References in periodicals archive ?
To allow the crystallization of ER[alpha] bound to the environmental molecules acting essentially as partial agonists that are unable to induce a stable conformation of the LBD, we used the ER[alpha]-Y537S LBD mutant described previously by Nettles et al.
Relevance of Vilazodone's 5-HT1A receptor partial agonist effect
Table Neurotransmitter Systems in the Brain Involved in Different Stages of the Addiction Cycle and Existing and Potential Pharmacotherapies Targeting Them in the Treatment of Alcohol Dependence Neurotransmitter System Existing and Potential Pharmacotherapies Dopamine system Dopamine receptor partial agonists * [D.
GLYX-13, an NMDA receptor glycine site functional partial agonist enhances cognition and produces antidepressant effects without the psychotomimetic side effects of NMDA receptor antagonists.
Vilazodone, if approved, will be a welcome addition to the treatment armamentarium for patients who suffer from depression, due to its overall efficacy and safety profile, combined with a novel mechanism of action as both an inhibitor of serotonin reuptake and a serotonin 1A receptor partial agonist.
GLYX-13 is a selective NMDA receptor partial agonist, a new class of central nervous system-active compounds discovered by Naurex scientists.
OBJECTIVES: We assessed the ability of generalized concentration addition (GCA) to predict effects of combinations of full AhR agonists with partial agonists or competitive antagonists.
GLYX-13 is Naurex's lead glycine-site functional partial agonist (GFPA) selective modulator of the NMDA receptor.
Given the role that the AhR plays in critical physiologic functions and the potential limitations in assessing the significance of exposures to contaminant mixtures, we propose that a broader perspective and a complementary biological approach be considered, specifically because the cumulative biological effects of agonists, partial agonists, and antagonists are impossible to predict from analytical assays.
is a private company developing novel therapies for depression and other CNS disorders based on a new mechanism of action for modulating the NMDA receptor in a safe way-glycine-site functional partial agonists (GFPAs).
BIND technology for cell-based assays offers an orthogonal screening tool to access new hits and lead molecules that are not detected by other systems, including compounds that undergo G-protein switching, non-G protein coupled pathways, inverse and partial agonists, and receptor desensitization.
Glycine site functional partial agonists, which modulate the NMDA receptor in a novel and selective way, are being developed with the goal of achieving the antidepressant efficacy and rapid onset seen with conventional NMDA receptor modulators, but without the psychotomimetic side effects that have limited the utility of these agents in the past.