Glutamate receptor ionotropic, kainate 1 (GluK1) (GluK1)

Glutamate receptor ionotropic, kainate 1 (GluK1) is a protein encoded by the GRIK1 gene and is a member of the ionotropic glutamate receptor family [1, 3]. It functions as a ligand-gated ion channel that mediates excitatory neurotransmission in the central and peripheral nervous systems by allowing the influx of cations upon binding glutamate or kainate [3, 6]. Beyond its canonical ionotropic role, GluK1 is involved in noncanonical metabotropic signaling through coupling with G-proteins, specifically Go, which modulates the release of other neurotransmitters like GABA and glutamate [5, 15]. GluK1 is highly expressed in areas such as the hippocampus, amygdala, and dorsal root ganglia, making it a key player in synaptic plasticity and sensory processing [9, 11]. It is a significant therapeutic target for neurological and psychiatric disorders, including epilepsy, chronic pain, migraine, and alcohol use disorder [5, 8, 11]. Pharmacological modulation of GluK1, particularly through selective antagonists, aims to reduce neuronal hyperexcitability and has demonstrated efficacy in preclinical models for treating seizures and nociception [11, 14].

Other names

GRIK1GluR5EAA3GLUR5GluR-5EEA3GLR5

Antagonist, Agonist, Allosteric modulator