Agmatine is a sports supplement (agmatine sulfate), which is often touted as the most active form of the nitrogen donor – arginine , however, when you compare the effects, it has quite a few similarities with it. In pharmacology, agmatine is presented as a nootropic that protects the brain from ischemic damage, and is also promising for the treatment of neuropathic pain and drug addiction. Positive effects on athletic performance and muscle growth are not directly proven, but well established.
Discovered and named in 1910 by the German scientist Albrecht Kossel, who isolated agmatine from herring milk.]From a chemical point of view, it is a biogenic amine that is formed from L-arginine by decarboxylation (removal of the carboxyl group). Agmatine is also present in the human body, acting as a neurotransmitter, it is deposited in some neurons and released when they are activated.
Mechanism of action
The agmatine molecule has pleiotropic (diverse) biological effects and has several proven mechanisms that may be beneficial to athletes.
Increases eNOS activity
NOS (nitric oxide synthase) is an enzyme that synthesizes nitric oxide . There are three types of this enzyme: iNOS (immune), nNOS (nervous) and eNOS (vascular). The first two species are inhibited by agmatine, but an increase in the level and activity of eNOS has been shown experimentally. [ As you know, nitric oxide is multifunctional and is formed in many cells and tissues. In bodybuilding, only eNOS is of interest, since it synthesizes nitric oxide in the blood, which leads to an expansion of the capillary bed and an improvement in muscle tissue nutrition. Thus, this mechanism could theoretically facilitate the transport of nutrients and oxygen, promote muscle recovery and provide pumping .
Activation of imidazoline receptors [
A number of studies have unequivocally proven the activation of imidazoline receptors; moreover, agmatine is an endogenous (natural) ligand of imidazoline receptors. The I1-imidazoline receptor agonists include the well-known pharmacological drugs moxonidine and rilmenidine, which are used to lower blood pressure.
When imidazoline receptors are activated, the following effects develop:
- suppression of the sympathetic nervous system (sedative effect)
- decreased secretion of adrenaline and other catecholamines
- vasodilation and a decrease in blood pressure
- increased secretion of the anabolic hormone insulin and improved tissue energy supply
- increased lipolysis (fat burning)
- reduction in lactic acid production
Side effects: Therapy with I1-imidazoline receptor agonists is accompanied by the development of a number of side effects, such as drowsiness or insomnia, asthenia, headache, dizziness, weakness during exercise, fear, depression, convulsions, palpitations, cold extremities, orthostatic hypotension, hot flashes, dry mouth, epigastric pain, diarrhea, nausea, constipation , peripheral edema, sexual dysfunction, skin rash, itching.
Stimulates the secretion of gonadotropin and gonadoliberin
It is known that these two peptides are able to increase the production of their own testosterone . A positive effect on the secretion of gonadotropin (luteinizing hormone) and gonadorelin was revealed only in a 1995 study on rats. In this case, agmatine was injected into the ventricles of the brain. Similar results were obtained by M. Kovach, J. Gulias in 1988 with intravenous administration of the GHRG peptide with the replacement of arginine by agmatine in the amino acid sequence.
Blocking NMDA receptors
This mechanism continues to be actively studied, since it is of great importance for neuroprotection. However, in bodybuilding it is not of particular interest.
Release of endorphins
Due to the release of beta-endorphin and an increase in the sensitivity of opioid receptors, it has an analgesic effect. At the same time, it does not cause dependence.
In addition, activation of serotonin and alpha2-adrenergic receptors, blocking of nicotinic receptors, activation of PI3K / Akt and adenylate cyclase were found.
As can be seen from the description of the mechanisms, agmatine sulfate implements its main action far from being due to nitric oxide. This is just one of many mechanisms whose usefulness is highly questionable. Moreover, there is a study [ that showed that nitric oxide inhibits the synthesis of its own steroid hormones (testosterone) in the testes .
Despite this, the imidazoline mechanism looks very attractive and well founded. It is worth noting that a noticeable decrease in strength and activity during training is possible, due to the sedative effect and a decrease in the level of catecholamines (although many manufacturers say the opposite, there is a supporting footnote in the section of mechanisms), therefore, the supplement can play a negative role for power workers, although in As part of pre-workout complexes, this may be unnoticed due to the additional inclusion of stimulants . There is also an open question about the bioavailability of agmatine sulfate, which is used in all sports supplements.
- AGMATINE 500 from USP labs
- Agmatine by Serious Nutrition Solutions
- Hybrid NO by MusclePharm
- Jack3d Micro (USPlabs)
- Fierce Domination by SAN
- Testogen-XR by Ronnie Coleman
- MOAB from Muscle Warfare
- Cannibal Perma Swole by Chaos & Pain
- Insane Veinz by Insane Labz
It is recommended to take 500-1000 mg approximately 45 minutes before training, or at any time of the day during rest with a meal. The maximum recommended dose is 6,000 mg, according to MayoClinic.com. Can be combined with other sports nutrition. The optimal duration of admission is not clearly regulated, approximately 1-2 months.