2021年8月5日 · Here the authors show that GluN2A and GluN2B NMDA receptors — the two principal subtypes NMDARs in the adult CNS — operate through distinct long range allosteric mechanisms.

GluN2A and GluN2B are the main types of NMDA receptor subunit in the adult forebrain. Studies have demonstrated that they play different roles in a number of pathophysiological processes.

Glutamate [NMDA] receptor subunit epsilon-2, also known as N-methyl D-aspartate receptor subtype 2B (NMDAR2B or NR2B), is a protein that in humans is encoded by the GRIN2B gene. [5] N -methyl-D-aspartate (NMDA) receptors are a class of ionotropic glutamate receptors.

Unfortunately, the results from studies that have investigated this hypothesis are contradictory, particularly in relation to LTD. Nevertheless, current evidence does suggest that the GluN2B subunit might be particularly important for plasticity and …

2023年6月2日 · Understanding of design rules and roles of GluN2B selective compounds will provide the link to medicinal chemists and neuroscientists to explore novel neurotherapeutic strategies against dysfunctions of glutamatergic neurotransmission.

GluN2B (GluRε2/NR2B) subunit is involved in synapse development, synaptic plasticity, and cognitive function. However, its roles in synaptic expression and function of NMDA receptors (NMDARs) in the brain remain mostly unknown because of the neonatal lethality of …

Glutamate N-methyl-D-aspartate receptor (NMDAR) is critical for promoting physiological synaptic plasticity and neuronal viability. As a major subpopulation of the NMDAR, the GluN2B subunit-containing NMDARs have distinct pharmacological properties, ...

2019年11月15日 · Overactivation leads to high intracellular Ca 2+ concentrations and cell death rendering GluN2B-selective inhibitors as promising drug candidates. Ifenprodil represents the first highly potent...

In this study, we evaluate a novel piperazine-containing GluN2B-selective NMDAR NAM (63,64) for its effects on morphine-induced analgesic tolerance in rodents. We also assess the actions of a class of enantiomeric propanolamines that function as GluN2B-selective NAMs.

Phosphorylation of GluN2B at Ser-1480 by CK2 disrupts PSD-95 binding, leading to a significant reduction of surface and synaptic NMDARs, an important mechanism that plays a role in the GluN2B to GluN2A switch during development (Sanz-Clemente et al., 2010).