Kainate receptors (KARs) are one of the three subtypes of ionotropic glutamate receptors in the CNS. These receptors are widely expressed pre- and postsynaptically throughout the brain. Thus, kainate receptor activation mediates a large variety of pre- and postsynaptic effects on either glutamatergic or GABAergic synaptic transmission. Although ionotropic functions for KAR have been described in multiple brain regions, there is considerable evidence from various CNS regions that KARs activation modulates GABA release through either G-protein dependent metabotropic pathway or secondary activation of G-protein coupled receptors. In the present chapter, we provide further evidence supporting that these two pathways are also involved in the modulation of GABA release in specific basal ganglia nuclei. Because of their more subtle effects on neurotransmisison regulation than other ionotropic glutamate receptors, KARs represent interesting targets for the future development of pharmacotherapy for basal ganglia diseases.