
Structural basis of subtype-selective competitive antagonism ... - Nature
Jan 22, 2020 · We also estimated EC 50 values of l-glutamate by measuring macroscopic currents at a fixed Gly concentration (100 µM) and varying l-glutamate concentrations (Fig. 2c).
A Common Molecular Basis for Exogenous and Endogenous …
Apr 4, 2012 · We first determined the EC 50 values from the Gly concentration–response curves in HEK-293 cells transfected with α1 α2 or α3 subunits of GlyR. The EC 50 values for Gly were …
Diverse modes of NMDA receptor positive allosteric modulation ...
Jan 1, 2017 · NMDAR PAMs work by either increasing maximal current (type I effect) or decreasing agonist EC50 (type II effect), or both. Several chemically distinct classes of …
Endogenous Opioid Peptides and Alternatively Spliced Mu …
Contrastingly, β-endorphin was more potent in stimulating [35 S]GTPγS binding in mMOR-1O (EC 50: 6 nM) than in mMOR-1D (EC 50: 73 nM). The mismatch between the K i and EC 50 values …
EC50 - Wikipedia
Half maximal effective concentration (EC 50) is a measure of the concentration of a drug, antibody or toxicant which induces a biological response halfway between the baseline and maximum …
Structural Determinants and Mechanism of Action of a GluN2C …
The EC 50 values for PYD-106 enhancement of the maximal response of GluN1-1b K211G and GluN1-1b K211R were 9.5 ± 0.9 μM (n = 3) and 9.0 ± 1.9 (n = 6) μM, respectively, which were …
Biased ligand quantification in drug discovery: from theory to high ...
This work demonstrates that using Δlog(Emax /EC50 ), drug discovery can apply the concept of biased ligand quantification on a large scale and accelerate the deliberate discovery of novel …
Presynaptic glycine receptors as a potential therapeutic target for ...
DH-CBD at 10 μM significantly reduced the Gly EC 50 value and increased the maximal I Gly for the α1R271Q GlyRs (Fig. 2b). The rescue of α1R271Q mutant GlyR deficiency was dependent …
Positive Allosteric Modulators of GluN2A-Containing NMDARs …
Mar 2, 2016 · Individual GluN2A PAMs exhibited variable degrees of glutamate (Glu) dependence, impact on NMDAR Glu EC 50, and slowing of channel deactivation. These …
Heterocarrier-mediated reciprocal modulation of glutamate and …
Jan 24, 1994 · Gly enhanced the outflow of [3H]D-Asp from rat cerebral cortex and spinal cord synaptosomes (EC50 = 75.0 and 99.5 microM, respectively). Gly was much more potent a …