Target intelligence / Profile preview

Glutamate receptor ionotropic NMDA 2B (GRIN2B)

Target
GRIN2B
Molecular classification
Ion channel, Glutamate receptor, NMDA receptor, Ligand-gated ion channel
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Overview

Glutamate receptor ionotropic NMDA 2B (GRIN2B) is a critical subunit of the N-methyl-D-aspartate (NMDA) receptor, a ligand-gated ion channel essential for excitatory neurotransmission in the mammalian central nervous system. It plays a fundamental role in synaptic plasticity, which underlies the processes of learning and memory formation by regulating calcium influx into neurons. Dysregulation or mutations in the GRIN2B gene are linked to a variety of neurological and psychiatric conditions, including epilepsy, autism spectrum disorders, and neurodegenerative diseases like Alzheimer's. Pharmacologically, GRIN2B is a major therapeutic target; drugs such as memantine and ketamine modulate its activity to treat cognitive decline and treatment-resistant depression, respectively. Selective NR2B antagonists are also being investigated for their potential to provide neuroprotection and analgesic effects with fewer side effects than broad-spectrum NMDA antagonists.

Other names
NMDA receptor subunit 2BN-methyl D-aspartate receptor subtype 2BNR2BGluN2BGlutamate [NMDA] receptor subunit epsilon-2hNR2B
02

Mechanism of action

Non-competitive antagonist, Channel blocker, Negative allosteric modulator (NAM)

03

Biological functions

Synaptic plasticityLong-term potentiation (LTP)Long-term depression (LTD)NeurotransmissionLearningMemoryCalcium signaling
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Disease associations

EpilepsyAutism spectrum disorderIntellectual disabilityAlzheimer's diseaseParkinson's diseaseMajor depressive disorderSchizophreniaChronic pain
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Safety considerations

Psychotomimetic effects (hallucinations, dissociation)Cognitive impairmentSedationMotor coordination issuesPotential for abuse
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Interacting drugs

Memantine

8 more in the full profile.

07

Biomarkers

GRIN2B gene mutationsNMDA receptor occupancy (PET imaging)CSF glutamate levels

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