Agmatine is derived from L-arginine through decarboxylation (the removal of a carboxylic acid group). It is stored in neurons and is released during neuronal activation. Agmatine is considered to be a neurotransmitter and neuromodulator.
Preliminary research suggests agmatine has potential use in the treatment of neuropathic pain and drug addiction. It also protects the brain from toxins and strokes.
Though supplementing agmatine by itself can increase the perception of pain, it works synergistically with painkillers like morphine and fentanyl. Agmatine’s synergy with opioids allows it to reduce pain killer tolerance, the possibility of addiction, and pain itself.
Agmatine has several mechanisms. It can inhibit N-methyl-D-aspartate (NMDA) and nicotinic acetylcholine receptors, as well as activate imidazoline receptors. Agmatine can also inhibit nitric oxide synthase enzymes, which allows it to regulate elevated levels of nitric oxide. Agmatine can inhibit calcium channels and certain serotonin receptors as well. Further research is needed to determine the full extent of agmatine’s mechanisms.
There is a lot of animal evidence to suggest agmatine is a highly promising research chemical. It is not a common supplement because there is a lack of human evidence for its effects. Several studies have been done on people, but the majority use agmatine injections, not oral ingestion. Research must establish that agmatine’s effects will work following oral ingestion in order for wide-scale supplementation to be considered.