Identification and characterization of novel NMDA receptor antagonists selective for NR2A-over NR2B-containing receptors

…, M Negri, F Andreetta, SA Senar-Sancho… - … of Pharmacology and …, 2010 - ASPET
NR1/NR2A is a subtype of N-methyl-d-aspartate receptors (NMDARs), which are glutamate
and glycine-gated Ca 2+ -permeable channels highly expressed in the central nervous …

High throughput screening assay to identify modulators of IL-17 expression

…, G Colmenarejo, SA Senar-Sancho… - … Chemistry & High …, 2017 - ingentaconnect.com
Objective: Herein we demonstrate the successful development of a new RORγt-enhanced IL-17F
promoter-luciferase reporter assay and its use in a parallel high throughput screening …

Validation and optimization of novel high-throughput assays for human epithelial sodium channels

MX Chen, K Gatfield, E Ward… - Journal of …, 2015 - journals.sagepub.com
The epithelial sodium channel (ENaC) plays a crucial role in salt and water homeostasis
and is primarily involved in sodium reabsorption in the kidney and lung. Modulators of ENaC …

Structure and symmetry inform gating principles of ionotropic glutamate receptors

S Zhu, E Gouaux - Neuropharmacology, 2017 - Elsevier
Ionotropic glutamate receptors (iGluRs) transduce signals derived from release of the
excitatory neurotransmitter glutamate from pre-synaptic neurons into excitation of post-synaptic …

NMDA-induced ERK signalling is mediated by NR2B subunit in rat cortical neurons and switches from positive to negative depending on stage of development

A Sava, E Formaggio, C Carignani, F Andreetta… - …, 2012 - Elsevier
It is known that NMDA receptor stimulation can activate or inhibit the extracellular signal-regulated
kinase (ERK) signalling cascade, a key pathway involved in neuronal plasticity and …

A structural biology perspective on NMDA receptor pharmacology and function

MC Regan, A Romero-Hernandez… - Current opinion in …, 2015 - Elsevier
Highlights • The NMDA receptor is a membrane protein critical to mammalian learning and
memory. • Heterotetrameric NMDARs consist of three structured domains that regulate ion flux…

NMDA receptors containing the GluN2D subunit control neuronal function in the subthalamic nucleus

SA Swanger, KM Vance, JF Pare, F Sotty… - Journal of …, 2015 - Soc Neuroscience
The GluN2D subunit of the NMDA receptor is prominently expressed in the basal ganglia
and associated brainstem nuclei, including the subthalamic nucleus (STN), globus pallidus, …

[PDF][PDF] Triheteromeric GluN1/GluN2A/GluN2C NMDARs with unique single-channel properties are the dominant receptor population in cerebellar granule cells

S Bhattacharya, A Khatri, SA Swanger, JO DiRaddo… - Neuron, 2018 - cell.com
NMDA-type glutamate receptors (NMDARs) are ligand-gated ion channels that mediate
excitatory neurotransmission in the CNS. Here we describe functional and single-channel …

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 …

Autoimmunity and COPD: clinical implications

G Caramori, P Ruggeri, A Di Stefano, S Mumby… - Chest, 2018 - Elsevier
COPD is a leading cause of morbidity and mortality worldwide. Long-term cigarette smoking
is the cause of > 90% of COPD cases in Westernized countries. However, only a fraction of …