AMPA Receptor
AMPA receptors mediate the majority of rapid excitatory synaptic transmission in the CNS[1]. Mechanistically, their activity and synaptic distribution are dynamically regulated and contribute to short- and long-term modification of synaptic efficacy[1]. Subunit structure, stoichiometry, and auxiliary proteins generate heterogeneous AMPA receptor assemblies tailored for fast synaptic signaling and plasticity[2]. In disease-relevant models, calcium-permeable AMPA receptors contribute to synaptic plasticity, learning, excitotoxic cell loss, neurodegeneration, seizures, and memory impairment[3][4]. Compared with related AMPA receptor isoforms, GluA2 is a key determinant because edited GluA2(R)-containing receptors are calcium-impermeable, whereas GluA2-lacking or unedited GluA2(Q)-containing receptors are calcium-permeable[3]. GluA1 and GluA2 also reciprocally modulate spinal synaptic plasticity and inflammatory pain, supporting isoform-focused experimental design[5]. For experimental applications, perampanel provides a selective, orally active, noncompetitive AMPA receptor antagonist that reduces seizure activity in rodent epilepsy models[6].
References:
- [1]. Song I, et al. Regulation of AMPA receptors during synaptic plasticity. Trends Neurosci. 2002 Nov;25(11):578-88. [Content Brief]
- [2]. Greger IH, et al. Structural and Functional Architecture of AMPA-Type Glutamate Receptors and Their Auxiliary Proteins. Neuron. 2017 May 17;94(4):713-730. [Content Brief]
- [3]. Wright A, et al. The essential role of AMPA receptor GluR2 subunit RNA editing in the normal and diseased brain. Front Mol Neurosci. 2012 Apr 11;5:34. [Content Brief]
- [4]. Konen LM, et al. A new mouse line with reduced GluA2 Q/R site RNA editing exhibits loss of dendritic spines, hippocampal CA1-neuron loss, learning and memory impairments and NMDA receptor-independent seizure vulnerability. Mol Brain. 2020 Feb 27;13(1):27. [Content Brief]
- [5]. Hartmann B, et al. The AMPA receptor subunits GluR-A and GluR-B reciprocally modulate spinal synaptic plasticity and inflammatory pain. Neuron. 2004 Nov 18;44(4):637-50. [Content Brief]
- [6]. Hanada T, et al. Perampanel: a novel, orally active, noncompetitive AMPA-receptor antagonist that reduces seizure activity in rodent models of epilepsy. Epilepsia. 2011 Jul;52(7):1331-40. [Content Brief]
All Product Categories
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AMPA Receptor Related Products (114)
Related Products (114)
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Corticosterone
0 ImagesSynonyms: 17-Deoxycortisol; 11β,21-Dihydroxyprogesterone; Kendall's compound BCorticosterone (17-Deoxycortisol) is an orally active and adrenal cortex-produced glucocorticoid, which plays an important role in regulating neuronal functions of the limbic system (including hippocampus, prefrontal cortex, and amygdala). Corticosterone increases the Rab-mediated AMPAR membrane traffic via SGK-induced phosphorylation of GDI. Corticosterone also interferes with the maturation of dendritic cells and shows a good immunosuppressive effect.
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L-Glutamic acid
0 ImagesL-Glutamic acid is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid can be used in the study of neurological diseases. L-Glutamic acid acts at ionotropic and metabotropic glutamate receptors.
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CNQX
0 ImagesSynonyms: FG9065CNQX (FG9065) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX is a competitive non-NMDA receptor antagonist. CNQX blocks the expression of fear-potentiated startle in rats.
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NBQX
0 ImagesSynonyms: FG9202NBQX (FG9202) is a highly selective and competitive AMPA receptor antagonist. NBQX has neuroprotective and anticonvulsant activity.
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L-Glutamic acid monosodium salt
0 ImagesL-Glutamic acid monosodium salt is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid monosodium salt has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid monosodium salt can be used in the study of neurological diseases. L-Glutamic acid monosodium salt acts at ionotropic and metabotropic glutamate receptors.
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TAK-137
0 ImagesCat. No.: HY-204388CAS No.: 1358749-55-9TAK-137 is an AMPA receptor potentiator with weak agonistic effect. TAK-137 binds to the AMPA receptor ligand binding domain in a glutamate-dependent manner. TAK-137 potentiates AMPA-induced currents and Ca2+ influx. TAK-137 can be used for the research of neurological disease.
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EGIS-9637
0 ImagesCat. No.: HY-182410CAS No.: 220669-66-9EGIS-9637 is a non-competitive AMPA antagonist and acylated dihydro-2,3-benzodiazepine class member.
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GYKI 53405
0 ImagesCat. No.: HY-15080CAS No.: 143691-37-6Synonyms: LY 293606GYKI 53405 (LY 293606) is a non-competitive, orally active AMPA receptor antagonist. GYKI 53405 shows no significant binding affinity for GABAA, GABAB or benzodiazepine receptors. GYKI 53405 increases self-grooming behavior, induces wet dog-like shakes, reduces spontaneous activity, produces anxiolytic-like behavior, reverses the anxiogenic effect induced by mCPP, inhibits locomotor activity, suppresses sound-induced and maximal electroshock-induced seizures, prolongs survival in global cerebral ischemia models, and exhibits sustained anticonvulsant effects at doses below the sedation threshold. GYKI 53405 can be used in research related to absence epilepsy, anxiety disorders and global cerebral ischemia.
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Decanoic acid
0 ImagesDecanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy.
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Topiramate
0 ImagesSynonyms: McN 4853; RWJ 17021Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.
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NBQX disodium
0 ImagesSynonyms: FG9202 disodiumNBQX disodium (FG9202 disodium) is a highly selective and competitive AMPA receptor antagonist. NBQX disodium has neuroprotective and anticonvulsant activity.
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(S)-AMPA
0 ImagesSynonyms: L-AMPA(S)-AMPA (L-AMPA), an active S-enantiomer of AMPA, is a potent and selective AMPA receptor agonist.
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CNQX disodium
0 ImagesSynonyms: FG9065 disodiumCNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist. CNQX disodium blocks the expression of fear-potentiated startle in rats.
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L-Glutamic acid-13C5,15N
0 ImagesL-Glutamic acid-13C5,15N is the 13C- and 15N-labeled L-Glutamic acid. L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
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Osavampator
0 ImagesSynonyms: TAK-653; NBI-1065845Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca2+ influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders.
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CX516
0 ImagesSynonyms: BDP 12CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).
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Cyclothiazide
0 ImagesCyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures.
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L-Glutamic acid-13C5
0 ImagesL-Glutamic acid-13C5 is the 13C-labeled L-Glutamic acid. L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
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L-Glutamic acid-d5
0 ImagesL-Glutamic acid-d5 is the deuterium labeled L-Glutamic acid. L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
