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Choline (Alpha-GPC & Bitrate)

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By Jonathan Roseland  Connect    

It's especially useful to our brains in synthesis and release process of the neurotransmitter acetylcholine by neurons.

Choline, a water-soluble nutrient, is essentially one step removed from the real nootropic, Acetylcholine, for which it is a chemical precursor. Choline itself cannot travel across the blood-brain barrier to become Acetylcholine (which we'll refer to from now on as ACh), bitrate Choline is somewhat more effective in crossing it and Alpha GPC freely moves from the bloodstream into the brain.

Choline and Alpha GPC is a favorite of responsible Biohackers because it balances out the brain chemistry that results from the heightened baselines of other neurotransmitters, particularly Dopamine and Serotonin, resulting from taking the Racetams and other Nootropics.
Any fairly vocal Biohacker is accustomed to hearing this general criticism:
"You shouldn't take things that unbalance your brain chemistry or use up your neurotransmitters because you don't know what that's going to do long term..."
My response is that everything in our environment - from a stressful day at the office or a decadent dessert we eat at a party to watching a scary movie - imbalances our brain chemistry.
Supplementing choline precursors is just a very direct way of rebalancing it. Also, our mind and body are a master self regulator, humans thrive and survive is vastly different spectrum of environments, if I take an excess of a particular cognitive enhancer the body will flush it out or just store it as fat.
It's a good idea to supplement Choline if you are taking Piracetam or other racetam nootropics which increases the rate at which your brain uses ACh. Otherwise the racetams can cause headaches.

Acetylcholine - a Neurotransmitter of Many Talents

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ACh works in both the peripheral nervous system and the central nervous system. The peripheral nervous system is what we think of as the system that pervades our entire body so our muscles can get instructions from our brain, the central nervous system consists of our brain, spinal cord and to an extent our auditory, olfactory and visual sensory systems in the head.
It's a communicator between our mind and muscles, so it affects everything from athletic performance to coordination. For this reason everyone from professional gamers to autosports drivers take it to give them a competitive edge. It's functions include:

  • It delivers instructions to cardiac muscle fibers.
  • It's release in the hippocampus is essential to learning and formation of new memories.
  • Levels of ACh in cortex are linked to responsiveness to audio and visual stimuli.

"I find myself typing faster and getting more done when I'm on ACh [precursor supplement]" once reported a now infamous Biohacker in Nicaragua.

Mechanisms of Action

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  • It's an essential cog in the lipid metabolite synthesis process, which results in the manufacture of ACh.
  • For the efficient transport/transmission function of the ACh system.
  • It provides membrane fluidity to cells throughout the body, a lack of which results in membrane rigidity. In this respect it's a factor in aging and cell death according to a 2008 Italian study.

Alpha GPC

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Glyceryl Phosphoryl Choline is the most bioavailable form of choline you can supplement regularly. It's an important part in both the genesis of ACh, as a building block of the neurotransmitter and in optimizing the ongoing effectiveness of the overall system. If the ACh system were a car, cholinerics are oil.
There's over 100 results on Pubmed for human research in just the past 5 years specifically for Alpha GPC. It is my preferred ACh precursor because it's the closest to the actual neurotransmitter. It's a little more expensive but my mind, especially my memory and capacity to learn fast, is my money maker so I get the most bioavaliable.

Neuroplasticity

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This is the capacity of our minds to adapt to novelty - learning Portuguese, studying philosophy or starting a martial art - and thrive. Personal development of any significance requires that the gears of the mechanisms of Neuroplasticity are well greased.
A 2009 paper Alternative medicine review stated "[Alpha GPC] is neuroprotective and supports neuroplasticity via nerve growth factor receptors."
ACh plays an especially important role in the formation of new long term memories;
Focusing effect of acetylcholine on neuroplasticity in the human motor cortex, a 2007 German study of 12 healthy human subjects, includes some great insights...
"Cholinergic neuromodulation is pivotal for arousal, attention, and cognitive processes..."
The German study went on to say that...
"...it has been hypothesized that ACh enhances the signal-to-noise ratio of input processing... These findings are in line with a cholinergic focusing effect that optimizes the detection of relevant signals during information processing in humans."
This finding is great news for overwhelmed lifehackers, entrepreneurs, professionals and students, who face the continual challenge of distraction. The healthy Germans in the study got better at focusing on the important information due to the long term excitability that ACh facilitates. It's been well said that we live finite lives in an age of infinite distraction; the screens that are rarely further than an arm's reach away from us are constantly socially engineering us to ignore our actual goals and instead get stuck in the quicksand of digital amusement. Nootropics like this are a potent tool for getting unstuck.

An Anti-Memory Loss Agent

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Forgot your keys? Walked into a room of your house and can't remember what you are supposed to be doing there? Opened a browser tab and forgot what you are working on? Or is the name of someone you met just a week ago 'on the tip of your tongue'?

  • A University of London study of over 7000 civil servants, demonstrated that age related memory decline can start in your 40's.
  • A University of Perugia review of the data of 13 clinical trials, totaling over 4000 human participants, identified it as an effective therapy for memory loss, as indicated by memory tasks. A placebo controlled study in the review, found that after 3 months those treated increased memory function by 15.6% while those on the placebo declined by 8%.

Cognition Enhancer

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A self experimenter on Longecity reported:
"I suffer from cognitive delays (tests indicate I function roughly at a third of the cognitive speed of most people), major depressive mood disorder, and chronic fatigue... I find that this also has a calming effect, but it leaves my mind razor sharp."
To quote a 2013 Italian paper "In a number of clinical studies, alpha-GPC demonstrated benefit in patients with cognitive dysfunction. In light of the limited therapeutical results obtained in the past decades by the use of cholinesterase inhibitors in dementia, and of the relevance of their side effects in long-lasting therapies..."

Alzheimer's

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To quote a 6 month double blind study of 261 human subjects afflicted with mild to moderate Alzheimer's:
"In this multicenter, double-blind, randomized, placebo-controlled trial, patients affected by mild to moderate dementia of the Alzheimer type were treated... Statistically significant differences were observed between treatments after 90 and 180 days..." on a variety of scales that are used to measure severity of cognitive decline as a result of supplementing 1200 milligrams (split into three doses daily) for 6 months.
A recent human study from Georg-August-University, Germany stated:
"Loss or dysregulation of cholinergic inputs leads to cognitive impairments like those manifested in Alzheimer's disease. Such dysfunction can be at least partially restored by an increase of [ACh]."
In a population study done in Hordaland, Norway of 46-74 year olds choline blood levels were found to be inversely correlated with anxiety symptoms. Choline is used as treatment for bipolar disorder, alcoholism and Alzheimer's disease.

Sleep

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A University of Barcelona, Neurology Department paper noted that Choline supplementation improved sleep as measured by the Pittsburgh Sleep Quality Index (PSQI).

Lucid dreaming

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An Alpha GPC supplement called Galantamine is particularly popular amongst lucid dreaming aficionados. The popular anecdotal experience reported by lucid dreamers is that they get the most lucidity bang for their cholinergic buck by doing Alpha GPC a few hours into their nightly sleep cycle, yes this means they wake up in the middle of the night to take pills, which while not ideal for sleep isn't so big of a problem if they are waking up anyways to write in a dream journal (see my Evernote lifehack for this).

Stoke

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Or mini--stroke (known in dorky medical jargon as transient ischemic attack) sufferers should strongly considering supplementing 1200 milligrams daily.
Integrated Brain Restoration after Ischemic Stroke, a 2009 paper University of California, Berkeley stated:
"Brain injury from ischemic stroke can be devastating, but full brain restoration is feasible... [Alpha GPC] has been administered to almost 3,000 stroke patients in five stroke trials. Brain plasticity underpins the function-driven brain restoration that can occur following stroke."

Pregnancy

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Choline is very important during pregnancy, rat experiments support the theory that healthy levels of Choline during pregnancy are essential long term memory capacity of the baby.

Sources

In nature we find Choline in high amounts in

  • Beef liver (5oz has +400 milligrams of Choline)
  • Atlantic cod
  • Salmon
  • Pastured eggs (One egg yolk contains 115 milligrams of Choline)
  • Grass-fed raw dairy

If you have a highly optimized, all organic diet you're in good shape, however Choline deficiency is common (90% of the general population by some estimations) and supplementation is a good idea, especially if you are taking other smart drugs that affect the ACh system.
Alpha GPC, consumed in powder form is clumpy has a mostly boring taste but is frequently described as sweet. It's a suspicious looking white powder that you really would want to keep out of sight of TSA agents, border guards or highway patrol officer.

Socializing Effects

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One self experimenter reported it's affects on socially induced nervousness:
"Also it's like social anxiety is suddenly disappearing. I'm not antisocial, but I normally have to force myself to greet others. For the last two weeks I have been casually going up and talking to people I normally avoided."

Athletes

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Interestingly this same Nootropic that maintains the minds of the aging and protects the cognition of those afflicted by stroke also provides a quantifiable advantage to top performing physical specimens; from MMA fighters and bodybuilders to collegiate athletes and endurance sports aficionados.
2004 paper published in Powerlifting USA Magazine, illuminates a few crucial considerations for athletes:
"Thomas Incledon, president of Human Performance Specialists, a sports pharmaceutical consulting firm, cites acetylcholine and associated neural co-factors as the next generation of ergogenics: "Increasing acetylcholine and neurotransmitter enhancers will be one of the next phases. When you increase acetylcholine, you are able to activate more muscle fiber, which, in turn, lowers the relative intensity of a workout [by increasing the amount of weight that can be lifted]."
"How does one simultaneously increase motor unit recruitment, increase muscle fiber stimulation, and decrease muscle fiber fatigue? Understanding the role and optimization of acetylcholine is the key to bridging the "power gap" and actualizing true genetic strength potential."
A 2012 Japanese study stated "...These findings suggest that a single dose of GPC increases growth hormone secretion and hepatic fat oxidation, with concomitant increases in choline levels, in young adults."
In another double blind study of 7 human males, the subjects improved their power output by 14% 90 minutes after supplementing 600 milligrams. To quote the study:
"These data indicate that a single 600 mg dose of [Alpha GPC], when administered 90 minutes prior to resistance exercise, increases post-exercise serum [growth hormone] and peak bench press force."

Antioxidant

It combats free radicals in the cells, that are introduced by stress and environmental pollutants, another important aging factor.

Nootropic Ingredients

Recommended Daily

For boost in brain power 500mg daily + normal dietary intake.

Popular Cofactors

Cofactors:

For the purposes of cognitive enhancement in healthy Biohackers, Alpha GPC is rarely consumed on it's own.
Racetams, especially Piracetam, are a popular combination. The Longecity.org crowdsourced recommended Piracetam-Choline ratio is 4:1
Alpha GPC is potent stuff so the ratio recommended is pretty asymmetrical; for 4-6 grams of Piracetam, you would want to take 500 milligrams, a 8:1 ratio.

Other Cofactors

A lot of Nootropics promote the release of ACh but do not provide the building blocks for it, so it's a good idea to add choline if you are supplementing
Ampakines, particularly Aniracetam, the popular dosage is 1500 milligrams Aniracetam to 500 milligrams Alpha GPC, a 3:1 ratio.
B Vitamins, are involved in the conversion of Choline into ACh, especially B5.

Side Effects:

In human study of 44 participants the researchers concluded "The trial confirms... and the low percentage of adverse events confirms its excellent tolerability."
Based upon my reading of hundreds of forum threads, reddit posts and user testimonials, it seems to me that higher percentage than usual of users report adverse effects of headaches, irritability and general moodiness either immediately or a few days after adding Alpha GPC to their supplemental regimen. The ACh system in the body is very complicated, supplementing it with such a bioavailable source is not conducive to everyone's constitution. The informed recommendation seems to be; if you aren't feeling great on Alpha-GPC switch to a different source of choline, CDP choline, choline bitrate or Centrophenoxine.
Rat testing has also demonstrated that alcohol lowers Choline levels, obviously this isn't good for your long term brain health so it's probably a good idea to supplement a Choline nootropic if you drink socially.More than 3500MG daily can lead to diarrhea, low blood pressure and fishy odor.

Photos

Videos

Medellín Biohacking #1: Mixing 8 Smart Drugs with Green Tea
Choline vs Alpha GPC vs Acetylcholine: Smart Drugs of Many Talents
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