Potential and Dangers of Phenethylamine
Phenethylamine is a trace amine found in tiny amounts in the brain that increases the release of the “happy hormones” dopamine and serotonin. Supplementing phenethylamine may boost mood and promote weight loss, as well as increase cognitive function. In addition, phenethylamine is the building block for several mood-altering drugs such as MDMA (ecstasy). Read this post to find out more about the positive role of phenethylamine in the brain, how you can increase your phenethylamine levels naturally, and the potential health effects, risks, and side effects of taking phenethylamine and its derivatives.
Disclaimer: By writing this post, we are not recommending this drug. Some of our readers who were already taking the drug requested that we commission a post on it, and we are simply providing information that is available in the clinical and scientific literature.
What Is Phenethylamine?
Phenethylamine (also known as PEA, β-phenylethylamine, β-phenethylamine, 2-phenylethane-1-amine, and Benzeneethanamine) is a nootropic or trace amine naturally found in the central nervous system and brain of humans and other mammals. The term “trace amine” refers to the fact that it is found at much lower concentrations than other amines [R, R].
Phenethylamine is metabolized by the enzymes monoamine oxidase B (MAO-B) and aldehyde dehydrogenase to phenylacetic acid, which is then excreted in the urine [R].
Phenethylamine Mechanism of Action
- Phenethylamine activates a receptor (TAAR-1) in the brain to trigger the release of neurotransmitters. Neurotransmitters send chemical signals to different targets in the body causing various responses e.g., happy, sad, scared, awake [R, R].
- By activating TAAR-1, phenethylamine increases the release of serotonin, epinephrine (adrenaline), dopamine, and norepinephrine (noradrenaline) from neurons, which are extremely important to proper mood, cognitive function, and mental well-being [R, R, R].
- Phenethylamine also prevents these same neurotransmitters from taken back up (through reuptake transporters) by neurons, meaning they stay in the spaces between neurons (synapses) longer and they have more time to exert their effects [R].
Potential Uses of Phenethylamine
1) May Reduce Depression and Improve Mood
Phenethylamine increases dopamine and serotonin in the brain, which may promote a positive mood and lead to a greater sense of well-being [R].
Studies have shown both phenethylamine and phenylacetic acid, the byproduct of phenethylamine, are decreased in depressed patients [R].
In one study (prospective cohort) of 14 depressed patients with major depressive episodes, 60 mg of phenethylamine combined with selegiline (a monoamine oxidase inhibitor that blocks the enzyme that breaks down phenethylamine) reduced symptoms of depression in 12 patients over the course of 50 weeks [R].
In another study, 9 out of 10 depressed patients that previously did not respond to conventional antidepressant treatments reported elevated mood after taking a combination of phenethylamine and selegiline [R].
2) May Improve Alertness and Focus
Dopamine is a key neurotransmitter involved in regulating attention. By increasing levels of dopamine, adrenaline, and noradrenaline (epinephrine and norepinephrine), phenethylamine may increase energy, focus, and alertness. In mice, high doses of phenethylamine led to the same behavior as amphetamines, including increased energy [R, R, R].
3) May Improve Symptoms of Schizophrenia
The role of phenethylamine in schizophrenia is still unclear.
One study in schizophrenic patients found lower amounts of phenethylamine and its metabolite, phenylacetic acid, in cerebrospinal fluid (CFS) [R].
The altered levels of phenethylamine may play a role in schizophrenia by increasing or decreasing dopamine levels. An increase in dopamine levels is often seen in patients with schizophrenia [R].
4) May Improve ADHD Symptoms
ADHD is a behavioral problem, mostly in children and teenagers, characterized by short attention spans. While ADHD is usually diagnosed by observing behavior, it can also be diagnosed by measuring phenylethylamine in urine samples [R].
Children with ADHD have lower phenethylamine levels compared to their healthy peers [R].
In another study, adults with ADHD also had less phenylethylamine [R].
Patients who experienced a decrease in symptoms after taking methylphenidate for ADHD had increased phenylethylamine levels [R].
5) May Improve Sexual Drive
Since dopamine and other catecholamines are released during excitement or arousal, phenethylamine has been linked to sexual drive and feelings of pleasure. Phenethylamine is therefore sometimes referred to as the “love drug” [R, R].
6) May Increase Weight Loss
How to Increase Phenethylamine Levels
As such, phenethylamine may be responsible for the effect known as “runner’s high”.
2) Chocolate and Other Foods
Phenethylamine is found in chocolate, especially dark chocolate [R].
Phenethylamine can be used to indicate food quality and freshness since large amounts of phenethylamine are produced by bacteria [R].
The phenethylamine in chocolate may explain its reputation as an aphrodisiac (a substance that increases libido) [R].
However, cheese and sausage also contain phenethylamine but do not have the same reputation for causing cravings. Chocolate also has small amounts of other stimulants like caffeine and theobromine [R]. These could also be responsible for the mood-enhancing effects.
Phenethylamine’s effect is limited when supplemented orally because it is quickly broken down in the body by the enzyme monoamine oxidase [R].
Phenethylamine passes easily through the blood-brain barrier (BBB). However, large continuous doses may be required to see any effects. Studies in dogs showed that phenethylamine had a very short half-life (5 to 10 minutes) [R, R].
In addition, phenethylamine injected intravenously in rats was absorbed mainly by the lungs, liver, and kidneys, and less than 1% reached the brain [R].
Nonetheless, dietary supplements are widely available. The salt form, phenylethylamine HCL, is the most common phenylethylamine supplement, and phenylethylamine powders and tablets are also available.
Slow-release versions of phenethylamine have been developed, designed to slowly release phenethylamine over time to prolong its effects.
However, there is no clinical evidence to support the efficacy of these supplements and user reports are mixed.
Drugs Made from Phenethylamine
Is Phenethylamine the Same as MDMA?
Phenethylamines (plural), or substituted phenethylamines as they are known, are made up of the same chemical structure as phenethylamine, but by making slight changes to the structure it is possible to create new drugs with significantly different effects. One example is MDMA, which can alter a person’s mood and behavior [R].
There are dozens of modified phenethylamines with stimulating and brain-altering effects. Other well-known phenethylamines such as amphetamines are often sold illegally as street drugs, but can also be found as prescription medications used to treat ADHD and depression [R, R, R, R, R].
Side Effects of Phenethylamine
For short-term use, phenethylamine is considered “safe”, although it is not currently on the list of FDA-approved substances.
A study in which 14 people were treated for depression with 10 – 60 mg of phenethylamine orally per day for 50 weeks reported no side effects [R].
Warnings on supplement packaging suggest some side effects including heartburn, constipation, nausea, and mild headaches. More serious side effects include insomnia, confusion, dizziness, intense headaches, and sudden increases in heart rate and blood pressure.
Note that taking phenethylamine supplements is different from taking substituted phenethylamines, which should be taken with extreme caution as they have been shown to cause schizophrenia-like psychosis [R, R].
Contraindications of Phenethylamine
People taking MAO inhibitors, which are used for treating depression, anxiety, and other neurological illnesses like Parkinson’s, or those that have a condition known as phenylketonuria (PKU) should not take phenethylamine since these disorders prevent the metabolism of phenylalanine in the body which can lead to negative side effects, such as severe headaches and hypertension, or even psychosis [R].
People suffering from schizophrenia or similar illnesses may already have high levels of phenethylamine and dopamine and should, therefore, avoid this supplement [R].
Taking Phenylethylamine-Based Drugs May Be Dangerous
While phenethylamine supplements are thought to be relatively safe for humans and no human fatalities due to phenethylamine intake have been reported, very high doses of phenethylamine supplements have been shown to cause death in mice [R].
Phenethylamine-based drugs, however, may be dangerous, which is why they are classified as illicit. The dangers and risks of heart attack and death from taking MDMA and methamphetamines are well-known [R, R, R].
In addition, at least 5 deaths have been reported in people who had taken “legal” phenethylamine-based drugs [R].
Dosage of Phenylethylamine
At present, there is not enough scientific evidence to determine an appropriate range of doses for phenethylamine. According to manufacturers of phenethylamine supplements, the recommended dosage is usually between 100 and 500 mg 1 to 3 times daily and should not exceed 1,000 mg per day.
Dosages between 10 and 60 mg are used when combined with a strong monoamine oxidase inhibitor (MAOI) like selegiline, which prevents the breakdown of phenethylamine in the stomach. This means a smaller dose is needed to achieve similar effects in large doses.
While phenethylamine supplements are widely available, they should be taken with caution as safety has not been fully verified.
Limitations and Caveats
Clinical trials are lacking in humans, especially double-blind, randomized controlled trials measuring the effects of phenethylamine by itself. Caution is warranted when applying the current research to use in humans.
Some positive effects have been reported by users of phenethylamine:
“My level of concentration has been getting better in the two short weeks that I have been taking it and I do not seem to tire as fast.”
“Noticeably positive mood and definite boost in energy.”
“Works better than caffeine.”
“Fantastic burst of energy. No side effects. Highly recommend it!!”
More extreme effects have also been experienced:
“I started having tingling in my lips which spread to my face and scalp, intense head rushes and very noticeable euphoria. These sensations are so intense, it’s almost scary. It’s not unpleasant just very intense. That lasts around 30 minutes.”
Some users that have taken phenethylamine with hordenine and also reported positive effects:
“… you will have clean energy and excellent focus.”
“I feel positive, smile more, joke and I’m doing great on my new job. This product also seems to help me retain more information.”
“… it gives a very pleasant euphoric feeling for about ten minutes afterward leaving you feeling happy and energized for the rest of the day. It also helped me focus at school and work.”
While others have reported no effect at all:
“It just doesn’t work for me. Took pretty high doses.”
“It did nothing.”
Other user reviews suggest phenethylamine supplements taste horrible and can cause mild headaches, loss of circulation, sleepiness, and loss of appetite, increased heart rate and in extreme cases vomiting:
“Horrible!! This product is SO disgusting… Don’t try to gag it down.”
“It works great for about 30-45 minutes… then it makes me sleepy.”
“I had pins and needles on my neck and face as if I lost circulation to my head.”