Agmatine

Last Updated: October 13, 2024

Agmatine is a metabolite of L-Arginine. It shows promise for alleviating neuropathic pain and drug addiction and shows some potential in protecting against strokes and benefitting cognitive health.

Agmatine is most often used for

What is agmatine?

Agmatine is a neurotransmitter and neuromodulator derived from L-arginine and has potential applications in treating neuropathic pain and drug addiction, based on animal studies. It is also present in certain fermented foods, such as wine.

What are agmatine’s main benefits?

Agmatine may influence pain perception and has shown weak general analgesic properties, and there is some evidence of dose-dependent pain relief for neuropathic pain. Additionally, preliminary studies suggest that it may help reduce alcohol withdrawal symptoms and that it has potential for treating depression and nerve-related pain, though more research is needed for its effectiveness in drug addiction.

What are agmatine’s main drawbacks?

Agmatine may cause mild to moderate side effects such as diarrhea and mild nausea, which typically resolve over time or with discontinuation of use. More research is necessary to establish its safety for use in humans.

How does agmatine work?

Agmatine is a naturally occurring neuromodulator that is produced from L-arginine and interacts with several transmembrane receptors, such as alpha-2 adrenergic, imidazoline I1, and NMDA receptors.

What are other names for Agmatine?
Note that Agmatine is also known as:
  • Clonidine-displacing substance
  • 4-(aminobutyl)guanidine
  • Decarboxylated arginine
Agmatine should not be confused with:
Dosage information

There are no standard dosages for agmatine because of the lack of human evidence for its effects. However, a single human study used 1,300-2,670mg of agmatine, daily for the treatment of neuropathic pain. The estimated human dose for improving cognition is 1.6-6.4mg/kg of agmatine, taken orally. This is based off of the 10-40mg/kg dosage range for rats, and is equivalent to 109-435mg for a 150lb person. Supplementation should not exceed 6.4mg/kg of bodyweight.

Studies on agmatine use a daily dosing protocol.

Agmatine is not absorbed well when taken with dietary protein, because it uses the same transporters as arginine. Further research is needed to determine if oral agmatine supplementation provides the same benefits as were observed in animal studies.

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References
  1. ^Fairbanks CA, Schreiber KL, Brewer KL, Yu CG, Stone LS, Kitto KF, Nguyen HO, Grocholski BM, Shoeman DW, Kehl LJ, Regunathan S, Reis DJ, Yezierski RP, Wilcox GLAgmatine reverses pain induced by inflammation, neuropathy, and spinal cord injury.Proc Natl Acad Sci U S A.(2000-Sep-12)
  2. ^Uzbay IT, Yeşilyurt O, Celik T, Ergün H, Işimer AEffects of agmatine on ethanol withdrawal syndrome in rats.Behav Brain Res.(2000-Jan)
  3. ^Li J, Li X, Pei G, Qin BYEffects of agmatine on tolerance to and substance dependence on morphine in mice.Zhongguo Yao Li Xue Bao.(1999-Mar)
  4. ^Taksande BG, Kotagale NR, Patel MR, Shelkar GP, Ugale RR, Chopde CTAgmatine, an endogenous imidazoline receptor ligand modulates ethanol anxiolysis and withdrawal anxiety in rats.Eur J Pharmacol.(2010-Jul-10)
  5. ^Cantin L, Lenoir M, Augier E, Vanhille N, Dubreucq S, Serre F, Vouillac C, Ahmed SHCocaine is low on the value ladder of rats: possible evidence for resilience to addiction.PLoS One.(2010-Jul-28)
  6. ^Shopsin BThe clinical antidepressant effect of exogenous agmatine is not reversed by parachlorophenylalanine: a pilot study.Acta Neuropsychiatr.(2013-Apr)
  7. ^Keynan O, Mirovsky Y, Dekel S, Gilad VH, Gilad GMSafety and Efficacy of Dietary Agmatine Sulfate in Lumbar Disc-associated Radiculopathy. An Open-label, Dose-escalating Study Followed by a Randomized, Double-blind, Placebo-controlled TrialPain Med.(2010 Mar)
  8. ^Rosenberg ML, Tohidi V, Sherwood K, Gayen S, Medel R, Gilad GMEvidence for Dietary Agmatine Sulfate Effectiveness in Neuropathies Associated with Painful Small Fiber Neuropathy. A Pilot Open-Label Consecutive Case Series Study.Nutrients.(2020-Feb-23)
  9. ^Halaris A, Plietz JAgmatine : metabolic pathway and spectrum of activity in brain.CNS Drugs.(2007)