Several years ago, somewhere around the year 2010-2011, a new substance appeared on the nutritional supplements market. The manufacturers spoke big words about it. Several years later, this substance is getting more and more popular in the food supplements market, it is sold as a stand-alone product and is also included in much of the pre-workout products.
We are talking about substance agmatine. In this article, we will pay some more attention to it. Agmatine is a well-known substance in our body because it occurs naturally in its parts and it present even in some food products.
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What Is Agmatine
There are different definitions of agmatine. It can also be found under its molecular name 4-(aminobutyl) guanidine. It is a well-known substance in our body because it occurs naturally in its parts and it present even in some food products.
It is a biogenic amine - an organic compound most commonly produced by the decarboxylation of certain amino acids. In the case of the agmatine, it is obtained by the decarboxylation of the amino acid L-arginine.
Agmatine is also considered a neurotransmitter and a neuromodulator because it is stored in the neurons and is released upon their activation. Studies on rats show that agmatine is mostly concentrated in the stomach, small intestine, thyroid gland, and some parts of the brain.
Agmatine is also found in some foods, with the most noticeable concentration being in wine (white and red), beer, sake, instant coffee, local products, and fish.
Before you run into the store and buy a lot of this product, we will specify that although these foods are richest in agmatine, the concentration in them is too low to be of practical significance.
What Role Does Agmatine Play and What Is Its Mechanism of Action
There have been scientific studies only conducted on animals (rats and mice) and in vitro so far. The studies on humans are few. However, several action mechanisms stand out.
One is the blocking of the NMDA receptors and the activation of the imidazoline ones. Agmatine also affects serotonin receptors. Agmatine has the ability to block the NOS (nitric oxide synthase) enzymes, which regulate the levels of nitric oxide in the blood.
Proven and Potential Benefits of Agmatine
These action mechanisms, as well as some other less well-researched ones, make agmatine potentially important in various areas of the human organism and human health.
1) Regulation and Reduction of Blood Pressure
Agmatine has the ability to bind to the imidazoline receptors. These receptors are three types, each with distinctive tasks:
- (1) – they mediate the actions required for the reduction of the blood pressure.
- (2) – they are important for the action and binding of the enzyme monoamine oxidase (MAO).
- (3) – they regulate the insulin secretion from the pancreatic beta cells.
The fact that it is an agonist to these receptors makes it important for the regulation and reduction of blood pressure.
Agmatine's ability to increase the levels of nitric oxide contributes to the expansion and relaxation of the blood vessels, which helps the blood circulation and the reduction of the blood pressure.
At this stage, the blood pressure reduction has been demonstrated by the injecting of agmatine into rats with high blood pressure.
2) Pain Reduction
Agmatine also has a good analgesic effect in certain conditions causing pain. Tests for neuropathic pain and pain due to inflammation in rats show that agmatine successfully reduces the sensation of pain. There has been a study, conducted for the analgesic effect of agmatine, a study on people with lumbar radiculopathy.
The study has included two groups:
- placebo group of 48 people;
- a group of 51 people who had taken 2,670 g of agamycan sulfate daily for a period of 14 days.
The results have been determined by the VAS scale, the McGill questionnaire, and the Oswestry disability index. Improvements have been seen in both groups, but in the agmatine group, they have been significantly better.
The sensation of pain has been improved by 26.7%, and the quality of life has increased by 70.80% (compared to 6% and 20%, respectively, for the placebo group). The results have been retained 60 days after the discontinuation of agmatine.
Agmatine also has the ability to significantly increase the duration of action of various opioids used in medicine such as morphine and fentanyl, for example. It also reduces the tolerance developed to various opiates with prolonged use.
3) Reduction of Stress, Anxiety, and Depression
There is a direct relationship between the levels of agmatine in the brain and the plasma during stressful situations. There is a significant increase in the levels of agmatine, probably due to an increase in the activity of the enzyme arginine decarboxylase, the enzyme that produces agmatine from the amino acid arginine.
The reduction of stress and anxiety has been demonstrated in various stress tests on mice - elevated plus maze, social and light signals. The efficacy of agmatine in these studies is comparable to imipramine and diazepam.
Comparable efficacy of anti-depressant properties with imipramine has also been observed in tests on rats. Agmatine works synergistically with other antidepressants - bupropriion and SSRIs.
A very small study on humans was conducted in 2013, involving only three individuals suffering from depression. Remission of depression has been found with the administration of 2-3 grams orally by all subjects.
4) Reduction of the Blood Sugar Levels
A study on rats, suffering from diabetes, has shown a strong potential for agmatine to lower the blood sugar levels. According to the investigators, this is done by activating the imidazoline receptors and secreting beta-endorphin.
More interesting in this case is that thanks to beta-endorphin, glucose is stored in the muscle tissue rather than the fatty tissue.
Agmatine Recommended Dose and Way of Intake
At this stage, the optimal dose has not yet been determined. In one of the pain reduction studies on humans, daily doses between 1.3 and 3.6 grams have been used.
The best time to take agmatine is 30-45 minutes before a workout.
Possible Interactions and Side Effects of Agmatine
There are no side effects with the tested doses of up to 3.6 grams, with the exception of the upset stomach with the highest doses. It is not known how safe the doses are when over the recommended ones.
The concomitant intake of agmatine is not recommended with:
- Arginine or citrulline due to blockage of some of the beneficial neurological effects, such as a reduction in the pain sensation or reduction of the tolerance to opiates;
- Yohimbine and rauwolscine, as they have the opposite effect;
- D-aspartic acid due to decreased efficiency;
- Alcohol - concomitant intake may increase the risk of ulcers.
Yes, agmatine has great potential, but for now, its effectiveness in athletes and non-athletes is not quite clear.