Target intelligence / Profile preview

Glutamate Receptor Ionotropic (iGluR)

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

Overview

Ionotropic glutamate receptors (iGluRs) are ligand-gated ion channels activated by glutamate, mediating fast excitatory synaptic transmission in the central nervous system. They are crucial for synaptic plasticity, learning, and memory. iGluRs function as tetramers, with each subunit containing an N-terminal domain (NTD), a ligand-binding domain (LBD), a transmembrane domain (TMD), and an intracellular C-terminal domain (CTD). The three main subtypes are AMPA, NMDA, and Kainate receptors, each with distinct pharmacology and ion permeabilities. iGluRs regulate numerous processes in the brain, spinal cord, and peripheral nervous system, and are implicated in various neurological diseases.

Other names
iGluRsIonotropic Glutamate Receptors
02

Mechanism of action

Ligand binding to the extracellular domain causes a conformational change, opening the ion channel pore and allowing the influx of cations (Na+, K+, and/or Ca2+), leading to neuronal depolarization and excitatory postsynaptic currents. NMDA receptors require both glutamate and a co-agonist (glycine or serine) binding, as well as membrane depolarization to relieve Mg2+ block.

03

Biological functions

NeurotransmissionSynaptic plasticityLearningMemoryExcitatory postsynaptic currents
04

Disease associations

Alzheimer's diseaseStrokeSchizophreniaParkinson's diseaseMotor neuron diseaseDepressionNeurodegenerative diseaseOther neurological disorders
05

Safety considerations

Excitotoxicity (excessive glutamate signaling leading to neuronal damage)Potential for seizuresDevelopment of tolerance or dependence
06

Interacting drugs

Glutamate

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