Agmatine: Clinical applications after 100 years in translation

John E. Piletz, Feyza Aricioglu, Juei Tang Cheng, Carolyn A. Fairbanks, Varda H. Gilad, Britta Haenisch, Angelos Halaris, Samin Hong, Jong Eun Lee, Jin Li, Ping Liu, Gerhard J. Molderings, Ana Lúcia S. Rodrigues, Joseph Satriano, Gong Je Seong, George Wilcox, Ning Wu, Gad M. Gilad

Research output: Contribution to journalReview articlepeer-review

191 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)880-893
Number of pages14
JournalDrug Discovery Today
Issue number17-18
Publication statusPublished - 2013 Sept

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery


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