Structure-activity relationships of dually-acting acetylcholinesterase inhibitors derived from tacrine on N-methyl-d-Aspartate receptors.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113434
Abstract: Tacrine is a classic drug whose efficacy against neurodegenerative diseases is still shrouded in mystery. It seems that besides its inhibitory effect on cholinesterases, the clinical benefit is co-determined by NMDAR-antagonizing activity. Our previous data… read more here.
Keywords: glun1 glun2a; glun1 glun2b; glun1; structure activity ... See more keywords
Allosteric Interactions between NMDA Receptor Subunits Shape the Developmental Shift in Channel Properties
Sign Up to like & getrecommendations! Published in 2017 at "Neuron"
DOI: 10.1016/j.neuron.2017.03.018
Abstract: During development of the central nervous system, there is a shift in the subunit composition of NMDA receptors (NMDARs) resulting in a dramatic acceleration of NMDAR-mediated synaptic currents. This shift coincides with upregulation of the… read more here.
Keywords: shift; glun1 nmdars; interactions nmda; nmda receptor ... See more keywords
Triheteromeric GluN1/GluN2A/GluN2C NMDARs with Unique Single-Channel Properties Are the Dominant Receptor Population in Cerebellar Granule Cells
Sign Up to like & getrecommendations! Published in 2018 at "Neuron"
DOI: 10.1016/j.neuron.2018.06.010
Abstract: NMDA-type glutamate receptors (NMDARs) are ligand-gated ion channels that mediate excitatory neurotransmission in the CNS. Here we describe functional and single-channel properties of triheteromeric GluN1/GluN2A/GluN2C receptors, which contain two GluN1, one GluN2A, and one GluN2C… read more here.
Keywords: glun1 glun2a; glun1; glun2c receptors; glun2a glun2c ... See more keywords
GluN1 deletions in D1- and A2A-expressing cell types reveal distinct modes of behavioral regulation
Sign Up to like & getrecommendations! Published in 2017 at "Neuropharmacology"
DOI: 10.1016/j.neuropharm.2016.03.026
Abstract: ABSTRACT N‐methyl‐d‐aspartate receptors (NMDARs) are profound regulators of glutamate neurotransmission and behavior. To coordinate components of the limbic system, the dorsal and ventral striatum integrate cognitive and emotional information towards the execution of complex behaviors.… read more here.
Keywords: glun1 mice; glun1; a2a glun1; mice ... See more keywords
7-Methoxyderivative of tacrine is a ‘foot-in-the-door’ open-channel blocker of GluN1/GluN2 and GluN1/GluN3 NMDA receptors with neuroprotective activity in vivo
Sign Up to like & getrecommendations! Published in 2018 at "Neuropharmacology"
DOI: 10.1016/j.neuropharm.2018.08.010
Abstract: Abstract N‐methyl‐d‐aspartate receptors (NMDARs) are ionotropic glutamate receptors that mediate excitatory neurotransmission in the mammalian central nervous system (CNS), and their dysregulation results in the aetiology of many CNS syndromes. Several NMDAR modulators have been… read more here.
Keywords: door open; open channel; glun1; meota ... See more keywords
Derivatives of (R)-3-(5-Furanyl)carboxamido-2-aminopropanoic Acid as Potent NMDA Receptor Glycine Site Agonists with GluN2 Subunit-Specific Activity.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01810
Abstract: NMDA receptors mediate glutamatergic neurotransmission and are therapeutic targets due to their involvement in a variety of psychiatric and neurological disorders. Here, we describe the design and synthesis of a series of (R)-3-(5-furanyl)carboxamido-2-aminopropanoic acid analogues… read more here.
Keywords: furanyl carboxamido; glun1; carboxamido aminopropanoic; activity ... See more keywords
Alternative splicing of GluN1 gates glycine site–dependent nonionotropic signaling by NMDAR receptors
Sign Up to like & getrecommendations! Published in 2021 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2026411118
Abstract: Significance N-methyl-D-aspartate receptors (NMDARs), which are critical in the brain, are increasingly being shown to signal without ion flux (i.e., “metabotropically”). What controls the metabotropic function of NMDARs is unknown. We discovered that a form… read more here.
Keywords: nonionotropic signaling; glun1; site; alternative splicing ... See more keywords
Different modes of synaptic and extrasynaptic NMDA receptor alteration in the hippocampus of P301S tau transgenic mice
Sign Up to like & getrecommendations! Published in 2022 at "Brain Pathology"
DOI: 10.1111/bpa.13115
Abstract: N‐methyl‐d‐aspartate receptors (NMDARs) are pivotal players in the synaptic transmission and synaptic plasticity underlying learning and memory. Accordingly, dysfunction of NMDARs has been implicated in the pathophysiology of Alzheimer disease (AD). Here, we used histoblot… read more here.
Keywords: density; pathology; hippocampus p301s; p301s mice ... See more keywords
The C-terminus of NMDAR GluN1-1a Subunit Translocates to Nucleus and Regulates Synaptic Function
Sign Up to like & getrecommendations! Published in 2018 at "Frontiers in Cellular Neuroscience"
DOI: 10.3389/fncel.2018.00334
Abstract: NMDARs, the Ca2+ permeable channels, play central roles in synaptic plasticity, brain development, learning, and memory. NMDAR binding partners and associated signaling has been extensively studied in synapse-to-nucleus communications. However, whether NMDARs could directly regulate… read more here.
Keywords: glun1 terminus; terminus; terminus nmdar; synaptic transmission ... See more keywords
Identification of a Subtype-Selective Allosteric Inhibitor of GluN1/GluN3 NMDA Receptors
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2022.888308
Abstract: N-methyl-D-aspartate receptors (NMDARs) are Ca2+-permeable ionotropic glutamate receptors (iGluRs) in the central nervous system and play important roles in neuronal development and synaptic plasticity. Conventional NMDARs, which typically comprise GluN1 and GluN2 subunits, have different… read more here.
Keywords: glun3 containing; glun1 glun3; inhibitor glun1; glun1 ... See more keywords
Binding and Dynamics Demonstrate the Destabilization of Ligand Binding for the S688Y Mutation in the NMDA Receptor GluN1 Subunit
Sign Up to like & getrecommendations! Published in 2023 at "Molecules"
DOI: 10.3390/molecules28104108
Abstract: Encephalopathies are brain dysfunctions that lead to cognitive, sensory, and motor development impairments. Recently, the identification of several mutations within the N-methyl-D-aspartate receptor (NMDAR) have been identified as significant in the etiology of this group… read more here.
Keywords: mutations within; ligand binding; ligand; mutation ... See more keywords