GluN2A‐Selective NMDA Receptor Antagonists: Mimicking the U‐Shaped Bioactive Conformation of TCN‐201 by a [2.2]Paracyclophane System
Sign Up to like & getrecommendations! Published in 2022 at "Chemmedchem"
DOI: 10.1002/cmdc.202200484
Abstract: Under physiological conditions, N‐Methyl‐D‐Aspartate (NMDA) receptors play a crucial role for synaptic plasticity, long‐term potentiation and long‐term depression. However, overactivation of NMDA receptors can result in excitotoxicity, which is associated with various neurological and neurodegenerative… read more here.
Keywords: nmda receptor; tcn 201; receptor antagonists; selective nmda ... See more keywords
Pharmacokinetic properties of enantiomerically pure GluN2B selective NMDA receptor antagonists with 3-benzazepine scaffold.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of pharmaceutical and biomedical analysis"
DOI: 10.1016/j.jpba.2019.04.032
Abstract: Recently, the eutomers of highly potent GluN2B selective NMDA receptor antagonists with 3-benzazepine scaffold were identified. Herein, pharmacokinetic properties regarding lipophilicity, plasma protein binding (PPB) and metabolism are analyzed. The logD7.4 values of 1.68 for… read more here.
Keywords: benzazepine scaffold; glun2b selective; selective nmda; nmda receptor ... See more keywords
The Selective NMDA Receptor GluN2B Subunit Antagonist CP-101,606 with Antidepressant Properties Modulates Cytochrome P450 Expression in the Liver
Sign Up to like & getrecommendations! Published in 2021 at "Pharmaceutics"
DOI: 10.3390/pharmaceutics13101643
Abstract: Recent research indicates that selective NMDA receptor GluN2B subunit antagonists may become useful for the treatment of major depressive disorders. We aimed to examine in parallel the effect of the selective NMDA receptor GluN2B subunit… read more here.
Keywords: selective nmda; nmda receptor; 101 606; receptor glun2b ... See more keywords