Picamilon

Key Takeaways

1. Picamilon is a combination of GABA and niacin that increases GABA levels in the brain by crossing the blood-brain barrier.
2. It is preferred over standalone GABA and niacin due to the essential nature of the bonded molecule for its effects.
3. Developed in Russia, Picamilon has been used as a pharmaceutical to treat brain-related disorders.
4. The benefits of Picamilon include mood balancing, improved cerebral circulation, and normalization of neurotransmitters like serotonin and dopamine.
5. Picamilon enhances cognition, cerebral blood flow, and dopamine uptake, providing a calming focus without sedative effects, and boosts brain cell mitochondria function when taken in recommended dosages of up to 50-100 mg daily.

Picamilon (nicotinyl-y-aminobutyric acid, or N-nicotinoyl-GABA) is a combination of the inhibitory neurotransmitter gamma aminobutyric acid (GABA) with nicotinic acid (Vitamin B₃ or niacin). The addition of niacin allows GABA to cross the blood-brain barrier (BBB).

Neurohackers prefer either Picamilon or Phenibut when the goal is to raise GABA levels in the brain because GABA alone cannot cross the BBB. And note that taking GABA and niacin as a stack will not produce the same effect as Picamilon. GABA is bonded with niacin to produce Picamilon and it’s this molecule that does its magic in the brain.

Picamilon was developed in Russia in 1969 by the All-Union Research Institute. And it has been used since 1986 as a pharmaceutical in Russia to treat attention, memory, and learning problems, and for treatment of loss of brain blood circulation, brain trauma, chronic alcoholism and other disorders.

The company’s promotional material states, “The important property of Picamilon is the ability to quickly restore mental and physical fitness for work, which was lost through overstress”.

Once Picamilon crosses the blood-brain barrier it hydrolyzes into GABA and niacin. GABA activates GABA receptors producing an anxiolytic response. And niacin acts as a vasodilator relaxing constricted blood vessels and increasing cerebral blood flow.

Picamilon helps:

• Balance mood. Picamilon has an inhibitory effect on overly stimulated neurons because it raises GABA levels in your brain. Low GABA levels lead to anxiety, depression and insomnia. GABA helps restore that balance. Promoting a more positive mood which improves focus and relaxation.[i]
• Cerebral Circulation. Picamilon is unique among GABA boosters because it can boost cerebral circulation as well.[ii] It increases cerebrovascular activity better than Piracetam and Vinpocetine. The nicotinic acid (niacin) in Picamilon boosts blood flow, enhances cell metabolism and oxygen supply in the brain. Resulting in an improvement in short-term and long-term memory.
• Neurotransmitters. Picamilon has been shown to normalize serotonin and dopamine content, and dopamine uptake in the brain. Dopamine aids in memory formation, attention, focus, and cognition.

Overview

Picamilon (nicotinyl-y-aminobutyric acid, or N-nicotinoyl-GABA) is a derivative of the inhibitory neurotransmitter GABA and nicotinic acid (niacin or Vitamin B₃).

Russian scientists conducted a lot of research into GABA and cognitive health in the 1960’s and 70’s. The nootropics community has benefited from this research. It was the Belgians who started the development of the racetam-family of nootropics. And not too long afterwards, Russian scientists continued the research on GABA-derived compounds and gave us Phenibut and Picamilon.

GABA’s role is to keep glutamate, the primary excitatory transmitter, from overwhelming your brain. Too much glutamate can cause a seizure, and too little GABA can put you in a coma. A healthy brain maintains a critical balance of GABA and glutamate.

GABA acts like a “brake” on neuron circuits during stress. Low GABA levels can result in anxiety, insomnia, poor mood and restlessness.

Clinical studies show that boosting GABA with a supplement like Picamilon relieves anxiety, stress, and boosts the production of alpha brain waves.[iii] If GABA is optimized in your brain you’ll feel focused, relaxed and stress-free.

But the big challenge for cognitive health is trying to boost GABA levels in the brain. GABA cannot cross the blood-brain barrier on its own. It needs help to carry it across this barrier.

Including Vitamin B₃ (niacin) in the Picamilon formula helps GABA to cross the blood-brain barrier. And the reason why some neurohackers prefer Picamilon when the goal is to raise GABA levels in the brain.

Picamilon is unique among GABA boosters because it can boost cerebral circulation as well.[iv] It increases cerebrovascular activity better than Piracetam and Vinpocetine. It’s even better at boosting blood flow than prescription vasodilating agents like cinnarizine, papaverine, and xanthinol niacinate.

So when using Picamilon to boost GABA, you enhance cerebral circulation, and lower blood pressure. GABA even stimulates the pituitary gland to secrete Human Growth Hormone. And helps produce endorphins that make you feel good after a workout or sex.

As a nootropic, when you use Picamilon to normalize GABA levels you’ll improve blood flow to and within your brain. And you’ll experience a reduction in anxiety, insomnia, nervousness, restlessness and stress.

Picamilon exhibits the properties of a tranquilizer with a stimulating component. But unlike tranquilizer drugs, Picamilon does not induce muscle relaxation, drowsiness or lethargy.

How does Picamilon work in the Brain?

Picamilon helps brain health and function in several ways. But two in particular stand out.

1. Picamilon boosts cognition. Picamilon is a derivative of GABA and niacin. And easily crosses the blood-brain barrier. GABA on its own cannot cross this barrier unless paired with a dedicated carrier.[v] When niacin is bonded to GABA the molecule easily enters the brain.

Once in the brain, Picamilon separates back into niacin and GABA. GABA works by preventing neural signaling associated with anxiety from reaching other neurons. It does this by attaching to the receptors that would otherwise excite those neurons. Over-stimulating neurons in certain areas of your brain is what causes anxiety-related symptoms.

Studies have shown this unique combination of niacin and GABA affect the regulation of neurotransmitters in the brain. Picamilon was shown in one study on Parkinson’s disease to normalize serotonin and dopamine content, and dopamine uptake in the brain.[vi]

2. Picamilon improves cerebral blood flow. Picamilon is more effective than Piracetam and Vinpocetine in improving blood flow to cerebral vessels in the brain. It easily crosses the blood-brain barrier to protect neurons against the effects of diminished oxygen flow. Improving cognitive function.

Picamilon separates into niacin and GABA once it crosses the blood-brain barrier. Niacin acts as a vasodilator relaxing blood vessels and allowing the freer flow of blood in the brain.

Picamilon is often prescribed in Russia for treatment of migraine headaches. A study published in Nutrition Journal reviewed clinical trials from 1990 – 2004 looking at studies using niacin to treat migraines, and other tension-type headaches.

The conclusion from this review showed niacin’s effectiveness for its vasodilatory properties in increasing cerebral blood flow. And its ability to improve mitochondrial energy metabolism.[vii] The result is fewer migraines and less headaches when using a nootropic containing niacin.

How things go bad

Low levels of GABA and poor cerebral circulation are associated with a variety of health problems.

↑ Anxiety[viii], panic attacks, stress and insomnia

↑ Muscle spasms, hypertension, convulsion, Tourette’s Syndrome and epilepsy

↓ Neurotransmitters decline

↓ ATP energy production levels decline within mitochondria in brain cells

When your neurotransmitters, including GABA, are in balance, you feel motivated, productive and energetic. And you feel calm and relaxed during downtime.

When GABA levels are low you feel filled with dread, you’re constantly worried, you have racing thoughts, and you’re frequently late and disorganized.[ix]

Many people in this GABA-slump resort to high carbohydrate foods, and drugs or alcohol to relax.

Picamilon benefits

Picamilon is an analogue of GABA and nicotinic acid (Vitamin B₃ or niacin). The addition of niacin allows GABA to cross the blood-brain barrier (BBB).

We need adequate GABA levels in our brain because it’s an inhibitory neurotransmitter. When we raise GABA levels by supplementing with Picamilon, we help keep glutamate in check.

Glutamate is your body’s most abundant excitatory neurotransmitter. Which is needed for attention, mental energy, learning and memory, and staying awake.

So GABA is calming and glutamate is stimulating. And they must be in balance with each other for optimal cognitive health.

An imbalance of these two neurotransmitters can cause fibromyalgia, chronic fatigue syndrome, poor memory and cognition, anxiety and depression.

But when these two neurotransmitters work together efficiently, you feel relaxed with no stress or feelings of anxiety. And you get a more restful night’s sleep.

The addition of nicotinic acid in the Picamilon formula helps improve cognition even more. One study with 96 healthy volunteers was done to determine the effects on memory with nicotinic acid. The study found that nicotinic acid (niacin) enhanced cell metabolism and oxygen supply in the brain. Resulting in an improvement in short-term and long-term memory.[x]

Adding Picamilon to your nootropic stack can help bring GABA and glutamate back into balance.

How does Picamilon feel?

When you balance GABA levels in your brain, you feel relaxed and calm. But many neurohackers who try using GABA as a supplement don’t feel the effects. Because the GABA molecule is too large to easily cross the blood-brain barrier.[xi]

Note: If you do feel the calming effects of supplementing with GABA within a ½ hour of taking it, it may mean you have a “leaky” blood-brain barrier. Not a good thing.[xii]

Because if GABA can get through, all kinds of nasty stuff can get through too. Including toxins, undigested food particles and anything else in your blood stream that shouldn’t be in your brain.

Learn how to fix a “leaky” blood-brain barrier here >How to Heal a Leaky Blood-Brain Barrier .

But here were talking about increasing our GABA levels using Picamilon. Neurohackers report that adding Picamilon to their stack relieves anxiety “better than Xanax”. There is less stress and they feel more relaxed.

Picamilon also offers a stimulant effect providing mental clarity, dreams can be vivid, and it’s not sedating like Phenibut.

Social functions could get some help with Picamilon. You could feel less inhibited, speak freely and feel more confident. Picamilon generates a calm focus without making you drowsy.

Some neurohackers maintain that the ‘magic’ with Picamilon is in the nicotinic acid. And I’d have to agree with this observation. It’s what provides the stimulant-effect and gives you an energized type of calmness.

The cognitive benefits of niacin are considerably understated in the nootropics community. Just check out the research and studies in my NADH article for more on the magic of niacin.

Picamilon Clinical Research

Nearly all the research with Picamilon has taken place in Russia. It’s published in Russian journals in Russian. Most of these trials are not indexed in international or US medical databases.

I won’t get into the politics of this type of behavior here on Nootropics Expert. I’m here to educate and collate information for you on nootropics to help cognitive health.

The sources I have been able to find shows Picamilon extensively studied in animals and humans. And has been shown to act like a tranquilizer without the sedative effects of muscle relaxation, drowsiness or lethargy.

The studies show Picamilon decreases anxiety, fear, irritability and symptoms of emotional stress. It inhibits aggression, and restores physical working capacity after stressful work.

Picamilon has been proven to prevent forgetfulness, enhance memory, recall and improve mood. It decreases headaches, dizziness and tinnitus. It increases mental and motor activity in patients with anxiety and depression.

Picamilon has been shown to prevent or suppress diabetic neuropathy[xiii], and alleviate the effects of alcohol withdrawal symptoms. It helps glaucoma, retinal and optic nerve damage[xiv]. And helps those with neurologically-based urinary problems.

Here I talk about how Picamilon, nicotinic acid and GABA can affect your cognition and overall health. This research supports the idea of using Picamilon to raise GABA and niacin levels. And the cognitive benefits can have a profound effect on your quality of life.

Picamilon increases dopamine uptake

Reports by neurohackers repeatedly show that Picamilon provides a ‘calm focus’ without making you drowsy. And this study done in the Ukraine gives us a clue on how this works.

This study was done with Parkinson’s patients. It’s well know that serotonin and dopamine content and dopamine uptake by neurons in Parkinson’s Disease is decreased.

This research found that Picamilon normalized dopamine uptake in Parkinsonism. And that Picamilon is “involved in the regulation of brain neurotransmission under experimental parkinsonism and can be useful in treatment of Parkinson’s disease”.[xv]

Picamilon boosts brain cell mitochondria function

We know from our research on Nootropics Expert that NADH boosts ATP energy production within brain cell mitochondria. And this “energizing” effect that’s often spoken of when using Picamilon comes at least in part from its niacin component.

This study done on one-month old rats looked at trauma of the brain. The researchers studied oxidative damage done on brain mitochondria 1, 4, 7 days and 4 weeks after the trauma.

The young rats were given several different nootropics to see the effect on the rat’s mitochondria. And they concluded that Picamilon had a protective effect on the function of brain mitochondria during the trauma.[xvi]

Picamilon increases blood supply, oxygen saturation and blood circulation in the brain.[xvii] This boost in blood flow[xviii] brings the nutrients and oxygen needed to produce ATP within brain cell mitochondria.

Recommended Picamilon Dosage

The recommended daily starting dosage of Picamilon for anxiety is 50 mg 2 or 3 times per day. If you’re looking for a stimulatory effect you can safely increase your dose to 100 mg 2 or 3 times daily.

Picamilon Side Effects

Picamilon is considered safe when taken in normal recommended doses.

Picamilon has not been shown in clinical trials to produce any allergic or toxic effects. The only side effects noted were headache, dizziness and nausea. And nearly always when taken above recommended doses.

At higher doses Picamilon can lower blood pressure. So if you are already on blood lowering medication, or have an issue with low blood pressure, you should not use Picamilon.

Where to buy Picamilon

Picamilon as a nootropic supplement is available in powder, tablet and capsule form.  I recommend Cosmic Nootropic – Picamilon tablets or Science-bio – Picamilon who sell Picamilon as a “research” compound. It is sold to be used in an academic laboratory research setting. They go on to state “nothing we sell is intended for nor is it manufactured for diagnostic or therapeutic purposes in humans.” Which they must say if they want to keep selling Picamilon and not get in trouble with the “authorities”.

If you choose to buy bulk Picamilon powder from a vendor, make sure you ask for a genuine Certificate of Analysis to verify its authenticity as you cannot always trust dietary supplements sold from just anyone .