Glutamate, ionotropic

L-glutamate is the major excitatory neurotransmitter in the central nervous system. The glutamate system represents an attractive molecular target in the treatment of epilepsy, neurodegenerative diseases (Alzheimer’s disease, Parkinson’s disease, Huntington’s chorea), schizophrenia, ischemia, pain, alcoholism and mood disorders[1].
Alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) is an artificial glutamate analogue. Its receptor (originally named quisqualate receptor) is a non-NMDA-type ionotropic transmembrane receptor for glutamate that mediates fast synaptic transmission in the central nervous system. Like all ionotropic glutamate receptors, it consists of tetramers of four different types of subunits (GluR1-GluR4). The AMPA receptor GluA2 (GluR2) tetramer was the first and currently only glutamate receptor ion channel to be crystallized[2].
Kainate, a natural product, is an excitotoxic glutamate analogue produced by an algae, while NMDA is N-methyl-d-aspartate. Although all three glutamate receptor subtypes respond to glutamate, they can be distinguished by their response to these artificial agonists. Their distribution in the brain, physiological function, and mechanism and kinetics of activation and regulation are very different[3]. In two ways, the NMDA receptor is distinct from the other LGICs. First, it is both ligand-gated and voltage-dependent. Second, it requires co-activation by two ligands: glutamate and either d-serine or glycine. What’s more, the receptor controls a cation channel that is highly permeable to multiple monovalent ions and calcium[4]

[1] Molecular structure of ionotropic glutamate receptors. A.A. Kaczor, D. Matosiuk. Curr Med Chem. 2010,17, 2608-2635.
[2] AMPA receptors as drug targets in neurological disease--advantages, caveats, and future outlook. P.K. Chang, D. Verbich, R.A. McKinney. Eur. J. Neurosci. 2012, 35, 1908-1916.
[3] Kainate receptors. P. Pinheiro, C. Mulle. Cell and Tissue Research. 2006, 326, 457-482.
[4] The Role of N-Methyl-D-Aspartate (NMDA) Receptors in Pain: A Review. A.B. Petrenko et al. Anest. Analg. 2003, 97, 1108-1116

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Axon ID Name Description From price
3088 1-BCP Brain-penetrant modulator of AMPA receptor €75.00
3415 AMPA Highly selective AMPA receptor agonist  Recently added €110.00
3335 AZD6765 dihydrochloride Noncompetitive NMDA antagonist €90.00
1217 CFM 2 AMPA antagonist €115.00
2079 CMPDA Positive allosteric modulator of AMPA receptor €85.00
1200 CNQX AMPA/Kainate antagonist €85.00
2522 CNQX disodium salt AMPA/Kainate antagonist €90.00
2254 CP 101606 NMDA NR2B antagonist €120.00
1406 CP 101606 mesylate NMDA NR2B antagonist €85.00
3089 CX516 Positive allosteric modulator of AMPA receptor €70.00
3090 CX546 Positive allosteric modulator of AMPA receptor €95.00
1201 DNQX AMPA/Kainate antagonist €50.00
1246 Eliprodil NMDA antagonist €90.00
2687 Farampator Second-generation ampakine that potentiates AMPA receptor function €99.00
1262 Gavestinel NMDA antagonist (glycine site) €110.00

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