Systematic variation of the benzoylhydrazine moiety of the GluN2A selective NMDA receptor antagonist TCN-201.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.09.006
Abstract: GluN2A containing N-methyl-D-aspartate receptors (NMDARs) are important ion channels in the central nervous system and highly involved in several different neurophysiological but also neuropathophysiological processes. However, current understanding of the contribution of GluN2A containing NMDARs… read more here.
Keywords: tcn 201; nmda receptor; negative allosteric; moiety ... See more keywords
A lack of GluN2A-containing NMDA receptors confers a vulnerability to redox dysregulation: Consequences on parvalbumin interneurons, and their perineuronal nets
Sign Up to like & getrecommendations! Published in 2018 at "Neurobiology of Disease"
DOI: 10.1016/j.nbd.2017.10.006
Abstract: The GluN2A subunit of NMDA receptors (NMDARs) plays a critical role during postnatal brain development as its expression increases while Glun2B expression decreases. Mutations and polymorphisms in GRIN2A gene, coding for GluN2A, are linked to… read more here.
Keywords: parvalbumin interneurons; glun2a containing; lack glun2a; glun2a ... See more keywords
GluN2A-NMDA receptor inhibition disinhibits the prefrontal cortex, reduces forced swim immobility, and impairs sensorimotor gating.
Sign Up to like & getrecommendations! Published in 2025 at "Acta pharmacologica Sinica"
DOI: 10.1038/s41401-025-01643-2
Abstract: Recent investigations into the rapid antidepressant effects of ketamine, along with studies on schizophrenia-related susceptibility genes, have highlighted the GluN2A subunit as a critical regulator of both emotion and cognition. However, the specific impacts of… read more here.
Keywords: nmda receptor; inhibition; glun2a nmda; glun2a ... See more keywords
Knockdown of astrocytic Grin2a aggravates β‐amyloid‐induced memory and cognitive deficits through regulating nerve growth factor
Sign Up to like & getrecommendations! Published in 2021 at "Aging Cell"
DOI: 10.1111/acel.13437
Abstract: Synapse degeneration correlates strongly with cognitive impairments in Alzheimer's disease (AD) patients. Soluble Amyloid‐beta (Aβ) oligomers are thought as the major trigger of synaptic malfunctions. Our earlier studies have demonstrated that Aβ oligomers interfere with… read more here.
Keywords: nerve growth; growth factor; astrocytic glun2a; glun2a ... See more keywords
Pharmacological characterisation of JNJ‐78911118, a novel, centrally‐penetrant, selective GluN2A antagonist
Sign Up to like & getrecommendations! Published in 2025 at "British Journal of Pharmacology"
DOI: 10.1111/bph.70069
Abstract: Non‐selective NMDA receptor antagonism produces rapid symptom improvement in treatment‐resistant depression; however, associated side effects necessitate medical oversight during administration. We hypothesised that selective GluN2A antagonism could provide similar efficacy with an improved side effect… read more here.
Keywords: characterisation jnj; pharmacology; jnj 78911118; pharmacological characterisation ... See more keywords
Targeted NMDA Receptor Interventions for Autism: Developmentally Determined Expression of GluN2B and GluN2A-Containing Receptors and Balanced Allosteric Modulatory Approaches
Sign Up to like & getrecommendations! Published in 2022 at "Biomolecules"
DOI: 10.3390/biom12020181
Abstract: Various ASD risk alleles have been associated with impairment of NMDA receptor activation (i.e., NMDA Receptor Hypofunction) and/or disturbance of the careful balance between activation mediated by GluN2B-subtype and GluN2A-subtype-containing NMDA receptors. Importantly, although these… read more here.
Keywords: expression; glun2a; receptor activation; nmda receptor ... See more keywords
Synaptic GluN2A-Containing NMDA Receptors: From Physiology to Pathological Synaptic Plasticity
Sign Up to like & getrecommendations! Published in 2020 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms21041538
Abstract: N-Methyl-d-Aspartate Receptors (NMDARs) are ionotropic glutamate-gated receptors. NMDARs are tetramers composed by several homologous subunits of GluN1-, GluN2-, or GluN3-type, leading to the existence in the central nervous system of a high variety of receptor… read more here.
Keywords: physiology pathological; physiology; glun2a; synaptic plasticity ... See more keywords