Regular ArticleModulating Excitatory Synaptic Neurotransmission: Potential Treatment for Neurological Disease?☆
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Role of the AMPA receptor in antidepressant effects of ketamine and potential of AMPA receptor potentiators as a novel antidepressant
2023, NeuropharmacologyCitation Excerpt :The combination of flip and flop splice variants, RNA editing, and changes in the number and subtype of receptor subunits provides a wide range of diversity and flexibility in the construction of AMPA-Rs. AMPA-R agonists, which can non-selectively activate resting AMPA-Rs, have been shown to induce AMPA-R desensitization and seizures (Beattie et al., 2000; Ehlers, 2000; Shaffer et al., 2013; Yamada, 1998). Thus, AMPA-R potentiators can have better pharmacological profiles with the selective promotion of physiological AMPA-R activation.
TAK-653, an AMPA receptor potentiator with minimal agonistic activity, produces an antidepressant-like effect with a favorable safety profile in rats
2021, Pharmacology Biochemistry and BehaviorCitation Excerpt :Thus, AMPAR could be a promising drug target for the treatment of TRD. AMPAR activators—including AMPAR agonists and AMPAR potentiators—have some limitations such as insufficient potency, the risk of seizure, and bell-shaped dose–response (Bai et al., 2003; Beattie et al., 2000; Bernard et al., 2010; Ehlers, 2000; Fowler et al., 2004; Yamada, 1998). For example, several AMPAR potentiators, such as CX516, CX691, CX717, Org26576, LY451395, S18986, and S47445, have been clinically evaluated for neuropsychiatric indications, including cognitive impairment associated with Alzheimer's disease or schizophrenia, depressive symptoms, and attention-deficit/hyperactivity disorder (Kadriu et al., 2021).
Zinc Modulates Olfactory Bulb Kainate Receptors
2020, NeuroscienceNeuronal TDP-43 depletion affects activity-dependent plasticity
2019, Neurobiology of DiseaseLarge Scale Synthesis of an Ampakine-type Active Pharmaceutical Ingredient Based on a Telescoped Regioselective Double Amidation Reaction
2019, Organic Process Research and DevelopmentMechanisms of zinc modulation of olfactory bulb AMPA receptors
2019, NeuroscienceCitation Excerpt :However, in the 16 cells with AMPAR-mediated currents inhibited by 1 mM zinc, there was no significant correlation between the degree of inhibition and the S:P ratio (N = 16; Pearson's r = − 0.05413, P = 0.8422) (Fig. 3B). Cyclothiazide (CTZ) is a drug that inhibits AMPAR desensitization (Yamada and Tang, 1993; Yamada, 1998). Yamada and Tang (1993) reported that CTZ (0.3–100 μM) reduced desensitization of whole-cell currents activated by quisqualate in a concentration-dependent manner (Yamada and Tang, 1993).
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M. G. PalfreymanI. J. ReynoldsP. Skolnick
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E-mail: [email protected]