Agmatine Sulfate – An Overview

Agmatine Sulfate - An Overview

Dietary Agmatine sulfate has been seen as a treatment for neuropathic pain and other disorders.

Aminoguanidine agmatine was discovered by Albrecht Kossel. It was discovered in 1910. It is found naturally in the human body. The decarboxylation of arginine forms it by the enzyme arginine decarboxylase. Studies have shown that agmatine can be used for the treatment of pain and addiction.

Agmatine is stored in the neurons. It is also found in many plants and animals naturally, such as:

  • Ergot Fungi
  • Herring Sperm
  • Mammalian Brain
  • Octopus Muscle
  • Ragweed Pollen
  • Sponges


It is seen that agmatine helps modulate different chemical pathways of the brain.

Mechanism of Action

The mechanism of action is still under investigation as the drug has gained the attention of scientists. Agmatine can bind to different receptors and can generate responses as a signal triggering molecule. It binds to many receptors such as:

  1. Nicotine Receptors
  2. Imidazole Receptors
  3. Glutamate NMDAr Receptors
  4. Serotonin Receptors
  5. Voltage-Dependent Calcium Channel

1.      Nicotine Receptors

Studies have shown that agmatine blocks nicotine receptors in a chick’s retina and rat’s superior ganglion at high concentrations. The studies were done with titrated agmatine.

2.      Imidazole Receptors

There are three types of imidazole receptors, and agmatine’s action depends on the type of receptor it binds to. According to the binding, it can either

  • Modulate the insulin
  • Decrease the blood pressure
  • Alleviate the neuropathic pain

3.      Glutamate NMDAr Receptors

The antidepressant effect of agmatine is because it blocks the glutamate NMDAr receptor. It enhanced the antidepressant effect of NMDA by 100-fold.  It also inhibits the NMDAr-mediated excitotoxicity.

4.      Serotonin Receptor

There is no direct effect of agmatine on serotonin receptors.

5.      Voltage-Dependent Calcium Channel

It inhibits the calcium channel present in the sympathetic nerve terminals.


It is absorbed through the gastrointestinal tract and distributed throughout the body readily. The half-life of agmatine is 2 hours.

Effect of Agmatine on Different Diseases

Effect of agmatine has been discovered for diabetes, neuroprotection, and psychiatric conditions. It produces a hypoglycemic effect by increasing the release of insulin from pancreatic islet cells. Through modulation of receptors, it shows its neuroprotective nature. It is also used in the treatment of depression. The reason for this is the modulation of the NMDAr receptor, serotonin receptor, and imidazole receptor.

Agmatine works synergistically with opioids like fentanyl and morphine. It works best for pain tolerance and pain.

Drug Interactions of Agmatine Sulfate

Different drug interactions of agmatine sulfate are:

Acarbose – the severity of the hypoglycemic effect can increase in the presence of agmatine.

Acebutolol – agmatine might increase the bradycardia effect of acebutolol.

Aceclofenac – when these two drugs interact, it can increase the severity of hyperkalemia.

Acetyldigitoxin – the arrhythmogenic effect might increase with the use of agmatine.

Acyclovir – the adverse effect of acyclovir are increased with the use of agmatine.

Acetohexamide – agmatine sulfate increases the hypoglycemic effect when given this drug.

Agmatine as an Neuroprotective Agent

Traumatic brain injury is the second largest killer disease. Agmatine is neuroprotective, which is why its use in traumatic brain injury is important. Nitric oxide and glutamate receptors both have been seen as contributing factors in hypoxia-ischemic brain injury. Therefore, agmatine is a perfect candidate because it inhibits the nitric oxide receptor and the glutamate NMDAr receptor. There is no human evidence yet of the neuroprotective nature of agmatine. Still, it has been seen to act as a neuroprotective agent in rats, specifically in the ischemic brain and spinal cord injury.

There are many ways through which agmatine can help in the injuries. As discussed above, it can potentiate the effect of opioids and painkillers that make it a great drug to be used in injuries of any kind.

Agmatine as Body Building Drug

Agmatine has been seen to improve muscle mass in both males and females. Agmatine is also an inhibitor of nitric acid that increases the amount of nitric acid, which in turn increases the blood flow that helps in bodybuilding. Agmatine is also seen to regulate insulin reserves. The glycogen storage will increase, which means less glucose will be turned into fat and lead to bodybuilding.

The inhibition of nitric acid increases blood flow. It enhances protein synthesis, which is important for the building of muscle mass.

Agmatine as Pain Reliever

Agmatine is a great pain reliever. It works great for inflammation, spinal cord injuries, and neuropathic pain. It may offer short-term pain relief.

How to Take Agmatine Sulfate?

There are little to no human studies on agmatine; that is why it isn’t easy to pinpoint the exact dosage for agmatine sulfate. However, the estimated dose is 1.6-6.4mg/kg taken orally. The dose should not exceed 6.4mg/kg. It should not be taken with dietary products as they hinder its absorption.

In a study in which agmatine was used to alleviate neuropathic pain, it was seen that there was a notable decrease in pain that made agmatine great for pain treatment. It is also used for the treatment of depression, but the study evidence is very little.

Side Effects of Agmatine

The side effects of agmatine are very few. It can disrupt the function of the gastrointestinal tract. It can cause nausea, vomiting, and diarrhea. If given in high doses, it can decrease the pain tolerance of the person.


The useful effects of agmatine sulfate are great. Its effect on alleviating pain and bodybuilding makes it a popular drug among athletes. It also has beneficial effects on insulin production. It has an anti-oxidant effect. The effect of it on depression is also note-worthy.

There is very little research and studies done on agmatine. That makes this drug high-risk. Though there are many benefits of agmatine, it should be taken with caution. Dosage should be taken according to the recommendation of the physician. More research is needed for this drug as it shows many potential health benefits.


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