Target intelligence / Profile preview

Glutamate receptor ionotropic, kainate 5 (GluK5)

Target
GluK5
Molecular classification
Receptor, Ion channel, Ionotropic glutamate receptor, Ligand-gated ion channel
01

Overview

Glutamate receptor ionotropic, kainate 5 (GluK5) is a subunit of the kainate-type ionotropic glutamate receptors, which are cation-permeable ligand-gated ion channels activated by the neurotransmitter L-glutamate and kainic acid. It does not form functional channels on its own but instead assembles with "low-affinity" subunits (e.g., GluK1-3) to create heteromeric functional receptors. These receptors play a crucial role in regulating synaptic transmission, neuronal excitability, and network oscillations in the central nervous system. GluK5-containing receptors have been implicated in numerous CNS pathologies, including epilepsy, neurodegeneration, and psychiatric disorders, making them targets of significant scientific and therapeutic interest.

Other names
Excitatory amino acid receptor 2Glutamate receptor KA-2KA2EAA2GRIK5
02

Mechanism of action

Agonists (like glutamate and kainic acid) bind and activate the ion channel, leading to cation influx and neuronal depolarization. Antagonists (such as select barbiturates or specific research compounds) block channel activation, inhibiting synaptic transmission.

03

Biological functions

Regulation of neuronal excitabilitySynaptic transmissionMediation of excitatory postsynaptic potentialModulation of neurotransmitter releasePostsynaptic depolarization and presynaptic modulation
04

Disease associations

Neurodegenerative diseaseEpilepsyPsychiatric diseaseStrokeExcitotoxic cell deathPain disorders
05

Safety considerations

ExcitotoxicityLack of subunit selectivity for drugsPossible CNS side effects
06

Interacting drugs

Butabarbital

5 more in the full profile.

07

Biomarkers

Altered expression or genetic variation in CNS disordersExpression levels in brain tissue

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