Target intelligence / Profile preview

Ionotropic Glutamate Receptors (AMPA, Kainate, NMDA) (iGluRs)

Target
iGluRs
Molecular classification
Receptor, Ion channel, Ligand-gated ion channel
01

Overview

Ionotropic glutamate receptors (iGluRs) are a family of ligand-gated ion channels that mediate fast excitatory synaptic transmission in the central nervous system. The three main subtypes are AMPA, kainate, and NMDA receptors. They are critical for neuronal communication, synaptic plasticity, learning, and memory. Dysfunction of these receptors is implicated in various neurological and psychiatric disorders. Each receptor has a unique subunit composition, ion permeability, and pharmacological profile. Activation leads to influx of cations and membrane depolarization. NMDA receptors are unique due to their voltage-dependent Mg2+ block and requirement for co-agonist binding.

Other names
AMPA receptorKainate receptorNMDA receptorGlutamate receptor (ionotropic)iGluR
02

Mechanism of action

Ligand binding to the receptor opens the ion channel, allowing influx of cations (Na+, K+, Ca2+), leading to membrane depolarization and excitatory postsynaptic currents (EPSCs). NMDA receptors also require co-agonist binding (glycine/D-serine) and are voltage-dependent due to Mg2+ block.

03

Biological functions

Synaptic transmissionExcitatory neurotransmissionSynaptic plasticityLearningMemory formationNeuronal signaling
04

Disease associations

StrokeEpilepsyNeurodegenerative diseasesSchizophreniaExcitotoxicityNeurological disordersPsychiatric disorders
05

Safety considerations

ExcitotoxicityOverstimulation can lead to neuronal damagePotential for off-target effects
06

Interacting drugs

AMPA agonists

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