The inhibitory glycine receptor is a member of the ligand-gated ion channel superfamily. It mediates inhibitory synaptic transmission in mammalian spinal cord and brainstem. Structure and function of the receptor, as well as its chromosomal localization and genetic structure, have been extensively studied. While hereditary and acquired receptor dysfunctions can be identified, selective and specific modulation of receptor function is still lacking. The preponderance of current literature regarding the inhibitory glycine receptor raises the prospect that adequate methods for the treatment of glycine receptor-mediated disorders might be developed.