High affinity angiotensin-converting enzyme (ACE) ligand (Kd = 2.79 nM). Exhibits no significant effect on ACE enzymatic activity up to 500 nM concentration. Potentiates NMDA + D-serine-induced dopamine release from striatal slices in vitro and the striatum in vivo.

N-alpha-Acetylarginine is one of the guanidino compounds found elevated in the serum of a hemodialyzed renal insufficient (uremic) pediatric population.

Gracillin can induce cell cycle arrest, oxidative stress, and apoptosis in HL60 cells, and has the potential to be developed as an antitumor agent.