Agmatine: clinical applications after 100 years in translation

Drug Discov Today. 2013 Sep;18(17-18):880-93. doi: 10.1016/j.drudis.2013.05.017. Epub 2013 Jun 13.


Agmatine (decarboxylated arginine) has been known as a natural product for over 100 years, but its biosynthesis in humans was left unexplored owing to long-standing controversy. Only recently has the demonstration of agmatine biosynthesis in mammals revived research, indicating its exceptional modulatory action at multiple molecular targets, including neurotransmitter systems, nitric oxide (NO) synthesis and polyamine metabolism, thus providing bases for broad therapeutic applications. This timely review, a concerted effort by 16 independent research groups, draws attention to the substantial preclinical and initial clinical evidence, and highlights challenges and opportunities, for the use of agmatine in treating a spectrum of complex diseases with unmet therapeutic needs, including diabetes mellitus, neurotrauma and neurodegenerative diseases, opioid addiction, mood disorders, cognitive disorders and cancer.

Publication types

  • Historical Article
  • Review

MeSH terms

  • Agmatine / chemistry
  • Agmatine / history
  • Agmatine / metabolism
  • Agmatine / pharmacology
  • Agmatine / therapeutic use*
  • Animals
  • Drug Discovery* / history
  • History, 20th Century
  • History, 21st Century
  • Humans
  • Signal Transduction / drug effects
  • Tissue Distribution


  • Agmatine