Structure, function, and pharmacology of glutamate receptor ion channels

KB Hansen, LP Wollmuth, D Bowie, H Furukawa… - Pharmacological …, 2021 - ASPET
Many physiologic effects of l-glutamate, the major excitatory neurotransmitter in the
mammalian central nervous system, are mediated via signaling by ionotropic glutamate …

Glutamate receptor ion channels: structure, regulation, and function

SF Traynelis, LP Wollmuth, CJ McBain, FS Menniti… - Pharmacological …, 2010 - ASPET
The mammalian ionotropic glutamate receptor family encodes 18 gene products that
coassemble to form ligand-gated ion channels containing an agonist recognition site, a …

Chemistry-intuitive explanation of graph neural networks for molecular property prediction with substructure masking

Z Wu, J Wang, H Du, D Jiang, Y Kang, D Li… - Nature …, 2023 - nature.com
Graph neural networks (GNNs) have been widely used in molecular property prediction, but
explaining their black-box predictions is still a challenge. Most existing explanation methods …

Ionotropic and metabotropic glutamate receptor structure and pharmacology

JNC Kew, JA Kemp - Psychopharmacology, 2005 - Springer
Rationale l-Glutamate is the major excitatory neurotransmitter in the central nervous system
(CNS) and mediates its actions via activation of both ionotropic and metabotropic receptor …

Medicinal chemistry of hERG optimizations: highlights and hang-ups

C Jamieson, EM Moir, Z Rankovic… - Journal of medicinal …, 2006 - ACS Publications
In recent years, withdrawal of marketed drugs including sertindole, grepafloxacin, and
terfenadine owing to prolongation of the length of time between the start of the Q wave and …

Predictive in silico modeling for hERG channel blockers

AM Aronov - Drug discovery today, 2005 - Elsevier
hERG-mediated sudden death as a side effect of non-antiarrhythmic drugs has been
receiving increased regulatory attention. Perhaps owing to the unique shape of the ligand …

A comprehensive description of GluN2B-selective N-methyl-D-aspartate (NMDA) receptor antagonists

W Liu, X Jiang, Y Zu, Y Yang, Y Liu, X Sun, Z Xu… - European journal of …, 2020 - Elsevier
Abstract l-glutamate is an excitatory neurotransmitter in the central nervous system (CNS),
which can activate ionotropic receptors (iGluRs) and metabotropic (mGluRs) receptors. N …

Control of assembly and function of glutamate receptors by the amino-terminal domain

KB Hansen, H Furukawa, SF Traynelis - Molecular pharmacology, 2010 - ASPET
The extracellular amino-terminal domains (ATDs) of the ionotropic glutamate receptor
subunits form a semiautonomous component of all glutamate receptors that resides distal to …

In vivo‐and in silico‐driven identification of novel synthetic quinoxalines as anticonvulsants and AMPA inhibitors

HS Abulkhair, S Elmeligie, A Ghiaty… - Archiv der …, 2021 - Wiley Online Library
The lack of effective therapies for epileptic patients and the potentially harmful
consequences of untreated seizure incidents have made epileptic disorders in humans a …

[HTML][HTML] Pharmacology of NMDA receptors

DT Monaghan, DE Jane - 2011 - europepmc.org
The discovery of NMDA receptors (NMDARs) was made possible by the synthesis and study
of NMDA (Figure 12.1) and various NMDAR antagonists by Jeff Watkins and colleagues [1] …