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Glutamate ionotropic receptor kainate type subunit 3 (GRIK3, also known as GluK3 or GLUR7) is a subunit of the kainate family of ionotropic glutamate receptors. It forms tetrameric, cation-permeable, ligand-gated ion channels primarily responsive to glutamate and the agonist kainic acid. GRIK3 can form heteromeric receptors with other kainate subunits (such as GRIK4 or GRIK5), and is predominantly expressed in the brain, where it mediates fast excitatory neurotransmission at both pre- and postsynaptic sites. These receptors play a vital role in regulating synaptic transmission and plasticity, and their dysfunction is associated with a range of neurological and neuropsychiatric disorders including schizophrenia and autism spectrum disorder. GRIK3 activity is modulated by N-glycosylation and protein–protein interactions, and the receptor demonstrates unique gating and desensitization kinetics within its family. Drugs targeting GRIK3 may modulate synaptic excitability and are under investigation for their role in neurological disease.
Kainate receptor agonists activate the cation channel, allowing influx of cations (Na+, Ca2+), leading to membrane depolarization and synaptic excitation. Antagonists bind the ligand binding domain to prevent channel opening.
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