Target intelligence / Profile preview

Alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPA receptor) (AMPAR)

Target
AMPAR
Molecular classification
Ion channel, Receptor, Glutamate receptor, Ionotropic receptor
01

Overview

The Alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor is a ligand-gated ion channel that mediates fast excitatory synaptic transmission in the central nervous system [1, 6]. It plays a pivotal role in synaptic plasticity, which is the cellular basis for learning and memory formation [1, 2]. The drug candidate NA-831 (Traneurocin) acts as a positive allosteric modulator of the AMPA receptor, a mechanism that triggers the upregulation of the Brain-Derived Neurotrophic Factor (BDNF) expression pathway [2, 8]. BDNF is a vital neurotrophin that promotes the survival, growth, and differentiation of neurons, particularly in the hippocampus [3, 4]. By enhancing this pathway, NA-831 stimulates adult hippocampal neurogenesis and provides neuroprotection against the cognitive decline associated with neurodegenerative diseases [5, 7]. This approach is currently being investigated for the treatment of Alzheimer's disease, where it aims to restore neuronal health and improve memory functions [9, 10].

Other names
Alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptorAMPARGlutamate receptor ionotropic AMPAGluRAMPA-type glutamate receptorQuisqualate receptor
02

Mechanism of action

Positive allosteric modulation of AMPA receptors leading to increased BDNF expression and subsequent neurogenesis and neuroprotection.

03

Biological functions

Signal transductionSynaptic plasticityNeurogenesisLearning and memoryNeuroprotection
04

Disease associations

Neurodegenerative diseaseAlzheimer's diseaseMajor depressive disorderStrokeRett syndromeFragile X syndromeCOVID-19 induced neuropathy
05

Safety considerations

HeadacheDiarrheaPotential for excitotoxicity
06

Interacting drugs

NA-831

4 more in the full profile.

07

Biomarkers

Brain-derived neurotrophic factor (BDNF)Doublecortin (DCX)ADAS-Cog-13 scoreMMSE scoreCDR-SB

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