Kainate Receptor Antagonists

Kainate receptors are cation-selective, ligand-gated ion channels, which cause a strong membrane depolarization in response to glutamate binding. Like other members of the ionotropic glutamate receptor family, they are named for their specific activation by kainate (kainic acid), which was initially isolated from the algae Digenea simplex.

Kainate receptors exist as tetramers, composed of the subunits GluK1 to 5. Each subunit has an extracellular N-terminus, a cytoplasmic C-terminus, three ...