AMPA Receptors

AMPA receptors are members of the ionotropic class of glutamate receptors, which also includes NMDA and Kainate receptors. AMPA receptors mediate fast excitatory synaptic transmission and play a role in hippocampal synaptic long-term potentiation and depression.

Products
Background
Literature (10)
Gene Data

Agonists

Cat. No. Product Name / Activity
1074 (RS)-AMPA hydrobromide
Selective AMPA agonist; more water soluble form of (RS)-AMPA (Cat. No. 0169)
0169 (RS)-AMPA
Selective AMPA agonist
0254 (S)-AMPA
Selective AMPA agonist; active isomer of (RS)-AMPA (Cat. No. 0169)
1673 Cl-HIBO
GluA1 and GluA2 selective AMPA agonist
3840 NPEC-caged-(S)-AMPA
Caged (S)-AMPA
0188 L-Quisqualic acid
AMPA agonist; also group I mGlu agonist

Antagonists

Cat. No. Product Name / Activity
1082 CFM-2
Non-competitive AMPA antagonist
0190 CNQX
Potent and selective non-NMDA iGluR antagonist
1045 CNQX disodium salt
Potent non-NMDA iGluR antagonist; more water soluble form of CNQX (Cat. No. 0190)
2932 CP 465022 hydrochloride
Selective and non-competitive AMPA antagonist
0189 DNQX
Selective non-NMDA iGluR antagonist
2312 DNQX disodium salt
Selective non-NMDA iGluR antagonist; water-soluble salt of DNQX (Cat. No. 0189)
0845 Evans Blue tetrasodium salt
Non-NMDA iGluR antagonist; P2X antagonist; also inhibits L-glutamate uptake into synaptic vesicles
3099 GYKI 47261 dihydrochloride
Non-competitive AMPA antagonist
1454 GYKI 52466 dihydrochloride
Selective non-competitive AMPA antagonist
2555 GYKI 53655 hydrochloride
Non-competitive non-NMDA iGluR antagonist
4198 IEM 1925 dihydrobromide
Voltage- and use-dependent open-channel AMPA blocker
2766 Naspm trihydrochloride
Ca2+-permeable AMPA antagonist
0373 NBQX
Potent AMPA antagonist; more selective than CNQX (Cat. No. 0190)
1044 NBQX disodium salt
Potent AMPA antagonist; more water soluble form of NBQX (Cat. No. 0373)
2770 Philanthotoxin 74
GluA1 and GluA3 selective AMPA antagonist
5032 Talampanel
Non-competitive non-NMDA iGluR antagonist
2701 YM 90K hydrochloride
Selective AMPA antagonist
2345 ZK 200775
Competitive non-NMDA iGluR antagonist

Modulators

Cat. No. Product Name / Activity
4373 CMPDA
Positive allosteric modulator of GluA2 receptors
2980 CX 546
AMPA potentiator
5149 CX 614
Positive allosteric modulator of AMPA receptors
0713 Cyclothiazide
Positive allosteric modulator of AMPA receptors; inhibits AMPA desensitization
6278 JNJ 55511118
High affinity and selective negative modulator of AMPA receptors containing TARP-γ8
5297 LY 404187
Selective positive allosteric modulator of AMPA receptors
3911 S 18986
Positive allosteric modulator of AMPA receptors
6353 UoS 12258
Positive allosteric modulator of AMPA receptors

Inhibitors

Cat. No. Product Name / Activity
0867 Aniracetam
Inhibits desensitization; AMPA > kainate
1219 IDRA 21
Inhibits AMPA desensitization
1600 pep2-AVKI
Peptide inhibitor of GluA2 subunit binding to PICK1
1599 pep2-EVKI
Peptide inhibitor of GluA2 subunit binding to PICK1
1597 pep2-SVKI
Peptide inhibitor of GluA2 subunit binding to GRIP, ABP and PICK1; increases AMPA current amplitude
3801 Pep2m, myristoylated
Peptide inhibitor of GluA2 subunit binding to NSF; myristoylated form of pep2m (Cat. No. 1595).

Blockers

Cat. No. Product Name / Activity
1636 IEM 1460
Open-channel blocker of AMPA currents; selective for non-GluA2-containing receptors
4199 IEM 1754 dihydrobromide
Voltage-dependent, open-channel AMPA blocker

Other

Cat. No. Product Name / Activity
0964 Diazoxide
Inhibits AMPA desensitization
6094 2R,6R-Hydroxynorketamine hydrochloride
Ketamine metabolite; enhances AMPA currents; lacks ketamine-related side effects
6095 2S,6S-Hydroxynorketamine hydrochloride
Ketamine metabolite; decreases D-serine (a NMDA co-agonist); antidepressant
5982 cis-6-Hydroxynorketamine hydrochloride
Metabolite of ketamine (Cat.No. 3131); enhances AMPA currents
1602 Pep1-AGL
GluA1 subunit C-terminus peptide analog; also analog of Pep1-TGL (Cat. No. 1601)
1601 Pep1-TGL
GluA1 subunit C-terminus peptide analog
1596 pep4c
Inactive control peptide for pep2m (Cat. No. 1595)
2973 Piracetam
Modulates Na+-flux at AMPA receptors; nootropic
6847 TAT-GluA2 3Y
Inhibitor of AMPA receptor endocytosis

AMPA receptors are cation-permeable, ligand-gated ion channels. Like other members of this family, AMPA receptors are named based on a compound that was found to be selective for these receptors; α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA). They consist of GluA1-4 subunits that assemble as homomers or heteromers to form functional receptors. Each subunit is encoded by a different gene, and alternative versions of the subunits may be produced by gene splicing. There is a large heterogeneity within the exact subunit conformation of endogenous AMPA receptors, with brain region specific expression seen for some splice variants.

The subunit composition of an AMPA receptor determines its physiological properties, in particular the extent to which these ion channels are permeable to Ca2+. Calcium permeability can be traced to a single amino acid residue within the re-entrant loop of subunit GluA2, termed the Q/R site. In GluA1, A3 and A4 subunits a glutamine (Q) is found at this site, however in the GluA2 subunit an arginine (R) is present, due to post-translation modification. AMPA receptors containing a GluA2 subunit are relatively impermeable to Ca2+, while receptors lacking this subunit are highly Ca2+ permeable. This site also regulates single channel conductance of AMPA receptors, and their sensitivity to some toxins.

AMPA receptors play a key role in synaptic plasticity, particularly in long-term potentiation (LTP), which is thought to be the cellular correlate of learning and memory. LTP describes an increase in excitatory postsynaptic potential (EPSP) size, which starts when glutamate binds to postsynaptic AMPA and NMDA receptors. Activation of AMPA receptors by ligand binding leads to opening of the pore and enables Na+ influx into the postsynaptic neuron causing depolarization. Once depolarization is strong enough to displace Mg2+ ions from the ion pore of NMDA receptors, these receptors allow more Na+ and Ca2+ to enter the cell. Entry of Ca2+ results in upregulation of trafficking of AMPA receptors to the membrane, through a CaMKII - Ras - MAPK signaling pathway. Phosphorylation of CaMKII caused by the rise in intracellular Ca2+ in turn phosphorylates AMPA receptors, increasing their single channel conductance.

External sources of pharmacological information for AMPA Receptors :

Literature for AMPA Receptors

Tocris offers the following scientific literature for AMPA Receptors to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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AMPA Receptor Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
GluA1 Human GRIA1 NM_000827 P42261
Mouse Gria1 NM_008165 P23818
Rat Gria1 NM_031608 P19490
GluA2 Human GRIA2 NM_001083620 Q12879
Mouse Gria2 NM_013540 P23819
Rat Gria2 NM_017261 P19491
GluA3 Human GRIA3 NM_000828 P42263
Mouse Gria3 NM_016886 Q9Z2W9
Rat Gria3 NM_032990 P19492
GluA4 Human GRIA4 NM_001077243 P48058
Mouse Gria4 NM_019691 Q9Z2W8
Rat gria4 NM_017263 P19493