Target intelligence / Profile preview

Glutamate Receptor Kainate Subtype (KAR)

Target
KAR
Molecular classification
Ion channel, Ligand-gated ion channel, Glutamate receptor
01

Overview

Kainate receptors (KARs) are a subtype of ionotropic glutamate receptors that function as ligand-gated ion channels. They respond to the neurotransmitter L-glutamate and play key roles in regulating synaptic transmission and modulating neuronal circuits in the central nervous system. KARs are distinct from other glutamate receptor subtypes, such as AMPA and NMDA receptors, both structurally and functionally. They are tetrameric complexes composed of GluK1-GluK5 subunits. KARs mediate excitatory neurotransmission by permitting cation flow—primarily Na⁺—upon activation by glutamate. Unlike AMPA receptors, kainate receptors often act as modulators at both pre-synaptic and post-synaptic sites.

Other names
Kainate receptorGluK1GluK2GluK3GluK4GluK5GluR5GluR6GluR7KA1KA2
02

Mechanism of action

Ligand-gated ion channel activation/inhibition

03

Biological functions

Synaptic transmissionModulation of neuronal excitabilityRegulation of neural circuit activitySynaptic developmentNeurotransmission
04

Disease associations

DepressionSchizophreniaStrokeAlzheimer’s diseaseParkinson’s diseaseNeurological disorders
05

Safety considerations

Potential for excitotoxicityLimited clinical use of selective antagonists
06

Interacting drugs

Kainic acid

3 more in the full profile.

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