Phenol—Benzoxazolone bioisosteres: Synthesis and biological evaluation of tricyclic GluN2B‐selective N‐methyl‐ d‐aspartate receptor antagonists
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DOI: 10.1002/ardp.202200147
Abstract: Tricyclic tetrahydrooxazolo[4,5‐h]‐[3]benzazepin‐9‐ols 22 were designed as phenol bioisosteres of tetrahydro‐3‐benzazepine‐1,7‐diols. Key features of the synthesis are the introduction of the trifluoromethylsulfonyl and allyl protective groups at the heterocyclic N‐atoms. Two methods were developed to convert… read more here.
Keywords: bioisosteres synthesis; glun2b; benzoxazolone bioisosteres; phenol benzoxazolone ... See more keywords
A comprehensive description of GluN2B-selective N-methyl-D-aspartate (NMDA) receptor antagonists.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112447
Abstract: l-glutamate is an excitatory neurotransmitter in the central nervous system (CNS), which can activate ionotropic receptors (iGluRs) and metabotropic (mGluRs) receptors. N-methyl-D-aspartate (NMDA) receptor is a ligand-gated ion channel belonging to the iGluRs family. Among… read more here.
Keywords: methyl aspartate; comprehensive description; glun2b; nmda receptor ... See more keywords
Synthesis and biological evaluation of conformationally restricted GluN2B ligands derived from eliprodil.
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DOI: 10.1016/j.ejmech.2022.114359
Abstract: N-Methyl-d-aspartate (NMDA) receptors containing one or two GluN2B subunits play a crucial role in a variety of neurodegenerative diseases, such as Alzheimer's and Huntington's disease. In order to increase selectivity for GluN2B NMDA receptors, the… read more here.
Keywords: synthesis biological; biological evaluation; conformationally restricted; affinity ... See more keywords
Striatal GluN2B involved in motor skill learning and stimulus-response learning
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DOI: 10.1016/j.neuropharm.2018.03.002
Abstract: &NA; Although the striatum has a well‐documented role in procedural learning and memory, the underlying mechanisms remain poorly understood. GluN2B subunit is abundantly expressed in striatum, however, the function of striatal GluN2B subunit in striatum‐related… read more here.
Keywords: striatal glun2b; glun2b; motor skill; striatum ... See more keywords
Acute stress regulates phosphorylation of N-methyl-d-aspartate receptor GluN2B at S1284 in hippocampus
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DOI: 10.1016/j.neuroscience.2017.03.029
Abstract: Exposure to acute stress leads to diverse changes, which include either beneficial or deleterious effects on molecular levels that are implicated in stress-related disorders. N-methyl-d-aspartate receptor (NMDAR)-mediated signalings, are thought to be vital players in… read more here.
Keywords: methyl aspartate; glun2b; s1284; acute stress ... See more keywords
Age-Dependent Changes in Synaptic NMDA Receptor Composition in Adult Human Cortical Neurons.
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DOI: 10.1093/cercor/bhaa052
Abstract: The molecular processes underlying the aging-related decline in cognitive performance and memory observed in humans are poorly understood. Studies in rodents have shown a decrease in N-methyl-D-aspartate receptors (NMDARs) that contain the GluN2B subunit in… read more here.
Keywords: age dependent; glun2b; adult human; age ... See more keywords
NYX-2925 induces metabotropic NMDAR signaling that enhances synaptic NMDAR and AMPAR.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of neurochemistry"
DOI: 10.1111/jnc.14845
Abstract: N-Methyl-D-Aspartate receptors (NMDARs) mediate both physiological and pathophysiological processes, though selective ligands lack broad clinical utility. NMDARs are composed of multiple subunits, but GluN2 is predominately responsible for functional heterogeneity. Specifically, the GluN2A- and GluN2B-containing… read more here.
Keywords: nmdar signaling; glun2b; synaptic glun2b; nyx 2925 ... See more keywords
Ubiquitination and functional modification of GluN2B subunit–containing NMDA receptors by Cbl-b in the spinal cord dorsal horn
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DOI: 10.1126/scisignal.aaw1519
Abstract: Peripheral inflammation overrides a developmental, ubiquitin-mediated switch limiting neuronal sensitivity. A painful return to developmental NMDAR activity Neuronal sensitivity is mediated, in part, by NMDA receptor (NMDAR) signaling, and increased abundance of GluN2B-containing NMDARs in… read more here.
Keywords: cbl; glun2b; dorsal horn; inflammation ... See more keywords
An autism-associated mutation in GluN2B prevents NMDA receptor trafficking and interferes with dendrite growth
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Cell Science"
DOI: 10.1242/jcs.232892
Abstract: ABSTRACT Autism spectrum disorders (ASDs) are neurodevelopmental disorders with multiple genetic associations. Analysis of de novo mutations identified GRIN2B, which encodes the GluN2B subunit of NMDA receptors, as a gene linked to ASDs with high… read more here.
Keywords: glun2b; nmda receptor; autism; grin2b mutations ... See more keywords
Chemical, pharmacodynamic and pharmacokinetic characterization of the GluN2B receptor antagonist 3-(4-phenylbutyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-1,7-diol – starting point for PET tracer development
Sign Up to like & getrecommendations! Published in 2022 at "Biological Chemistry"
DOI: 10.1515/hsz-2022-0222
Abstract: Abstract GluN2B-NMDA receptors play a key role in several neurological and neurodegenerative disorders. In order to develop novel negative allosteric GluN2B-NMDA receptor modulators, the concept of conformational restriction was pursued, i.e. the flexible aminoethanol substructure… read more here.
Keywords: glun2b; benzazepine diol; tetrahydro benzazepine; glun2b nmda ... See more keywords
The LILI Motif of M3-S2 Linkers Is a Component of the NMDA Receptor Channel Gate
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DOI: 10.3389/fnmol.2018.00113
Abstract: N-methyl-D-aspartate receptors (NMDARs) mediate excitatory synaptic transmission in the central nervous system, underlie the induction of synaptic plasticity, and their malfunction is associated with human diseases. Native NMDARs are tetramers composed of two obligatory GluN1… read more here.
Keywords: glun2b; lili motif; motif linkers; channel ... See more keywords