Background Kainate receptor(KA) form a family of ionotropic glutamate receptors that appear to play a special role in the regulation of the central nervous system. KA are composed of five subunits——Glutamate Receptor(GluR)5, GluR6, GluR7, KA1, and KA2. The molecular properties of GluR6 and its physiological functions were known less previously. Recent advances in the molecular biology and the pharmacology have altered this situation profoundly. GluR6 subunit is the most important KA, which could form functional homomeric receptors as well as combine with other KA subunits. It is widely expressed throughout the nervous system, where they serve as key players in the modulation many physiological and pathophysiological functions. Objective To investigate whether GluR6 subunit have multiple action on central nervous system. Content This review presents the structures, distribution, activate mechanism of GluR6 and the evidence that implicates GluR6 subunit in physiological and pathophysiological conditions such as cerebral ischemia/reperfusion injury, psychiosis, pain, and human molecular genetics. Trend This review shows that GluR6 subunit represents promising therapeutic targets.