A decade ago, our understanding of the molecular properties of kainate rece
ptors and their involvement in synaptic physiology was essentially null. A
plethora of recent studies has altered this situation profoundly such that
kainate receptors are now regarded as key players in the modulation of tran
smitter release, as important mediators of the postsynaptic actions of glut
amate, and as possible targets for the development of antiepileptic and ana
lgesic drugs. In this review, we summarize our current knowledge of the pro
perties of kainate receptors focusing on four key issues: 1) their structur
al and biophysical features, 2) the important progress in their pharmacolog
ical characterization, 3) their pre- and postsynaptic mechanisms of action,
and 4) their involvement in a series of physiological and pathological pro
cesses. Finally, although significant progress has been made toward the elu
cidation of their importance for brain function, kainate receptors remain l
argely an enigma and, therefore, we propose some new roads that should be e
xplored to obtain a deeper understanding of this young, but intriguing, cla
ss of proteins.