Glycine is the smallest non-essential, neutral and metabolically inert amino acid, with a carbon atom bound to two hydrogen atoms, and to an amino and a carboxyl group. This amino acid is an essential substrate for the synthesis of several biologically important biomolecules and compounds. It participates in the synthesis of proteins, of the tripeptide glutathione and in detoxification reactions. It has a broad spectrum of anti-inflammatory, cytoprotective and immunomodulatory properties. To exert its actions, glycine binds to different receptors. The GlyR anion channel is the most studied receptor for glycine. However, there are GlyR-independent mechanisms for glycine cytoprotection and other possible binding molecules of glycine are the NMDA receptor and receptors GlyT1 and GlyT2. Although, in humans, the normal serum level of glycine is approximately 300 μM, increasing glycine intake can lead to blood levels of more than 900 μM that increase its benefic actions without having harmful side effects. The herbal pesticide glyphosate might disrupt glycine homeostasis. Many in vitro studies involving different cell types have demonstrated beneficial effects of the addition of glycine. Glycine also improved conditions of isolated perfused or stored organs. In vivo studies in experimental animals have also tested glycine as a protector molecule and some studies on the beneficial effects of glycine after its clinical application have been done. Although at high-doses, glycine may cause toxic effects, further studies are needed to investigate the safe range of usage of this aminoacid and to test the diverse routes of administration.