Glutamate ionotropic receptor kainate type subunit 1 (GluK1 (alternatively GRIK1))

Glutamate ionotropic receptor kainate type subunit 1 (GluK1/GRIK1) is a protein subunit of kainate-type ionotropic glutamate receptors, acting as a ligand-gated cation channel predominantly in the brain. Activated by glutamate or kainic acid, these receptors contribute to fast excitatory neurotransmission and have critical roles in synaptic function and plasticity. GRIK1 is subject to RNA editing and alternative splicing, further diversifying its function and pharmacology. Abnormal activation or genetic variation in GRIK1 is implicated in seizure disorders (especially epilepsy), as well as wider neurological and psychiatric conditions. The receptor is actively studied for therapeutic modulation though few drugs directly target it in clinical practice

Other names

GluK1GRIK1Glutamate receptor, kainate 1Glutamate receptor, ionotropic kainate 1EAA3 (older literature)KA1, iGluR5 (less commonly used)

Agonists: Bind GluK1, open cation channel, depolarize neuronal membrane, increase excitatory currents Antagonists: Inhibit kainate receptor, reduce excitatory neurotransmission Positive allosteric modulators: Prolong activation, inhibit desensitization (e.g., concanavalin A, BPAM344) RNA editing/modulation: Alters channel permeability for calcium; potential implications in disease-modifying therapies