Results 71 to 80 of about 121,181 (303)

Pharmacokinetics of Fipaxalparant, a Small‐Molecule Selective Negative Allosteric Modulator of Lysophosphatidic Acid Receptor 1, and the Effect of Food in Healthy Volunteers

Clinical pharmacology in drug development
Dysregulated lysophosphatidic acid receptor 1 (LPAR1) signaling is implicated in fibrotic diseases, including systemic sclerosis (SSc) and idiopathic pulmonary fibrosis (IPF).
Yang Song, Farah N. Ali, Zhan Ye, Jennifer Zarzoso, John Rogowski, Yajing Sun, Yan Xin   +6 more
semanticscholar   +1 more source

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

Neurochemistry International, 2012
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 conditions. Until recently, the types of agents available to pharmacologically regulate NMDAR function have been quite limited in terms of mechanism of action and subtype selectivity ...
Monaghan, Daniel T., Irvine, Mark W., Costa, Blaise Mathias, Fang, Guangyu, Jane, David E.   +4 more
openaire   +3 more sources

Effect of γ value on binding of allosteric modulator to two allosteric sites.

, 2019
Simulation of tracer binding (ordinate) in the presence an allosteric modulator binding to two allosteric sites for various combinations of positive and negative cooperativity with the tracer indicated at headings of individual plots.
Esam E. El-Fakahany (339452), Alena Randáková (339451), Jan Jakubík (339449), Vladimír Doležal (339453)   +3 more
core   +1 more source

A Light-Controlled Allosteric Modulator Unveils a Role for mGlu4 Receptors During Early Stages of Ischemia in the Rodent Cerebellar Cortex

Frontiers in Cellular Neuroscience, 2018
Metabotropic glutamate receptors (mGlus) are G Protein coupled-receptors that modulate synaptic transmission and plasticity in the central nervous system.
Simon Bossi, Romain Helleringer, Micaela Galante, Ester Monlleó, Ana Trapero, Xavier Rovira, Hervé Daniel, Amadeu Llebaria, Heather McLean   +8 more
doaj   +1 more source

Radiprodil, a selective GluN2B negative allosteric modulator, rescues audiogenic seizures in mice carrying the GluN2A(N615S) mutation

British Journal of Pharmacology
GRIN‐related disorders are neurodevelopmental disorders caused by mutations in N‐methyl‐D‐aspartate receptor (NMDAR) subunit genes. A large fraction of these mutations lead to a ‘gain of function’ (GoF) of the NMDAR.
I. Bertocchi, L. Cifarelli, A. Oberto, Carola Eva, R. Sprengel, N. Mirza, Pierandrea Muglia   +6 more
semanticscholar   +1 more source

Effect of δ value on binding of allosteric modulator to two allosteric sites.

, 2019
Simulation of tracer binding (ordinate) in the presence an allosteric modulator binding to two allosteric sites for various combinations of positive and negative cooperativity with the tracer indicated at headings of individual plots.
Esam E. El-Fakahany (339452), Alena Randáková (339451), Jan Jakubík (339449), Vladimír Doležal (339453)   +3 more
core   +1 more source

Negative and positive allosteric modulators of the α7 nicotinic acetylcholine receptor regulates the ability of adolescent binge alcohol exposure to enhance adult alcohol consumption

Frontiers in Behavioral Neuroscience, 2023
Rationale and Objectives: Ethanol acts directly on the α7 Nicotinic acetylcholine receptor (α7). Adolescent-binge alcohol exposure (ABAE) produces deleterious consequences during adulthood, and data indicate that the α7 receptor regulates these damaging ...
Zachary A. Rodd, Zachary A. Rodd, H. Scott Swartzwelder, R. Aaron Waeiss, R. Aaron Waeiss, Serhii O. Soloviov, Serhii O. Soloviov, Debomoy K. Lahiri, Debomoy K. Lahiri, Debomoy K. Lahiri, Debomoy K. Lahiri, Debomoy K. Lahiri, Eric A. Engleman, Eric A. Engleman, William A. Truitt, William A. Truitt, Richard L. Bell, Richard L. Bell, Sheketha R. Hauser, Sheketha R. Hauser   +19 more
doaj   +1 more source

A novel class of negative allosteric modulators of NMDA receptor function

Bioorganic & Medicinal Chemistry Letters, 2015
NMDA receptors mediate a slow Ca(2+)-permeable component of excitatory synaptic transmission, and are involved in numerous normal brain functions including learning and memory. NMDA receptor over-activation can lead to cell death and abnormal excitation in ischemia associated with stroke, traumatic brain injury, and epilepsy.
Brooke M. Katzman, Riley E. Perszyk, Hongjie Yuan, Yesim Altas Tahirovic, Ayodeji E. Sotimehin, Stephen F. Traynelis, Dennis C. Liotta   +6 more
openaire   +3 more sources

Concentration dependence of binding of allosteric modulator to two allosteric sites.

, 2019
Simulation of tracer binding (ordinate) in the presence an allosteric modulator binding to two allosteric sites for various combinations of positive and negative cooperativity with the tracer indicated at headings of individual plots.
Esam E. El-Fakahany (339452), Alena Randáková (339451), Jan Jakubík (339449), Vladimír Doležal (339453)   +3 more
core   +1 more source

Cell geometry and membrane protein crowding constrain Escherichia coli growth rate, overflow metabolism, respiration, and maintenance energy

FEBS Letters, EarlyView.
The physical dimensions and shape of bacterial cells define the surface area available to acquire nutrients and the volume available for synthesizing proteins and DNA. Here, we use computational systems biology to decode the importance of cell geometry as a major determinant of prokaryotic phenotype, including growth rate and metabolic efficiency. This
Ross P. Carlson, Tomáš Gedeon, Mauricio Garcia Benitez, Campbell Putnam, William R. Harcombe, Radhakrishnan Mahadevan, Ashley E. Beck   +6 more
wiley   +1 more source