Target intelligence / Profile preview

Glutamate Kainate Receptor (KAR)

Target
KAR
Molecular classification
Ionotropic glutamate receptor, Receptor, Ligand-gated ion channel
01

Overview

Glutamate kainate receptors (KARs) are a subfamily of ionotropic glutamate receptors (iGluRs) that mediate fast excitatory neurotransmission in the central nervous system. They are tetrameric ligand-gated ion channels activated by glutamate and composed of GluK1-5 subunits. KARs are found both pre- and postsynaptically, modulating neurotransmitter release and synaptic plasticity. They are implicated in various neurological and psychiatric disorders including epilepsy, schizophrenia, Alzheimer’s disease, Parkinson’s disease, and autism spectrum disorder.

Other names
Kainate ReceptorKainate-selective glutamate receptorGluK1 receptorGluK2 receptorGluK3 receptorGluK4 receptorGluK5 receptorGluR5 receptorGluR6 receptorGluR7 receptorKA1 receptorKA2 receptor
02

Mechanism of action

Ligand-gated ion channel activation; modulation of ion flow and neuronal excitability

03

Biological functions

Fast excitatory neurotransmissionModulation of neurotransmitter releaseSynaptic plasticityModulation of network activity
04

Disease associations

EpilepsySchizophreniaDepressionStrokeAlzheimer’s diseaseParkinson’s diseaseAutism Spectrum DisorderNeurodevelopmental disorders
05

Safety considerations

Potential for excitotoxicityOff-target effects due to lack of subtype-selective drugs
06

Interacting drugs

CNQX

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