesis. Which means that CDP-Choline helps repair those same cell membranes. To maintain neuron integrity.[xi]
CDP-Choline is only about 18% choline by weight. But it packs a punch when it comes to brain optimization. And is a favorite nootropic stack addition with many experienced neurohackers.
CDP-Choline vs Alpha GPC
When it comes to choosing between CDP-Choline or Alpha GPC for your nootropic stack. There really is no contest. These two choline supplements work well together.
The synthesis of acetylcholine (ACh) is largely dependent on the choline provided by phosphatidylcholine (PC).
Alpha GPC is a byproduct of phosphatidylcholine (PC). And supplemental CDP-Choline provides the uridine needed for PC synthesis.
So taken together, you provide your brain with the type of choline it needs right down at the cellular level.
Combining CDP-Choline together with Alpha GPC
is a winning combination for any nootropic stack.
Side Effects of Choline
Choline is considered safe and non-toxic. Small amounts are made in your body. And it is an “essential” nutrient.
But too much choline, like all nutrients and supplements, can become toxic if too much is taken. Or your body does not need supplemental choline.
My wife is a classic example. This stunningly beautiful, charming, intelligent women turns into the Wicked Witch From the West if she takes a choline supplement.
Serotonin and acetylcholine have an inverse relationship in your brain. In other words, as one goes up, the other goes down. So taking too much of a choline supplement can boost ACh too much. And force serotonin levels to drop.
Symptoms of too much choline or acetylcholine can include:
- Irritability or anger
- Anxiety and/or depression
- Fatigue or feeling overly sleepy
- Trouble concentrating, brain fog, lack of focus
- Mental confusion or fatigue
- Decreased motivation
- Negativity, pessimism, rumination
- Poor memory
- Problems understanding or performing tasks
- Feelings of helplessness or hopelessness
- Diarrhea, constipation, gas, bloating, nausea, vomiting, dizziness
- Muscle weakness
- Tingling or numbness in the arms or legs
- Joint pain, discomfort or swelling[xii]
Nootropics Expert Recommendation
Every one of us needs choline to function. Choline is an essential nootropic supplement for anyone whose goal is brain optimization.
Choline is needed to synthesize acetylcholine (ACh). We need choline for cell-membrane signaling (phospholipids), lipid transport (lipoproteins), and methyl-group metabolism (homocysteine reduction).[xiii]
We need choline to provide the acetylcholine affected by any of the racetam-family of nootropics.
Your brain will start to literally consume itself to get the building blocks it needs to make acetylcholine. If you don’t provide it with enough choline.
I use 500 mg of Cognizin™ (branded form of citicoline) per day in my nootropic stack. Cognizin is included in the double-dose of Mind Lab Pro I use every day.
Whenever I feel a racetam-headache coming on I’ll take 500 mg of Alpha GPC. And the headache is gone within 15 minutes.
Your Mileage May Vary. Each of us has a unique body and brain. So what works for me may not work as well for you. Listen to your body and give your brain the choline it needs.
[ii] Kidd P.M. “Neurodegeneration from mitochondrial insufficiency: nutrients, stem cells, growth factors, and prospects for brain rebuilding using integrative management.” Alternative Medicine Revue. 2005 Dec;10(4):268-93. (source)
[iii] Ceda G.P., Ceresini G., Denti L., Magnani D., Marchini L, Valenti G., Hoffman A.R. “Effects of cytidine 5′-diphosphocholine administration on basal and growth hormone-releasing hormone-induced growth hormone secretion in elderly subjects.” Acta Endocrinologica (Copenhagen).1991;124(5):516-20. (source)
[iv] Vega J.A., Cavallotti C., del Valle M.E., Mancini M., Amenta F. “Nerve growth factor receptor immunoreactivity in the cerebellar cortex of aged rats: effect of choline alfoscerate treatment.” Mechanisms of Ageing and Development 1993 Jun;69(1-2):119-27. (source)
[v] Trabucchi M., Govoni S., Battaini F. “Changes in the interaction between CNS cholinergic and dopaminergic neurons induced by L-alpha-glycerylphosphorylcholine, a cholinomimetic drug.” Farmaco Sci.1986 Apr;41(4):325-34. (source)
[vi] Canal N., Franceschi M., Alberoni M., Castiglioni C., De Moliner P., Longoni A. “Effect of L-alpha-glyceryl-phosphorylcholine on amnesia caused by scopolamine.” International Journal of Clinical Pharmacology, Therapy, Toxicology. 1991 Mar;29(3):103-7. (source)
[vii] Naber M., Hommel B., Colzato L.S. “Improved human visuomotor performance and pupil constriction after choline supplementation in a placebo-controlled double-blind study.” Scientific Reports 2015 Aug 14;5:13188. (source)
[ix] Ebenhöh O., Heinrich R. “Evolutionary optimization of metabolic pathways. Theoretical reconstruction of the stoichiometry of ATP and NADH producing systems.” Bulletin of Mathematical Biology. 2001 Jan;63(1):21-55. (source)
[xi] Wang L., Pooler A.M., Albrecht M.A., Wurtman R.J. “Dietary uridine-5′-monophosphate supplementation increases potassium-evoked dopamine release and promotes neurite outgrowth in aged rats.” Journal of Molecular Neuroscience 2005;27(1):137-45. (source)
[xiii] Penry J, Manore M. ‘Choline: an important micronutirent for maximal endurance-exercise performance?’ International Journal of Sports Nutrition, Exercise and Metabolism. 2008;18:191–203. (source)
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