Kainate receptors have only recently been characterized both from the pharmacological and biological point of view. Due to the limited number of truly kainate selective ligands, most of the known agonists and antagonists are generally classified as AMPA/kainate receptors ligands. The increasing interest in the search for selective kainate ligands aims at understanding the physiological role played by these receptors and finding out potential therapeutic approaches for the treatment of a number of neurological pathologies, i.e. schizophrenia, as well as acute and chronic neurodegenerative diseases, i.e. epilepsy, cerebral ischaemia, Parkinson's and Alzheimer's diseases. This review will focus on the recently discovered ligands for kainate receptors, with a particular attention given to those molecules displaying a selectivity for the different subunits of the kainate receptors and, on the other hand, to the role played by these receptor subtypes in the pathophysiology of the central nervous system.