Glycine accomplishes several functions as a transmitter in the central nerv
ous system (CNS). As an inhibitory neurotransmitter, it participates in the
processing of motor and sensory information that permits movement, vision,
and audition. This action of glycine is mediated by the strychnine-sensiti
ve glycine receptor, whose activation produces inhibitory post-synaptic pot
entials. In some areas of the CNS, glycine seems to be co-released with GAB
A, the main inhibitory amino acid neurotransmitter. In addition, glycine mo
dulates excitatory neurotransmission by potentiating the action of glutamat
e at N-methyl-D-aspartate (NMDA) receptors. It is believed that the termina
tion of the different synaptic actions of glycine is produced by rapid reup
take through two sodium-and-chloride-coupled transporters, GLYT1 and GLYT2,
located in the plasma membrane of glial cells or pre-synaptic terminals, r
espectively. Glycine transporters may become major targets for therapeutic
of pathological alterations in synaptic function. This article reviews rece
nt progress on the study of the molecular heterogeneity, localization, func
tion, structure, regulation and pharmacology of the glycine transporter pro
teins.