Melatonin

Melatonin


Summary: Melatonin is known for helping insomnia, is a powerful antioxidant and anti-inflammatory, protects against neurodegenerative diseases, stroke and brain trauma. At a microdose of 300mcg, Melatonin is gaining wide popularity and most healthy nootropic users are found to include it in their evening stack.




Introduction


What is Melatonin?

Melatonin is a multitasking hormone produced by the brain’s pinecone-shaped pineal gland. [R]

Melatonin plays several roles in the body, including helping to regulate blood pressure, boost immune function, and manage cortisol levels. [R] [R]

But melatonin is probably best known for its soporific powers. Chief among its responsibilities is regulating the body’s circadian rhythm so it knows when to rest and when to wake up. That’s why melatonin is often referred to as the body’s sleep hormone.


Benefits & Effects


Melatonin Regulates Circadian Rhythm and Enhances Sleep Quality

Melatonin increases the quality of sleep. The Circadian Rhythm influences the body’s sleeping habits.

Think of it as a built-in clock that controls our bodies processes 24 hours a day.

Scientists have observed that Melatonin normalizes the Circadian rhythm which can sometimes become distorted due to modern lifestyle. [R]

Melatonin Alleviates Anxiety and Depression Symptoms

Conditions like depression and anxiety usually worsen by a disturbed, intermittent or a lack of a sleeping pattern.

Having these disturbances regulated can alleviate the symptoms of these conditions, not mainly offering a cure but by far offering an improvement in the standard of life. [R]

Melatonin is a Potent Antioxidant

Antioxidant enzymes roles within our bodies are to help clean the cells in our bodies and filter our bloodstream from harmful cells. Melatonin increases the rate at which our body produces these enzymes that would be naturally.

These molecules in question can also bond to what is called Reactive Oxygen Species (ROS) & Reactive Nitrogen Species (NOS) which can decrease the level of damage each of these can cause respectively.

The benefits directly from this are that Melatonin prevents any harm coming to your organ systems or tissues. These advantages combined make Melatonin a very useful protectorate within your body internally. These antioxidants can also have benefits for the most critical organ in our body, our brain. [R]

Melatonin Supports BDNF

Nerve cells are also protected by the increase of these enzymes produced by Melatonin, having a positive onward affect towards the spinal cord including white matter and optic nerves. Its regeneration is down to something called the ‘Brain-Derived Neurotrophic Factor’ (BDNF); in simple terms, this is a protein responsible for the nerves regeneration and well-being within our brains. [R]

Melatonin Strengthens the Blood-Brain Barrier

Melatonin strengthens the ever significant barrier between the brain and our blood. If the strength of this barrier were to deteriorate and for example leak, this can lead to cognitive dysfunction (also known as brain fog) and could potentially result in future to conditions such as Alzheimer’s. [R]

Melatonin is Neuroprotectant

In addition to defending against conditions such as Alzheimer’s development, Melatonin can also aid as a coping mechanism for users who have Parkinson’s.

Melatonin in tests was shown to prohibit cell death and brain damage, sometimes as a cause of a leaky blood-brain barrier.

Referring back to the regulation of sleep, this can also help people who, however, there is currently no proof it helps with any of the other side-effects of the condition. [R]

Melatonin Replaces Benzos for Sleep

Its widely known that benzos usually depress the natural levels of melatonin within our bodies.

Our recommendation is if you are using one of these drugs for sleep, it would be wise to start using melatonin instead. Moreover, start weaning yourself off the benzos. [R]


Mechanism of Action


Melatonin works together with your body’s circadian rhythm.

In simple terms, the circadian rhythm is your body’s internal clock. It lets you know when it’s time to sleep, wake and eat.

Melatonin also helps regulate your body temperature, blood pressure and hormone levels [R]

Melatonin levels start to rise in your body when it is dark outside, signaling to your body that it is time to sleep [R]

It also binds to receptors in the body and can help you relax. For instance, melatonin binds to receptors in the brain to help reduce nerve activity. In the eyes, it can help reduce dopamine levels, a hormone that enables you to stay awake. [R] [R]

Melatonin is controlled by light and darkness. When we’re awake and the sun’s out, we don’t produce any melatonin. But at night, the onset of darkness signals to our pineal gland to release melatonin into the bloodstream.

Your melatonin levels begin to increase about two hours before you go to bed, typically around 9 p.m., and peak about five hours later. As melatonin levels rise throughout our body — it’s found in a variety of our organs, including our eyes, bones, ovaries/testes and gut — our body knows it’s time to drift off to Slumber Town. [R]

Melatonin exerts many of its effects vicariously through melatonin receptors, similar to how insulin affects the insulin receptor. The melatonin receptors are named MT1 and MT2, and are G-protein coupled receptors (GPRCs) coupled to Gi proteins (a heterotrimer of α, β, and γ that dissociates into α and βγ when the receptor is activated). These two receptors are quite different from each other, as they structure pharmacological characteristics and chromosomal location, yet both have high affinity for melatonin. A third ‘receptor’ exists, known as MT3, but it is not a GPRC like MT1/2. Due to the cytoplasmic protein quinone reductase II having the same melatonin binding properties as ‘MT3’, and deletion of quinone reductase II causing ‘MT3’ to disappear, MT3 may just be quinone reductase II.

Examine.com

Dosage


How To Take Melatonin?

You’ll see melatonin recommended in a range of doses, starting at around 0.5 milligrams up to 10 milligrams for people with sleep disorders, with the most common dosage being around 3 milligrams.

But even this is probably way more than you need.

You’re better off basing your melatonin intake on increments that mirror how much melatonin our bodies produce at night. According to clinical studies, the optimal dose is 0.3 milligrams. [R]

Melatonin Overdose

Even though the overwhelming verdict is that melatonin is safe, you can have too much of a good thing. Overdosing on melatonin has not been shown to be fatal, but it can produce the aforementioned side effects, like dizziness and grogginess. In one known case, after taking 24 milligrams of melatonin, a man became lethargic and disoriented, but returned to normal and did not continue to have issues once he lowered his dosage.

In addition, large doses could potentially cause amenorrhea (skipped periods) in women, due to it suppressing gonadotropin-releasing hormones, but if you can easily remedy this side effect by simply stopping your melatonin supplements. [R]


Side Effects


Overall, the side effects of melatonin are pretty toothless. Unlike other sleep aids, like benzodiazepines and z-drugs (think: Ambien and Lunesta), melatonin does not cause dependence or withdrawal symptoms. [R]

The most commonly reported melatonin side effect is daytime drowsiness. Other melatonin side effects include nausea, headache, and dizziness. [R]

If course, if you’re taking other medications, you should check with your physician before popping a melatonin. It has been known to interact with some antidepressants, blood pressure medications, sedatives, antibiotics, and antihistamines. [R]

Up to 240 mg and 500 mg oral and intravenous injections of melatonin taken acutely is not associated with any toxicological effects. [R]

A handful of large scale, 6-12 month studies, suggest continued administration of melatonin does not result in tolerance.

Examine.com

Conclusion


There’s great amount of evidence suggesting as well as proving the benefits of supplementing with melatonin whether for sleep purposes or overall general health.

Best practices when supplementing with melatonin for long-term benefits is to take a microdose of 300 mcg on daily basis before bedtime.

This microdose will serve a host of benefits most noteworthy of which is antioxidation and supporting mitochondria and antioxidation.

Many Nootropic focused companies are now aware of this and its benefits and so finally starting to see products in microdoses such as Nootropic Depot’s, which I have personally been using for a long time. Prior to which, I tried a couple of different products at the doses of 3 mg and it made me very heavy and groggy for a long time.


User Experience


First User Experience

A reddit user documented his experience after 2 years of using microdose of melatonin as recommended alongside magnesium, and his realization of how beneficial it had been working for him after he stopped.

I took Magnesium Citrate (200-400mg) and Melatonin (0.3mg) both every night for over 2 years and thought they didn’t make much difference in my sleep. It turned out to be very wrong – I now remember how poor my sleep was 3 years ago, before starting to take them. I wake up from the slightest noise and can’t go back to sleep for many hours afterwards – even if I wake up after only 4 hours, I would need to wait 3 hours before I fall asleep again, without Magnesium and Melatonin. This has been this way since I was a child. I find Melatonin is better for actually falling asleep initially, while Magnesium is better for maintaining quality sleep afterwards.

u/SuperAgonist on Nootropics subreddit

Second User Experience

I have learned the same lesson with melatonin in that less is more. I took 30 mg one evening and had very unsettling and vivid dreams. Not restful at all. I find 5 mg timed release works well. If you are interested in another natural sleep / relaxation aid, I have had success with Red Bali Kratom.

u/beesler70

Further & External Readings


Wikipedia

Examine

Melatonin for Sleep: How Effective Is It?

By Mary Squillace published at the Bulletproof Blog


Key Points:

  • Melatonin activates by light and dark.
  • Melatonin can be obtained from plants and used as a supplement.
  • When supplementing with melatonin, 0.3 mcg is the ideal dosage.



Wouldn’t it be great if you could pop a pill for better sleep? A pill that’s non-habit-forming, doesn’t require a prescription, and doesn’t make you do strange things like eat in your sleep? Well, maybe you can. While more satisfying zzz’s in pill form sounds too good to be true, there’s promising evidence that melatonin, the naturally occurring hormone in our bodies, can be harnessed as a supplement for better sleep.

What is Melatonin?

Melatonin is a multitasking hormone produced by the brain’s pinecone-shaped pineal gland. [1

Melatonin plays several roles in the body, including helping to regulate blood pressure, boost immune function, and manage cortisol levels. [2] [3]

But melatonin is probably best known for its soporific powers. Chief among its responsibilities is regulating the body’s circadian rhythm so it knows when to rest and when to wake up. That’s why melatonin is often referred to as the body’s sleep hormone.

How Does Melatonin Work?

Melatonin is controlled by light and darkness. When we’re awake and the sun’s out, we don’t produce any melatonin. But at night, the onset of darkness signals to our pineal gland to release melatonin into the bloodstream.

Your melatonin levels begin to increase about two hours before you go to bed, typically around 9 p.m., and peak about five hours later. As melatonin levels rise throughout our body — it’s found in a variety of our organs, including our eyes, bones, ovaries/testes and gut — our body knows it’s time to drift off to Slumber Town. [4] [5]

Supplementing with Melatonin

Humans aren’t the only organism that produces melatonin. It’s also found in meat (eggs and fish are particularly high in melatonin compared to other animal products) [6] as well as leaves and seeds, in which it protects plants from oxidative and environmental stress. As a result, many plants are a good source of melatonin. But melatonin is also extracted from these leaves and seeds and conveniently packed into melatonin supplements, for all of your sleep-hacking needs. [7]

Melatonin Pills

Melatonin supplements are used to treat a variety of sleep and circadian rhythm disorders, ranging from insomnia to jet lag. It also makes sleep more efficient and helps people fall asleep faster.

Melatonin supplements work the same as the melatonin we naturally produce works. Ingested melatonin simply adds to our melatonin levels, so people who are melatonin-deficient will likely experience the biggest benefit from supplementing with melatonin.

And according to research, there’s no need to worry that supplements will interfere with your body’s ability to produce melatonin on its own.

Melatonin Dosage

To get the most out of melatonin supplements, take them one to two hours before you hit the sack. [8] [9]

You’ll see melatonin recommended in a range of doses, starting at around 0.5 milligrams up to 10 milligrams for people with sleep disorders, with the most common dosage being around 3 milligrams. But even this is probably way more than you need. You’re better off basing your melatonin intake on increments that mirror how much melatonin our bodies produce at night. According to clinical studies, the optimal dose is 0.3 milligrams

Melatonin Side Effects

Overall, the side effects of melatonin are pretty toothless. Unlike other sleep aids, like benzodiazepines and z-drugs (think: Ambien and Lunesta), melatonin does not cause dependence or withdrawal symptoms. [11]

The most commonly reported melatonin side effect is daytime drowsiness. Other melatonin side effects include nausea, headache, and dizziness. [12]

If course, if you’re taking other medications, you should check with your physician before popping a melatonin. It has been known to interact with some antidepressants, blood pressure medications, sedatives, antibiotics, and antihistamines. [13]

Melatonin Overdose

Even though the overwhelming verdict is that melatonin is safe, you can have too much of a good thing. Overdosing on melatonin has not been shown to be fatal, but it can produce the aforementioned side effects, like dizziness and grogginess. In one known case, after taking 24 milligrams of melatonin, a man became lethargic and disoriented, but returned to normal and did not continue to have issues once he lowered his dosage.

In addition, large doses could potentially cause amenorrhea (skipped periods) in women, due to it suppressing gonadotropin-releasing hormones, but if you can easily remedy this side effect by simply stopping your melatonin supplements. [17]


Original article is found here

Choline: The Essential Vitamin Nutrient

Choline


Summary: Choline is an essential nutrient, and the precursor for neurotransmitter acetylcholine. Acetylcholine interacts directly with many functions such as the liver, brain, and nerve functions. It further extends to muscle control, energy level, as well as the metabolic process.




INTRODUCTION


Choline is an essential nutrient crucial for liver, brain, and nerve functions. It is also important for muscle motion and energy levels, as well as the metabolic process. It exists as phosphatidylcholine, a substance that comprises the structural part of the fat, hence discoverable in many types of foods. Naturally consisting of particular fats.

What is Choline?

Choline – (also known as choline bitartrate, and trimethylethanolamine) is an essential nutrient. It is crucial for liver, brain, and nerve function. As well as muscle motion, energy levels and the metabolic process. It exists as phosphatidylcholine, a substance that comprises the structural part of the fat, hence discoverable in many types of foods. Naturally consisting of particular fats.

Choline plays a major role in crucial procedures within the body. Mots of which perform multiple times a day. It is a water-soluble nutrient that belongs to other vitamins, such as folate and those in the B vitamin complex household. Much like B vitamins, choline plays a comparable function in regards to supporting energy and brain function, along with keeping the metabolic process active.

When Does Supplementing with Choline Becomes Necessary?

Choline assists in the procedure of methylation, which is utilized to produce DNA, for nerve signaling, and detoxing. It’s also essential for performance of a critical neurotransmitter: acetylcholine.
Acetylcholine also assists nerves in interaction as well as functioning as an anti-aging neurotransmitter. It carries out other fundamental functions. Neither a mineral nor a vitamin, Choline is rather an ‘essential nutrient’, required for many of the body’s functions. And particularly for brain function.
While at this time there isn’t a Recommended Daily Intake for Choline developed by the USDA, it’s crucial to prevent a choline-deficiency. Lack of which is explained further on in the article.

What is the Recommended Daily Intake of Choline?

The Recommended Daily Intake ranges between 280 to 550 mg depending on a number of factors as shown in the table below

Infants (under 1): 125 – 150 mg
Children (1-8): 150 – 250 mg
Kids (8-13): 250 – 375 mg
Girls (14 & over): 425–550 mg
Guys (14 & over): 500 – 550 mg
Pregnant: 450 – 550 mg
Breastfeeding: 500 – 550 mg

What Are The Best Sources of Choline?

Choline is naturally found in foods such as eggs, liver, beef, salmon, cauliflower, Brussel sprouts, and breast milk. Eggs are in some cases called “brain food” because they are known for providing high quantities of choline. The following is some of the foods high in choline, providing high levels of choline naturally, in addition to lots of other nutrients. All portions listed are based upon the advised quantity of 550 mg daily.


What foods are high in Choline?

    Beef Liver: 3 ounces: 283 mg (51% DV)
    Salmon: 1 filet: 242 mg (44% DV)
    Chickpeas: 1 cup raw: 198 mg (36% DV)
    Split Peas: 1 cup raw: 188 mg (34% DV)
    Navy Beans: 1 cup raw: 181 mg (32% DV)
    Eggs: 1 big egg: 147 mg (27% DV)
    Grass-Fed Beef: 3 ounces: 78 mg (14% DV)
    Turkey: 3 ounces: 57 mg (10% DV)
    Chicken Breast: 3 ounces: 50 mg (9% DV)
    Cauliflower: 1 cup raw: 47 mg (8% DV)
    Goat Milk: 1 cup: 39 mg (7% DV)
    Brussel Sprouts: 1 cup raw: 17 mg (3% DV)


BENEFITS & EFFECTS


Central Nervous System Support

Choline helps form tissue within the nervous system that plays a part in brain development and growth. It can improve signaling capacity of nerves, support structural integrity, and protect vital neuronal membranes. (R)

Neuroprotective Against Cognitive Degeneration

Another advantage of choline is its capability to keep your mind mentally sharp as you age.

Since it belongs to cell membranes and neurotransmitters that utilizes nerve signaling, choline also contributes to memory perseverance and preventing dementia, amnesia and other cognitive degeneration conditions.

As we age, our brain become less flexible. Choline does a crucial task here. It preserves brain flexibility by working to maintain levels of acetylcholine, which naturally decrease in the process of aging. Some studies suggest low levels of acetylcholine might cause a cognitive decline, that being inclusive of Alzheimer’s and dementia. (R)

Clients who develop Alzheimer’s often show a deficiency in acetylcholine levels. Some medications prescribed to manage Alzheimer’s do so by simulate choline’s impact of increasing this neurotransmitter’s levels. (R)

Choline Improves Cognitive Function, Attention and Mood

Acetylcholine is vital for brain function. Cognitive decline is often due to lack of sufficient acetylcholine levels within the brain. (R)

In 1391 individuals, greater choline consumption associated with better cognitive efficiency in spoken as well as visual memory. (R)

One research study reveals that subjects taking CDP-choline + caffeine drinks had measurable enhancement in cognitive capabilities (R)

Sixty healthy adult females aged 40– 60 who took CDP-choline for 28 days notice improving attention (R)

This elevating effect is explainable by the additional choline present, which increases attentiveness and promotes clarity. It’s also a link to its production of human growth hormone, which provides energizing, longevity effects. (R) In combination with other nootropics, it offers adequate choline to achieve optimal cognitive enhancement effects, and it prevents the minor headaches often associates use of Piracetam and pretty much all its derivatives.

Choline Improves Memory

The best recognition of it goes to its capacity in improving memory. This effect is mainly due to the increase of choline it makes available for conversion to acetylcholine, which is profoundly correlating with cognitive functions and the ability to create and revive memories. Studies confirm its efficacy as treatment for memory impairment due to aging; including Alzheimer’s and dementia.

It has further proven to be capable of recovering memory in volunteers following brief chemically-induced amnesia. (R), (R) ,(R)

Choline May Help Schizophrenia, Bipolar, and Autism

Schizophrenia and autism developed due to genetic predispositions may also be avoided by prenatal choline supplements (R)

In rats, it was found that prenatal choline supplements can help reduce the likelihood of at-risk subjects developing these disorders later on in life (R)

In a study performed on subjects with Schizophrenia, subjects taking CDP-choline showed improved cognition and working memory after treatment (R)

A few studies have shown that choline could help treat bipolar disorder and may be a useful complement to pharmaceutical interventions (R)

Increases Energy, Athletic Performance and Power Output, and Speeds up Recovery

Because it stimulates the production of human growth hormone (HGH), Alpha-GPC is valuable for individuals looking to perform better, increase lean muscle mass, feel peak energy during workouts and recover quickly afterward. A pilot study shows that 600 mg of Alpha-GPC taken 90 minutes before bench pressing increases power output by 14%. (R), (R), (R)


MECHANISM OF ACTION



Citicoline restores and repairs neuronal damage, increases dopamine levels in the central nervous system, as well as enhances production of neurotransmitter acetylcholine. Acetylcholine is especially important for those using racetams.

After ingestion, it breaks down into choline, and cytidine. After which it flows throughout the body and  easily crosses the blood-brain barrier. The cytidine then converts into uridine; a nucleotide base essential to neural membrane synthesis. The choline release is cholinergic, increasing levels of choline within the brain.

Choline is a precursor to acetylcholine and  vital to most cognitive functions. In particular to the ones relating to memory and learning.

Racetams are acetylcholine agonists compounds . They increase production and release of acetylcholine. When sufficient choline is available, it creates notable cognitive improvements such as memory improvement and heighten focus. Additionally, it prevents racetam headaches.

On Acetylcholine

It is a fundamental associate of many cognitive functions including memory formation, learning capacity, and attention. (R), (R), (R), (R). By stimulating the production of acetylcholine, it acts as a neuroprotectant; maintaining neuronal health and preventing potential damage.

On Dopamine

Oral ingestion of Alpha-GPC can also be dopaminergic, by increasing dopamine release during neuronal action potentials and possibly by stimulating the expression of receptors (R), (R). It also has involvement in increasing brain serotonin concentrations following oral administration (R).

DOSAGE AND HOW TO TAKE


Alpha-GPC digests and absorbs smoothly and is gentle on the stomach taken at the typical dose of 300mg. Although many nootropists tend to prefer a dose of 600mg, with a total daily intake ranging from 300 to 1200 mg, either at once or split into two doses (R).

Personally I find 300mg is effective enough especially because I almost always take it as part of a stack. Frequently with AniracetamPhenylpiracetam, Coluracetam, or Noopept. On the few occasions where I took it on its own, I still felt very at ease and eager to produce, learn, move.

As with any other nootropic, start with the lowest effective dose and build up gradually as desired.

SIDE EFFECTS


Some side effects rarely occur, such as headaches, fatigue, nervousness, nausea, diarrhea and gastrointestinal distress. It may rarely induce dizziness and low blood pressure in some individuals.

Personally never experienced any side effects from its use. But I’ve never taken more than 300mg in one dose (Alpha-GPC) and never more than 600mg in a 24-hours frame.

CONCLUSION


Choline is an excellent memory enhancing and focus amplifying nootropic that can be (and should be) added to almost any stack. Using it on its own is effective enough for that mild stimulation and to fire your focus. Then pair it with a racetam, and the effects of both are amplified to an amazing extent.

Furthermore, it provides neuroprotection. That is something anyone can benefit from due to many reasons. Such as environmental changes and the accumulation of oxidative stress in today’s world. It is very well tolerated and safe — there are no reports of serious adverse effects (on CDP-choline), and enlighten me if I’m wrong.

Moreover, its an approved medical treatment in Europe for a number of conditions relating to cognitive impairment (R), Ischemic Stroke (R), to mention a few.

Choline nootropics are affordable and easily accessible. Alpha-GPC is supposedly the most expensive out of the choline supplements. I’ve used both that and CDP-choline, both of which had identical effects. As a matter of fact, only now I started realizing that I might have been feeling citicoline more profoundly than I tend to feel Alpha-GPC. (I prefer it generally because it adds so much convenience to my life, when getting it along with a bunch of preformulated good mix in MindLab Pro.

It is worth buying for anyone looking after cognition boost and overall brain health. But especially worth it for those using multiple nootropics at a time, including racetams. Personally, at this point, I would not even bother taking a racetam if I don’t have a choline source to pair it with.

Alpha-GPC

Alpha-GPC


Summary: Alpha-GPC is a natural choline compound. It works on its own as a powerful memory booster. In combination with other nootropics, it works as a potentiator boosting cognitive capabilities. It’s also used as a milt stimulant to boost energy and power output when exercising. Furthermore, it promotes cell regeneration and acts as a neuroprotective agent, against cognitive decline.




Introduction


What is Alpha-GPC?

Alpha-GPC is a cholinergic compound naturally present in the body in small amounts and commercially manufactured as an extract of purified soy lecithin (R).

Although there are dietary resources of Alpha-GPC such as dairy products, organ meats, and wheat germ, concentrations achieved by dietary intake are lower than those obtainable by a supplement. It works rapidly and reliably by delivering necessary choline to the brain. (R)

It provides valuable nootropic qualities, including memory enhancement and protection against brain aging, attributing to longevity. Clinical trials covering thousands of participants confirm Alpha-GPC is a remarkable remedy for memory loss that accompanies Alzheimer’s disease (R), vascular dementia (R), and stroke (R).

Moreover, it provides neuroprotective, anti-aging benefits. Studies further suggest it is useful in the treatment of generalized anxiety (R), (R).

Another benefit is its ability to enhance cells membrane health and promote rapid recovery following physical activity. Studies indicate that it also acts as a dopaminergic, encouraging the release of dopamine, meaning it works as a potential treatment for neurodegenerative diseases such as Parkinson’s, in addition to being an overall mood enhancer (R), (R).

Potent Potentiator

However, many consider the real strengths of Alpha-GPC is the potentiating feature when in combination with other nootropics. The choline that it provides the brain with significantly magnify the cognitive enhancing effects of other nootropics, especially the racetams.

I’ve always liked both Alpha-GPC and Citicoline and appreciated their profound effect, until one day I added Aniracetam 750mg and it was as if I had just took a racetam for the first time. The effects of both nootropics synergize together so well, a year later both of them are on the front line among my nootropic stack.


Benefits & Effects


Alpha-GPC Improves Memory Formation and Recall

This effect is mainly due to the increase of choline it makes available for conversion to acetylcholine, which is profoundly correlating with cognitive functions and the ability to create and revive memories. Studies confirm it an effective treatment for memory impairment caused by age-related diseases, including Alzheimer’s and several forms of dementia. It has further proven to be capable of recovering memory in volunteers following brief chemically-induced amnesia. (R) (R,R)

Neuroprotection and Development of New Brain Cells

It protects and maintains overall brain health by promoting the development of new brain cells and enhancing the body’s capability to repair damaged cell membranes. This attribute is a significant longevity advantage. (R)

Alpha-GPC Increases Energy and Speeds up Recovery

Because it stimulates the production of human growth hormone (HGH), Alpha-GPC is valuable for individuals looking to perform better, increase lean muscle mass, feel peak energy during workouts and recover quickly afterward. A pilot study shows that 600 mg of Alpha-GPC taken 90 minutes before bench pressing increases power output by 14%. (R), (R), (R)

Increases Attention and Enhances Mood

Users report that using Alpha-GPC provides distinguished mental clarity while improving mood. This elevating effect is explained partially by the additional choline it presents, which increases attentiveness and promotes effortless clear-thinking. It’s also a link to its production of human growth hormone, which provides energizing, longevity effects. (R)

In combination with other nootropics, it offers adequate choline to achieve optimal cognitive enhancement effects, and it prevents the minor headaches often associating with racetams.


Mechanism of Action


Alpha-GPC is comprising of choline, glycerol, and phosphate and its classification is cholinergic. The mechanism of its action is examined with high understanding. However, the manner in which it affects some neuronal functions remains unclear. A water-soluble supplement that is fast-acting and highly bioavailable orally. It crosses the blood-brain barrier shortly after ingestion, and effects work within an hour. It metabolizes into a combination of choline and byproduct glycerophosphate. Additional choline forming by Alpha-GPC is the essence of its nootropic abilities.

On Acetylcholine

It is a fundamental associate of many cognitive functions including memory formation, learning capacity, and attention. (R), (R), (R), (R). By stimulating the production of acetylcholine, it acts as a neuroprotectant; maintaining neuronal health and preventing potential damage. 

On Dopamine

Oral ingestion of Alpha-GPC can also be dopaminergic, by increasing dopamine release during neuronal action potentials and possibly by stimulating the expression of receptors (R), (R). It also has involvement in increasing brain serotonin concentrations following oral administration (R). 


Dosage


How to take: Alpha-GPC digests and absorbs smoothly and is gentle on the stomach taken at the typical dose of 300mg. Although many nootropists tend to prefer a dose of 600mg, with a total daily intake ranging from 300 to 1200 mg, either at once or split into two doses (R).

Personally I find 300mg is effective enough especially because I almost always take it as part of a stack. If not Aniracetam then its Phenylpiracetam or Noopept. On the few occasions where I took it on its own, I still felt very at ease and eager to produce, learn, move.

As with any other nootropic, start with the lowest effective dose and build up gradually as desired.


Side Effects


Some side effects rarely occur, such as headaches, fatigue, nervousness, nausea, diarrhea and gastrointestinal distress. It may rarely induce dizziness and low blood pressure in some individuals.

Personally never experienced any side effects from its use. But I’ve never taken more than 300mg in one dose, and never more than 600mg in a 24-hours frame.

Alpha-GPC interacts adversely with scopolamine. Those using scopolamine are advised to avoid it.


User Experience


Here is 3 random alpha-gpc reddit community thoughts and experiences:

This might be considered a bit on the excessive side, but I’ve been taking 300mg of GPC daily for ~2.5 years. I’ve found it to be one of the most effective ways to treat the severe anxiety that I’ve suffered throughout most of my life. Initially, I periodically experienced the insomnia you mentioned, but that passed within a month or so. Every once in a while, I’ll go several days without taking the stuff. During those short, sporadic periods of “cycling off”, I’ve noticed that I feel significantly more “dull” and lethargic than I otherwise do, but that might just be placebo in action. I understand that such a lengthy use of an under-researched substance might be a bit careless. I suppose the greatest concern would likely be downregulation of choline receptors and reduced choline production, but I doubt that any studies of the effects of long-term heavy choline supplementation currently exist to prove that one way or another.

davinsburg

As the title says, Alpha GPC has next to eradicated my social anxiety. It’s incredible. Only downside is I’m having a hard time sleeping at night. Guess my question is, how long can I cycle this stuff safely?

Entropy-Reigns

So I used to take Alpha GPC, as well as a ton of other nootropics for a few months but recently took a couple months off. Anyway, I’ve been trying to get back into them so I took only Alpha GPC this morning. I already feel more at ease with everything. I font have much depression but its crazy how great I feel already. I happened to just see this and put it all together.

IamSlink

Conclusion


Alpha-GPC is a compound with decades of research, and its worldwide appreciation comes from the effects of memory enhancement. In addition to the dominant nootropic qualities, it’s also an excellent companion to racetams. Moreover, it stimulates the production of human growth hormone. This hormone production improves strength, reduces recovery time, and support the development of lean muscle mass. Therefore; it is an excellent nootropic for individuals who enjoy leading an active lifestyle.


Further Readings


Choline: The Essential Vitamin Nutrient

N-Acetyl Cysteine (NAC)

Agmatine


L-Theanine

L-Theanine


Summary: L-theanine is a natural amino acid, often called the “natural xanax”. It almost only exists in green tea leaves. It works brilliantly in unwinding and relaxing the body and brain without causing drowsiness, while reducing stress and increasing cognitive function. Due to not causing drowsiness, it is the perfect choice to combine with stimulants of any sort to take the edge off.




Introduction


What is L-Theanine?

L-theanine is a relaxing, non-sedating amino acid that is synergistic with stimulants to ‘take the edge off.’ Especially with coffee, it synergizes so well resulting in clean energy, furthermore preventing the nasty caffeine crash that many people experience after caffeine intake. It is also useful on its own, promoting relaxation and minimizing stress without causing drowsiness. A combination of L-theanine with caffeine at a 2:1 ratio is increasing in popularity as a remarkably synergetic combination that boosts cognition and attention.

It is an amino acid that naturally exists in green tea leaves as its main active ingredient, and that is the only source that provides it. It is famous for its fantastic nootropic features such as improving memory, expanding learning capacity, as well as providing a calming, zen-like effect.

L-Theanine, for the most part, is a relaxing but not sedating amino acid that is synergistic with stimulants such as caffeine as it can ‘take the edge off’. It is effective by itself in the standard supplemental dosages as well, and although it can be attained via a diet high in green tea ingestion that is the only dietary source of L-Theanine

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Benefits & Effects


L-Theanine Reduces Anxiety & Stress

A review by researchers of a small set of trials concluded that there are benefits of L-theanine in reducing acute stress and anxiety in people with stressful conditions. [R]

Oral intake of L-theanine in rats at feasible dosages reduces circulating biomarkers of stress with or without an actual stressor being present. Therefore, it reduces the adverse effects of stress such as memory impairment. Reductions of perceived stress reported in human subjects given oral theanine at the standard dosages. [R] [R] [R]

L-Theanine Improves Memory, Attention, and Cognition

In a 16-week long study on individuals with mild cognitive impairment, supplementing with l-theanine shows an improved delayed recognition as well as immediate recall comparing to those receiving a placebo during a mental exercise. Furthermore, attention span and alertness levels increased during the memory test. [R]

Theanine Enhances Sleep Quality

Theanine enhances sleep quality. In a study measuring sleep time with individuals supplementing with L-theanine, sleep time increases by 11 and up to 21%, therefore making it a valuable compound for achieving better nighttime sleep. (R)

Promotes Longevity and Increases Lifespan

In a study using the model organism C. elegans, L-theanine shows to promote longevity and promote healthy and increased lifespan. Due to those findings, the study suggests that the compound might have similar effects on mammals and humans (R)

Reduces Symptoms of Depression

L-Theanine intake for a period of eight weeks during an open-label study helped easing depressive symptoms, anxiety, sleep disturbance, as well as cognitive impairments in subject suffering major depressive disorder. (R)

Promotes Relaxation without causing Drowsiness

Theanine is proving to be a great agent in promoting relaxation without the accompanying effect of drowsiness. The company developing ‘suntheanine’, l-theanine supplement, won the 1998’s Food Ingredient Research Award for the outstanding research and findings. (R)

Significantly Reduces Symptoms of Schizophrenia

In persons diagnosed schizophrenia receiving 400mg L-theanine in addition to antipsychotic medication for eight weeks were able to reduce anxiety as well as psychopathology symptoms significantly. (R)

Enhances Blood Flow and Stimulates Nitric Oxide Production

Theanine appears to promote nitric oxide formation at relatively low concentrations and is likely practically relevant following oral ingestion. (R)

Reduces Negative Effects of Caffeine & Improves Cognitive Boosting Effects

Theanine and caffeine are typically found together in tea. A combination of caffeine and theanine together significantly improves alertness, reduce fatigue, and improves task-switching accuracy.

High dose caffeine (250 mg, equivalent to 2.5 cups of coffee) has some negative effects, such as jitters and increased blood pressure. Theanine was able to mitigate the increase in blood pressure.

L-Theanine decreases the negative and jittery effects of caffeine in rats.

However, human studies found that L-Theanine helps reduce caffeine jitters, although the changes were not significant.

L-Theanine changes the pharmacological profile of caffeine in humans, as the combination of caffeine and L-Theanine have somewhat different cognitive enhancement effects.

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Additional Benefits

Large studies in humans have not been undertaken; however, several smaller-scale studies (fewer than 100 participants) have shown increased alpha wave generation and lowered anxiety, along with benefits to sleep quality in people with ADHD. [R]


Mechanism of Action


L-theanine has a comparable chemical composition to glutamate, an amino acid that assists in the transmission of nerve impulses in the brain. Thereby, providing a host of benefits for the mind. It has a remarkable ability of crossing the blood-brain barrier, which means that it reaches the brain directly. Furthermore, it has positive effects on stress levels proving to increase both dopamine and serotonin levels in brain; which are two of the brain’s feel-good chemicals. Green tea is known to be effective at helping people relax due to the positive impact on those neurotransmitters.

Theanine is an antagonist of the NMDA receptors (albeit with fairly weak efficacy) and can inhibit synaptic release of glutamate via blocking the transporter competitively. Theanine may also reduce glutamate levels, but this is also a fairly weak mechanism requiring a high concentration of theanine

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Dosage


How to Take L-Theanine?

The effective l-theanine dose is 200mg.

For optimal nootropic results, take l-theanine with caffeine (coffee or supplement, whatever suits you) at a 2:1 ratio. As a stack, it would be:

  • L-Theanine 200mg
  • Caffeine 100mg

For those interested, you can actually purchase a supplement pre-made that has 200 mg Theanine & 100 mg Caffeine pressed into one capsule. I’ve personally used and still use Nootropic Depot’s.

Note: if you have anxiety or hypertension, you may want to skip caffeine entirely as it aggravates the symptoms.

Experimenting is the best way to find out how you react to it.


Side Effects


L-theanine is very safe as very high doses have failed to cause toxicity. However, that doesn’t mean you should go for such high dosage. (R)

L-theanine is exceptionally reliable. Furthermore, it is classified Generally Recognized as Safe by the Fraud and Deception FDA in the US.


Conclusion


L-Theanine is a natural safe amino acid offering many benefits. It’s a popular choice for individuals wanting a simple and effective way to boost their mental performance. Alone, with caffeine, or even with an advanced nootropic stack; L-theanine is worth trying.


Further Reading



Citicoline (CDP-choline)

Citicoline


Summary: Citicoline or CDP-choline is a safe, potent, and extremely well-tolerated nootropic. Enhances memory and protects the brain on its own. In combination with other supplements, it works as a powerful potentiator, especially racetams.




Introduction


What is Citicoline?

CDP Choline (also known as Citicoline or Cytidine diphosphocholine) is a potent nootropic and a highly bioavailable choline source that is praised for its ability to cross the blood-brain barrier quickly, improving memory and protecting the brain against memory injury. Furthermore; it heightens focus, increases mental energy, and provides thought clarity.

Recent studies suggest its usefulness in the treatment of many medical problems from head injuries to stroke, and neurodegenerative diseases to glaucoma, ADHD, and even cocaine dependency.

Citicoline, also known as cytidine diphosphate-choline or cytidine 5′-diphosphocholine is an intermediate in the generation of phosphatidylcholine from choline, a common biochemical process in cell membranes. Citicoline is naturally occurring in the cells of human and animal tissue, in particular the organs.

Wikipedia

For nootropists – (new term just coined here!), the most exciting part of supplementing with a choline source is its ability to amplify and enhance the effects of other nootropics. It works synergistically with racetams nootropics such as Aniracetam, Sunifiram, Fasoracetam, potentiating the effects of memory boosting such as piracetam and pramiracetam while preventing the minor headaches that often come along with racetam use.

CDP Choline, along with Alpha-GPC (and Centrophenoxine) are the most useful choline-source supplements available.


Benefits & Effects


CDP-choline Improves Memory

CDP Choline is popular for its effect on improving memory and preventing memory loss. It associates with anti-aging and longevity, as well as having the possibility of being an add-on to the treatment of Alzheimer’s disease. (R)

Increases Mental Stamina and Works as Neuroprotectant

Clinical trials show CDP-Choline to affect mental energy positively, increasing frontal lobe bioenergetics and mitigating the cognitive declines associated with aging. Thereby becoming a neuroprotective agent. (R)

Heightens Focus and Concentration

CDP-choline increases the ability to concentrate for extended periods of time and minimizes distraction, which makes it essential for studying, learning new information, or completing enduring and mentally demanding tasks. This seems to be true even in severe cases of conditions like brain injuries and Alzheimer’s disease. (R)

To benefit from the focus, concentration, and enduring prologing tasks, you could pair it with an amino acid nootropic like N-Acetyl L-Tyrosine. The senergy of the two will improve the ability to concentrate to a new level.

This is especially true in subjects with ADHD (like myself). I’ve found including NALT and Citicoline together in my moring stack to be one of the most beneficial for pulling through in my corporate office job.

Potentiating the Effects of other Nootropics

Many Nootropists consider CDP-choline a must-have in any stack. Especially those including racetams. It works particularly well with racetams, amplifying their effects and preventing the associating headache due to the utilization of acetylcholine within the brain.

Furthermore, it seems to delay the onset of cognitive decline in Alzheimer’s disease when used in combination with piracetam according to a study by the Biomedical Research Center in Spain. (R)


Mechanism of Action


CDP-choline is a “slightly” stimulating nootropic – depending on whom you ask. Many people myself included find it to be more than “slightly” stimulating. However, I take it along with a couple other supplements so my experience shouldn’t be as credible.

Citicoline restores and repairs neuronal damage, increases the dopamine levels in the central nervous system, and furthermore, enhances the production of the neurotransmitter acetylcholine. Acetylcholine is especially important for those using racetam nootropics.

Post consumption, CDP-choline breaks down into choline, and cytidine. After which it flows throughout the body and  easily crosses the blood-brain barrier.

The cytidine then converts into uridine, a nucleotide base essential to neural membrane synthesis. The choline release is cholinergic, increasing levels of choline within the brain.

Choline is a precursor to acetylcholine,  vital to most cognitive functions — particularly those relating to memory and learning capacity.

Racetams are acetylcholine agonists compounds that increase the production and release of acetylcholine. When sufficient choline is available, it creates notable cognitive improvements such as memory improvement and heighten focus, thought clarity, and faster recall. Additionally, it prevents racetam headaches.


Dosage


How To Take Citicoline?

How to take: the typical dose is usually ranging from 250mg being the lowest effective, to up to 1000 mg while keeping an  8 to 12-hour time intervals.

I find 250mg effective enough to potentiate racetam effects. I’ve also taken 500mg at other times but that was in a preformulated nootropic, which is  MindLab Pro.


Side Effects


Rare occurrences are:

  • Indigestion
  • Headache
  • Insomnia – this is applicable if taken late in the evening
  • Diarrhea

These are the reported possible (although rare) side effects.

I have been using both Citicoline and Alpha-GPC for over a year or two now and never experienced any of those.


Conclusion


CDP-choline is an excellent memory enhancing and focus amplifying nootropic that can be (and should be) added to almost any stack.

Using it on its own is effective enough for that mild stimulation and to fire your focus. Then pair it with a racetam, and the effects of both are amplified to an amazing extent.

Furthermore, it provides neuroprotection. That is something anyone living today can benefit from due to so many reasons such as environmental changes and the accumulation of oxidative stress in today’s world.

It is very well tolerated and safe — there are no reports of serious adverse effects on CDP-choline, and enlighten me if I’m wrong.

Moreover, it is an approved medical treatment in Europe for a number of conditions such as cognitive impairment (R) as well as Ischemic Stroke (R), to mention a few.

It is affordable and easily accessible. You can get it for around $15 for a 60 capsules of 300mg, and that is the first result I looked at for the sake of elaborating. I tend to use Alpha-GPC more often which is slightly more expensive, but no more than $10 more than citicoline.

It is worth buying for anyone looking after cognition boost and overall brain health. But especially worth it for those using multiple nootropics at a time, including racetams.

I mean at this point, I would not even bother taking any racetam if I don’t have a choline source to pair it with.


User Experience


This question was asked on Reddit’s Nootropic geeks about users experiences on Citicoline, which had 19 answers. I will share a few from both positive and negative to not seem biased.

The question asked was this:

“Has anyone had a boost in long term memory using cdp choline?”

and 4 out of the 19 answered the following:

I have but I take 1 gram daily. There’s tons of studies on it and older adults on helping memory so it does work.

peptidehunter

I can’t say whether it was the choline or not since I use it with noopept but I will say both have helped with long term memory.

cryogen

The real answer is no, CDP Choline is not profound enough to warrant noticeable increases in memory. Slightly, perhaps. Significant? No chance.

then00breaper

Due to infamous way of reddit answers end up leading to the most random off topic discussions, I had to add my answer as the 4th to have a total of 4 testimonials here.


Personal Experience


yes yes yes and a 100 yes. i’ve been using both alpha gpc and citicoline/cdp for about 2 years and has seem tremendous positive impact both onset and long-term.

Moe

So there you have it all. Now its on you to do the rest of the research, if necessary, and decide for yourself. Good luck and let me know how you respond to it! 


Further Readings


Choline: The Essential Vitamin Nutrient