ArticleMolecular pharmacology2011
Structural and functional analysis of two new positive allosteric modulators of GluA2 desensitization and deactivation.
Article in Molecular pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed.
- Computational Identification of Blood-Brain Barrier-Permeant Microbiome Metabolites with Binding Affinity to Neurotransmitter Receptors in Neurodevelopmental Disorders.Molecules (Basel, Switzerland) · 2026Article
- Positive AMPA and Kainate Receptor Modulators and Their Therapeutic Potential in CNS Diseases: A Comprehensive Review.International journal of molecular sciences · 2025Review
- DART.2: bidirectional synaptic pharmacology with thousandfold cellular specificity.Nature methods · 2024Article
- A Novel Phenylpyrrolidine Derivative: Synthesis and Effect on Cognitive Functions in Rats with Experimental Ishemic Stroke.Molecules (Basel, Switzerland) · 2021Article
- Structure, Function, and Pharmacology of Glutamate Receptor Ion Channels.Pharmacological reviews · 2021Review
- Bivalent AMPA receptor positive allosteric modulators of the bis(pyrimidine) series.MedChemComm · 2019Article
- Unitary Properties of AMPA Receptors with Reduced Desensitization.Biophysical journal · 2017Article
- Pharmacological characterisation of S 47445, a novel positive allosteric modulator of AMPA receptors.PloS one · 2017Article
- Replenishing the cyclic-di-AMP pool: regulation of diadenylate cyclase activity in bacteria.Current genetics · 2016Review
- Ampakine CX717 potentiates intermittent hypoxia-induced hypoglossal long-term facilitation.Journal of neurophysiology · 2016Article
- Kinetic contributions to gating by interactions unique to N-methyl-D-aspartate (NMDA) receptors.The Journal of biological chemistry · 2015Article
- AMPA receptor potentiators: from drug design to cognitive enhancement.Current opinion in pharmacology · 2015Review
- Novel bivalent positive allosteric modulators of AMPA receptor.Doklady. Biochemistry and biophysics · 2015Article
- The multifaceted subunit interfaces of ionotropic glutamate receptors.The Journal of physiology · 2015Review
- Functional insight into development of positive allosteric modulators of AMPA receptors.Neuropharmacology · 2014Article
- A charge-inverting mutation in the "linker" region of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors alters agonist binding and gating kinetics independently of allosteric modulators.The Journal of biological chemistry · 2014Article
- A combined bioinformatics and chemoinformatics approach for developing asymmetric bivalent AMPA receptor positive allosteric modulators as neuroprotective agents.ChemMedChem · 2013Article
- Functional insights from glutamate receptor ion channel structures.Annual review of physiology · 2013Review
- Functional analysis of a novel positive allosteric modulator of AMPA receptors derived from a structure-based drug design strategy.Neuropharmacology · 2013Article
Corrections and comments
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5 authors.
Funding
Abstract
At the dimer interface of the extracellular ligand-binding domain of α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors a hydrophilic pocket is formed that is known to interact with two classes of positive allosteric modulators, represented by cyclothiazide and the ampakine 2H,3H,6aH-pyrrolidino(2,1-3',2')1,3-oxazino(6',5'-5,4)benzo(e)1,4-dioxan-10-one (CX614). Here, we present structural and functional data on two new positive allosteric modulators of AMPA receptors, phenyl-1,4-bis-alkylsulfonamide (CMPDA) and phenyl-1,4-bis-carboxythiophene (CMPDB). Crystallographic data show that these compounds bind within the modulator-binding pocket and that substituents of each compound overlap with distinct moieties of cyclothiazide and CX614. The goals of the present study were to determine 1) the degree of modulation by CMPDA and CMPDB of AMPA receptor deactivation and desensitization; 2) whether these compounds are splice isoform-selective; and 3) whether predictions of mechanism of action could be inferred by comparing molecular interactions between the ligand-binding domain and each compound with those of cyclothiazide and CX614. CMPDB was found to be more isoform-selective than would be predicted from initial binding assays. It is noteworthy that these new compounds are both more potent and more effective and may be more clinically relevant than the AMPA receptor modulators described previously.
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