Functional characterization of a novel NMDA receptor positive allosteric modulator

V Li - 2017 - open.library.ubc.ca
The NMDA receptor is a glutamatergic ionotropic receptor key in mediating neuronal
plasticity across virtually all synaptic circuits in the brain. An increasing list of neurological …

[PDF][PDF] Structural basis for negative allosteric modulation of GluN2A-containing NMDA receptors

F Yi, TC Mou, KN Dorsett, RA Volkmann, FS Menniti… - Neuron, 2016 - cell.com
NMDA receptors mediate excitatory synaptic transmission and regulate synaptic plasticity in
the central nervous system, but their dysregulation is also implicated in numerous brain …

Di-aryl Sulfonamide Motif Adds π-Stacking Bulk in Negative Allosteric Modulators of the NMDA Receptor

SL Summer, SA Kell, Z Zhu, R Moore… - ACS Medicinal …, 2019 - ACS Publications
The N-methyl-d-aspartate receptor plays a critical role in central nervous system processes.
Its diverse properties, as well as hypothesized role in neurological disease, render NMDA …

Discovery of GluN2A-selective NMDA receptor positive allosteric modulators (PAMs): tuning deactivation kinetics via structure-based design

M Volgraf, BD Sellers, Y Jiang, G Wu… - Journal of medicinal …, 2016 - ACS Publications
The N-methyl-d-aspartate receptor (NMDAR) is a Na+ and Ca2+ permeable ionotropic
glutamate receptor that is activated by the coagonists glycine and glutamate. NMDARs are …

Pharmacological modulation of NMDA receptor activity and the advent of negative and positive allosteric modulators

DT Monaghan, MW Irvine, BM Costa, G Fang… - Neurochemistry …, 2012 - Elsevier
The NMDA receptor (NMDAR) family of l-glutamate receptors are well known to have
diverse roles in CNS function as well as in various neuropathological and psychiatric …

[HTML][HTML] Allosteric inhibitors of NMDA receptor functions

GK Popescu, S Murthy, WF Borschel - Pharmaceuticals, 2010 - mdpi.com
NMDA receptors are glutamate-activated ion-channels involved in many essential brain
functions including learning, memory, cognition, and behavior. Given this broad range of …

[HTML][HTML] A single-channel mechanism for pharmacological potentiation of GluN1/GluN2A NMDA receptors

DA Chopra, K Sapkota, MW Irvine, G Fang, DE Jane… - Scientific reports, 2017 - nature.com
NMDA receptors (NMDARs) contribute to several neuropathological processes. Novel
positive allosteric modulators (PAMs) of NMDARs have recently been identified but their …

[HTML][HTML] Diverse modes of NMDA receptor positive allosteric modulation: Mechanisms and consequences

DH Hackos, JE Hanson - Neuropharmacology, 2017 - Elsevier
NMDA Receptors (NMDARs) play key roles in synaptic physiology and NMDAR
hypofunction has been implicated in various neurological conditions. In recent years an …

A novel binding mode reveals two distinct classes of NMDA receptor GluN2B-selective antagonists

D Stroebel, DL Buhl, JD Knafels, PK Chanda… - Molecular …, 2016 - ASPET
N-methyl-d-aspartate receptors (NMDARs) are glutamate-gated ion channels that play key
roles in brain physiology and pathology. Because numerous pathologic conditions involve …

Allosteric modulators of NMDA receptors: multiple sites and mechanisms

S Zhu, P Paoletti - Current opinion in pharmacology, 2015 - Elsevier
Highlights•NMDA receptors form massive multi-domain multi-subunit molecular
complexes.•NMDA receptors harbor a multiplicity of binding sites for allosteric modulators.•N …