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References from Therapeutic potential of positive allosteric modulators of AMPA receptors in brain disorders. Local targets link to admitted publications; unresolved targets remain external evidence.
Architecture and subunit arrangement of native AMPA receptors elucidated by cryo-EM
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Structure, Function, and Pharmacology of Glutamate Receptor Ion Channels
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Flip and flop: a molecular determinant for AMPA receptor channel opening
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Glutamate receptors as regulators of synaptic plasticity in neuropsychiatric disorders: pathological insight and translational perspectives
10.1007/s11571-026-10446-y · 2026 · External reference
Amplification of the therapeutic potential of AMPA receptor potentiators from the nootropic era to today
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Randomized phase III study 306
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AMPA/kainate antagonist LY293558 reduces capsaicin-evoked hyperalgesia but not pain in normal skin in humans
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Positive α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Modulators Have Different Impact on Synaptic Transmission in the Thalamus and Hippocampus
10.1124/jpet.104.078196 · 2005 · External reference
AMPA receptor modulators have different impact on hippocampal pyramidal cells and interneurons
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Recovery from AMPA Receptor Potentiation by Ampakines
10.3390/futurepharmacol5020027 · 2025 · External reference
The waveform of synaptic transmission at hippocampal synapses is not determined by AMPA receptor desensitization
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High Impact AMPAkines Induce a Gq-Protein Coupled Endoplasmic Calcium Release in Cortical Neurons: A Possible Mechanism for Explaining the Toxicity of High Impact AMPAkines
10.1002/syn.22310 · 2024 · External reference
Positive Allosteric Modulation of AMPA Receptors from Efficacy to Toxicity: The Interspecies Exposure-Response Continuum of the Novel Potentiator PF-4778574
10.1124/jpet.113.204735 · 2013 · External reference
Pharmacology of Ampakine Modulators: From AMPA Receptors to Synapses and Behavior
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Brain Vacuolation Resulting From Administration of the Type II Ampakine CX717 Is An Artifact Related to Molecular Structure and Chemical Reaction With Tissue Fixative Agents
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Strictly regulated agonist-dependent activation of AMPA-R is the key characteristic of TAK-653 for robust synaptic responses and cognitive improvement
2021 · External reference
Modulation of AMPA receptor kinetics differentially influences synaptic plasticity in the hippocampus
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A profile of the behavioral changes produced by facilitation of AMPA-type glutamate receptors
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Positive AMPA Receptor Modulation Rapidly Stimulates BDNF Release and Increases Dendritic mRNA Translation
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Effects of chronic systemic low-impact ampakine treatment on neurotrophin expression in rat brain
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Brain-derived neurotrophic factor promotes long-term potentiation-related cytoskeletal changes in adult hippocampus
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Facilitative effects of the ampakine CX516 on short-term memory in rats: correlations with hippocampal neuronal activity
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Facilitation of olfactory learning by a modulator of AMPA receptors
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Evaluation of the pro-cognitive effects of the AMPA receptor positive modulator, 5-(1-piperidinylcarbonyl)-2,1,3-benzoxadiazole (CX691), in the rat
10.1007/s00213-008-1325-2 · 2009 · External reference
Effects of an AMPA receptor modulator on methamphetamine-induced hyperactivity in rats
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Enhancement by an ampakine of memory encoding in humans
10.1006/exnr.1997.6581 · 1997 · External reference
Evidence that a positive modulator of AMPA-type glutamate receptors improves delayed recall in aged humans
10.1006/exnr.1997.6447 · 1997 · External reference
Acute effects of the ampakine farampator on memory and information processing in healthy elderly volunteers
10.1038/sj.npp.1301257 · 2007 · External reference
Effect of CX516, an AMPA-modulating compound, on cognition and behavior in fragile X syndrome: a controlled trial
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AMPA potentiator treatment of cognitive deficits in Alzheimer disease
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Low-impact ampakine CX717 exhibits promising therapeutic profile in adults with ADHD - A phase 2A clinical trial
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Safety, Tolerability, and Pharmacokinetic Profile of the Low-Impact Ampakine CX1739 in Young Healthy Volunteers
10.1002/cpdd.1475 · 2025 · External reference
Low-Impact Ampakine CX1739 Exerts Pro-Cognitive Effects and Reverses Opiate-Induced Respiratory Depression in Rodents
10.3390/futurepharmacol4010012 · 2024 · External reference
Acute ampakines increase voiding function and coordination in a rat model of SCI
10.7554/elife.89767 · 2024 · External reference
Central nervous system effects of TAK-653, an investigational alpha-amino-3-hydroxy-5-methyl-4-isoxazole receptor (AMPAR) positive allosteric modulator in healthy volunteers
10.1038/s41398-022-02148-w · 2022 · External reference
Examination of Org 26576, an AMPA receptor positive allosteric modulator, in patients diagnosed with major depressive disorder: an exploratory, randomized, double-blind, placebo-controlled trial
10.1177/0269881112458728 · 2012 · External reference
Synaptic failure and α-synuclein
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Amyloid-β Induces AMPA receptor ubiquitination and degradation in primary neurons and human brains of Alzheimer’s disease
10.3233/jad-170879 · 2018 · External reference
Pharmacological characterisation of S 47445, a novel positive allosteric modulator of AMPA receptors
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The AMPA receptor positive allosteric modulator S 47445 rescues in vivo CA3-CA1 long-term potentiation and structural synaptic changes in old mice
10.1016/j.neuropharm.2017.06.009 · 2017 · External reference
Upregulation of neurotrophins by S 47445, a novel positive allosteric modulator of AMPA receptors in aged rats
10.1016/j.phrs.2017.04.019 · 2017 · External reference
S 47445 Produces antidepressant- and anxiolytic-like effects through neurogenesis dependent and independent mechanisms
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Anti-GluA3 autoantibodies define a new sub-population of frontotemporal lobar degeneration patients with distinct neuropathological features
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A 24-week double-blind placebo-controlled study of the efficacy and safety of the AMPA modulator S47445 in patients with mild to moderate Alzheimer’s disease and depressive symptoms
10.1016/j.trci.2019.04.002 · 2019 · External reference
CX691, as an AMPA receptor positive modulator, improves the learning and memory in a rat model of Alzheimer’s disease
2018 · External reference
Mibampator (LY451395) randomized clinical trial for agitation/aggression in Alzheimer’s disease
10.1017/s1041610212002141 · 2013 · External reference
Benzamide-type AMPA receptor modulators form two subfamilies with distinct modes of action
10.1124/jpet.102.040360 · 2002 · External reference
Positive Modulation of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid-Type Glutamate Receptors Elicits Neuroprotection after Trimethyltin Exposure in Hippocampus
10.1006/taap.2002.9534 · 2002 · External reference
Ampakine CX516 ameliorates functional deficits in AMPA receptors in a hippocampal slice model of protein accumulation
10.1016/j.expneurol.2008.07.010 · 2008 · External reference
CX-516 Cortex pharmaceuticals
2002 · External reference
Randomized, double-blind, placebo-controlled international clinical trial of the Ampakine CX516 in elderly participants with mild cognitive impairment: a progress report
10.1007/s12031-002-0032-4 · 2002 · External reference
Cognitive impairment in early-stage non-demented Parkinson’s disease patients
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10.1002/mds.26424 · 2015 · External reference
Parkinson’s disease
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Extrasynaptic NMDARs oppose synaptic NMDARs by triggering CREB shut-off and cell death pathways
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Opposing role of synaptic and extrasynaptic NMDA receptors in regulation of the extracellular signal-regulated kinases (ERK) activity in cultured rat hippocampal neurons
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Treatment of Parkinson’s disease with biologics that penetrate the blood-brain barrier via receptor-mediated transport
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Pharmacological effects of AMPA receptor potentiators LY392098 and LY404187 on rat neuronal AMPA receptors in vitro
10.1016/s0028-3908(01)00040-5 · 2001 · External reference
Potentiation of responses to AMPA on central neurones by LY392098 and LY404187 in vivo
10.1016/s0028-3908(01)00031-4 · 2001 · External reference
LY404187, a potentiator of AMPARs, enhances both the amplitude and 1/CV2 of AMPA EPSCs but not NMDA EPSCs at CA3–CA1 synapses in the hippocampus of neonatal rats
10.1016/j.neulet.2012.10.020 · 2012 · External reference
An AMPA receptor potentiator modulates hippocampal expression of BDNF: an in vivo study
10.1016/s0028-3908(02)00066-7 · 2002 · External reference
Novel AMPA receptor potentiators LY392098 and LY404187: effects on recombinant human AMPA receptors in vitro
10.1016/s0028-3908(01)00027-2 · 2001 · External reference
Neurotrophic actions of the novel AMPA receptor potentiator, LY404187, in rodent models of Parkinson’s disease
10.1016/j.ejphar.2003.12.023 · 2004 · External reference
LY503430: Pharmacology, Pharmacokinetics, and Effects in Rodent Models of Parkinson’s Disease
10.1111/j.1527-3458.2005.tb00037.x · 2005 · External reference
LY503430, a Novel α-Amino-3-hydroxy-5-methylisoxazole-4-propionic Acid Receptor Potentiator with Functional, Neuroprotective and Neurotrophic Effects in Rodent Models of Parkinson’s Disease
10.1124/jpet.103.049445 · 2003 · External reference
Pharmacological Characterization of cGMP Regulation by the Biarylpropylsulfonamide Class of Positive, Allosteric Modulators of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid Receptors
10.1124/jpet.106.105734 · 2006 · External reference
AMPA receptor blockade improves levodopa-induced dyskinesia in MPTP monkeys
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Pharmacological modulation of respiratory control: Ampakines as a therapeutic strategy
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BDNF mediates the neuroprotective effects of positive AMPA receptor modulators against MPP+-induced toxicity in cultured hippocampal and mesencephalic slices
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Ampakine CX614 increases respiratory rate in a mouse model of Parkinson’s disease
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Huntingtin Controls Neurotrophic Support and Survival of Neurons by Enhancing BDNF Vesicular Transport along Microtubules
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Brain-derived neurotrophic factor in Huntington disease
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Modulation of AMPA receptor surface diffusion restores hippocampal plasticity and memory in Huntington’s disease models
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Transcranial magnetic stimulation as a translational biomarker for AMPA receptor modulation
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Dynamics of AMPA receptors regulate epileptogenesis in patients with epilepsy
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Characterization of patients with major psychiatric disorders with AMPA receptor positron emission tomography
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The dynamics of AMPA receptors underlies the efficacy of ketamine in treatment resistant patients with depression
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