It is now generally recognised that glutamate is the major excitatory neurotransmitter in vertebrate central nervous system (CNS). It acts at ionotropic and metabotropic receptors which appear to play important roles in all aspects of CNS functions. The ionotropic receptors, which are involved in fast synaptic transmission, belong to three subtypes named after three relatively selective agonists: NMDA (N-methyl-D-aspartate, AMPA [2- amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)-propionate] and KA (kainate) receptors. The compounds acting as AMPA antagonists are potentially useful for the prevention and treatment of a broad range of acute and chronic neurological disorders. This article describes the development of recent AMPA receptor antagonists, reviewing both the primary and patent literature.