Phenylethylamine – For millennia, people have been trying to find the means to help them feel happier. In this laborious struggle, one of the main weapons was herbs and food. Green tea, coffee, cocoa and herbs are adaptogens and have always been relevant. While some natural tonics stimulate and energize us, others make us feel happier. And the chocolate? Oh yeah! Chocolate definitely makes us feel happy and in the following lines we will meet the main culprit for this.
Table of Contents
What is phenylethylamine?
Phenylethylamine or beta-phenylethylamine – this is a type of small monoamine, which chemically belongs to the group of alkaloids. Phenylethylamine is also known as PEA and is the basis of a whole class of substances that are known for their psychoactive and stimulating properties. In the human body, PEA acts primarily as a neuromodulator and neurotransmitter, and its secondary functions are related to metabolism. PEA itself is an amine whose mechanism differs drastically from biogenic amines such as serotonin and dopamine.
The structure of phenylethylamine is similar to that of tyramine, chordenine and octopamine. Phenylethylamine is easily soluble in aqueous media, but does not dissolve very easily in fat, which means that intake on an empty stomach with a glass of water will lead to easier absorption when taken orally, compared to food rich in fat. .
Sources of phenylethylamine
PEA is a natural alkaloid and is found in many plant and animal sources. The main mechanism of phenylethylamine formation is related to the fermentation and functions of different classes of bacteria such as lactobacillus, clostridium, pseudomonas and enterobacteriaceae. This is the reason why PEA is found in Japanese NATO grains, where fermenting bacteria predominate. PEA is also found in various green, blue and brown algae, as well as in eggs. Chocolate is perhaps the best known source of phenylethylamine, which is formed by the breakdown of the amino acid L-phenylalanine by heat treatment.
It is L-phenylalanine that is the main dietary precursor of beta-phenylethylamine, but PEA is not the main metabolic product of the amino acid because most of it is converted to L-tyrosine. A specific methylated form of PEA, known as beta-methylphenethylamine, has been found in the leaves of the acacia berlandieri plant, which differs from amphetamine only in the location of the carbon molecule.
How does phenylethylamine work?
Beta-phenylethylamine can be synthesized in the human body, the main source being the amino acid L-phenylalanine. The process is expressed in decarboxylation, the mediator being the aromatic amino acid decarboxylase (AADC). The human body contains specific intracellular receptors, known as TAARs, that respond to neurotransmitters in the human body that are too small to have their own receptors.
This group of neurotransmitters includes PEA, as well as tyramine, tryptamine, octopamine and 3-iodothyronamine. The response of TAARs to unpopular neurotransmitters affects the signaling of catecholamines, which include dopamine, adrenaline and noradrenaline. PEA is a potent agonist of two TAARs receptors – TA1 and TA2 – and its activity exceeds that of all other amines. It is this effect on these receptors that explains the positive effect of PEA on dopamine, adrenaline and cAMP levels.
Although phenylethylamine is a natural amine contained in the mammalian brain, it is a secondary neurotransmitter because its content is only 1-5% of the total catecholamines. The main reason is the limited synthesis and the fast metabolism. When PEA is injected into the blood, the amine easily crosses the blood-brain barrier and nearly 83% is concentrated in the brain, with a half-life of only half a minute due to the rapid metabolism by the enzymes monoamine oxidase (MAO).
At this stage, there are insufficient observations on the metabolism of PEA when taken orally by humans, but it is assumed that its metabolism will again be “lightning fast”. A study in dogs found that the half-life of phenylethylamine when taken orally was between 6 and 16 minutes, with a higher dose leading to a longer metabolic time. Phenylethylamine has been found to successfully use the major dopamine transporter to increase its own levels as well as dopamine levels.
Proven and potential benefits in humans
- Octopamine, tyramine and phenylethylamine, as amines of one class, can suppress prolactin levels. The effectiveness of prolactin suppression depends on the dose, the mechanism being explained by the ability of PEA to induce the release of dopamine, which stimulates its own receptors to suppress the hormone prolactin;
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Even small doses of PEA can act as an immunosuppressant. Phenylethylamine can activate leukocytes in the blood by stimulating TAAR1 and TAAR2 receptors, acting on both cell types – T cells and B cells. Other biogenic amines have similar functions, but their degree of activation is relatively low. The synthesis of small doses by the body leads to increased migration of leukocytes, while when taking PEA as a dietary supplement, a stronger effect is assumed;
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A study on exercisers linked the role of phenylethylamine to the antidepressant properties of exercise. It has been found that with a 30-minute workout that uses 70% of the maximum heart rate, the body releases more phenylacetic acid. Eating foods rich in PEA also improves depression. The possible mechanism is related to the neuromodulatory properties of the alkaloid;
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PEA has been used successfully in the treatment of addictions to stimulants and alcohol. Phenylethylamine is known to be an agonist of the dopamine and serotonin receptors. Namely, by acting on both receptors, PEA suppresses dependencies without creating dependence on dopamine, what danger do pure dopamine receptor agonists pose;
- PEA is a potent dopamine receptor agonist, with comparable activity to dopamine, but the exposure time is too short due to the rapid metabolism of the alkaloid. The activity of phenylethylamine is explained by the fact that the chemical itself is synthesized around dopamine receptors. It is interesting to note that PEA caused a strong increase in dopamine, but at the same time regulated the binding of dopamine in neurons;
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PEA is a known serotonin receptor agonist, but its ability to increase serotonin is nearly 100 times weaker than dopamine secretion;
- Phenylethylamine is a known antagonist of alpha and beta adrenogenic receptors. PEA acts as an alpha-blocker on receptors in blood vessels and muscle fibers, calming blood vessels, lowering blood pressure and improving blood supply. In the brain and heart, however, phenylethylamine acts as a beta-blocker and the result is a calming of the heart rhythm and dilation of the blood vessels;
Proven and potential benefits in animals
- Although no serious human observations have been performed, in vitro tests and animal studies have established a link between phenylethylamine levels and brain suppression in Parkinson’s disease. Phenylethylamine itself is synthesized and functions in the brain region of substantia nigra, whose function is severely affected by Parkinson’s disease. The disease itself appears to reduce the concentration of PEA in the blood and cerebrospinal fluid, and additional phenylethylamine intake may partially improve the condition;
- When injected into E. coli-infected meat, PEA drastically reduces the activity of the bacterium and the number of cells, and when the meat is stored for one week at a temperature of 10 ° C, almost 90% of the bacteria are eliminated. It is accepted, although there are no serious studies, that PEA may exhibit antibacterial properties in the human body;
- The properties of PEA to act on serotonin and dopamine receptors have also been demonstrated in animals, with rats being the most commonly used in the tests;
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When the effect of amphetamine and phenylethylamine on the hypothalamus of rats was observed, it was found that there are certain receptors in the hypothalamus that respond to the anorexic activity of both substances. This partly explains PEA’s ability to suppress appetite;
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When phenylethylamine was administered to rats, an increase in motor activity was observed in parallel with an increase in PEA concentrations in the brain.
Recommended dose
Science has not established an exact daily dose. The practice recommends taking between 300 and 1000 mg daily. It is not recommended to take 1000 mg at a time, a better option is to distribute the dose up to 2-3 doses per day. If side effects are found, it is good to limit the intake to the minimum dose of 300 mg per day.
Side Effects
Phenylethylamine can rarely have side effects such as nausea, constipation, headache. The most common side effects, very often caused by a high dose, are: palpitations, insomnia, agitation, nervousness and severe headache. PEA is not recommended for schizophrenia, hyperactivity and migraine because it can worsen your health.
The metabolism of phenylethylamine is directly related to the metabolism of its main precursor – L-phenylalanine. Deviations in the enzymes that process L-phenylalanine can lead to problems such as hyperphenylalaninemia or phenylketonuria. People with these diseases are generally more sensitive to all biogenic amines, including phenylethylamine, and it is advisable to avoid taking PEA as a dietary supplement.
With what to (not) combine phenylethylamine?
Phenylethylamine as a dietary supplement is nootropic and can be combined with other similar substances or stimulants for more focus, mood, tone and energy. It is often recommended to combine PEA with yohimbine, theobromine, taurine, tyrosine, n-acetyl tyrosine, caffeine or adaptogenic herbs such as rhodiola rosea and schisandra. PEA can be used as a fat burner, with combinations with classic thermogenics such as green tea, synephrine and yohimbine being suitable.
The combination of phenylethylamine with MAO inhibitors is not recommended. It has also been found that taking sources of phenylethylamine and tyramine (chocolate and cheese) together with MAO inhibitors leads to a sharp rise in blood pressure. Phenylethylamine has a strong synergism with amphetamine. Concomitant use of both substances is not recommended because PEA dramatically enhances the action of amphetamine.
Where to find phenylethylamine?
PEA is a food supplement of medium popularity. As a stand-alone product, it is rarely found and is usually available in the form of pure powder or capsules with a concentration of up to 500 mg per capsule. More often PEA is part of complex formulas, these are mainly thermogenic fat burners or nitrogen boosters. Popular phenylethylamine fat burners are Pure Nutrition Black Fire, Universal Animal Cuts and MAN Scorch, and popular nitrogen boosters are Pure Nutrition Black Jack and Universal Animal Rage XL. In the food industry, PEA is used as a compound with hydrochloric acid.
