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
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)
0253 (R)-AMPA
Inactive isomer 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
Subtype-selective AMPA agonist (GluR1 and GluR2)
1543 (S)-CPW 399
Subtype-selective weakly desensitizing AMPA agonist
3840 NPEC-caged-(S)-AMPA
Caged (S)-AMPA
0188 L-Quisqualic acid
AMPA/group I mGlu agonist

Antagonists

Cat No Product Name / Activity
1082 CFM-2
Non-competitive AMPA antagonist
0190 CNQX
Potent AMPA/kainate antagonist
1045 CNQX disodium salt
Potent AMPA/kainate antagonist. More water soluble form of CNQX (Cat. No. 0190)
2932 CP 465022 hydrochloride
Selective, non-competitive AMPA antagonist
0189 DNQX
Selective non-NMDA antagonist
2312 DNQX disodium salt
Selective non-NMDA antagonist. Water-soluble salt of DNQX (Cat. No. 0189)
0845 Evans Blue tetrasodium salt
AMPA/kainate antagonist
3099 GYKI 47261 dihydrochloride
Non-competitive AMPA antagonist
1454 GYKI 52466 dihydrochloride
Selective non-competitive AMPA antagonist
2555 GYKI 53655 hydrochloride
Non-competitive AMPA receptor antagonist
4198 IEM 1925 dihydrobromide
Voltage- and use-dependent open-channel antagonist of AMPA receptors
2766 Naspm trihydrochloride
Ca2+-permeable AMPA receptor 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
GluR1 and GluR3 AMPA receptor antagonist
0961 SYM 2206
Non-competitive AMPA antagonist
5032 Talampanel
Non-competitive AMPA/kainate antagonist
1765 UBP 282
AMPA/kainate antagonist; distinguishes between motoneuron and dorsal root kainate receptors
2701 YM 90K hydrochloride
Selective AMPA antagonist
2345 ZK 200775
Competitive AMPA/kainate antagonist

Modulators

Cat No Product Name / Activity
4373 CMPDA
Positive allosteric modulator of GluR2 receptors
2980 CX 546
AMPA receptor potentiator
5149 CX 614
AMPAkine; positive allosteric modulator of AMPA
0713 Cyclothiazide
AMPA selective desensitization inhibitor
6278 JNJ 55511118
Selective, high affinity negative modulator of AMPA receptors containing TARP-γ8
5297 LY 404187
Selective AMPA receptor positive allosteric modulator
2929 PEPA
Allosteric potentiator of AMPA receptor desensitization
4900 PF 4778574
Positive allosteric modulator of AMPA receptors
3911 S 18986
Positive allosteric modulator of AMPA

Inhibitors

Cat No Product Name / Activity
0867 Aniracetam
Desensitization inhibitor (AMPA > kainate)
1219 IDRA 21
Inhibits AMPA receptor desensitization
1600 pep2-AVKI
Peptide inhibitor of GluR2 subunit binding to PICK1
1599 pep2-EVKI
Peptide inhibitor of GluR2 subunit binding to PICK1
1597 pep2-SVKI
Peptide inhibitor of GluR2 subunit binding to GRIP, ABP and PICK1. Increases AMPA current amplitude
1595 pep2m
Peptide inhibitor of GluR2 subunit binding to NSF. Reduces AMPA currents
3801 Pep2m, myristoylated
Myristoylated form of pep2m (Cat. No. 1595). Peptide inhibitor of GluR2 subunit binding to NSF

Blockers

Cat No Product Name / Activity
1636 IEM 1460
Open-channel blocker of AMPA currents; selective for non-GluR2-containing receptors
4199 IEM 1754 dihydrobromide
Voltage-dependent, open-channel blocker of AMPA currents

Ligand-sets

Cat No Product Name / Activity
1822 AMPA Receptor Tocriset™
Selection of 5 AMPA receptor ligands (Cat. Nos. 0254, 0306, 1044, 0713 and 1454)

Other

Cat No Product Name / Activity
1048 1-BCP
Modulates AMPA-mediated responses
2334 D15
Endocytosis blocker, impairs AMPA receptor cycling
0964 Diazoxide
Blocks desensitization of AMPA receptors
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
GluR1 subunit C-terminus peptide analog. Analog of Pep1-TGL (Cat. No. 1601)
1601 Pep1-TGL
GluR1 subunit C-terminus peptide analog
1598 pep2-SVKE
Inactive control peptide for pep2-SVKI (Cat. No. 1597)
1596 pep4c
Inactive control peptide for pep2m (Cat. No. 1595)
2973 Piracetam
Nootropic; modulates Na+-flux at 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 in the CNS and play a key role in hippocampal synaptic long-term potentiation (LTP) and depression (LTD).

AMPA receptors consist of GluR1-4 subunits which assemble as homomers or heteromers to form functional AMPA receptors. The subunit composition determines the physiological properties of AMPA receptors: those containing the GluR2 subunit show low permeability to Ca2+ whereas those lacking this subunit show high Ca2+ permeability.

External sources of pharmacological information for AMPA Receptors :

    Literature for AMPA Receptors

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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