• NMDA
  • These strychnine-sensitive binding sites are different from the strychnine-insensitive binding sites found in the N-methyl-D-aspartate (NMDA) subtype of glutamate receptors. (novusbio.com)
  • Moreover, PSD‐95, the central organising element of the PSD that links NMDA receptors to the cytoskeleton, has been shown to be phosphorylated by the serine/threonine kinase Cdk‐5, and this event appears to negatively regulate the clustering of NMDA receptors ( Morabito et al , 2004 ). (embopress.org)
  • Work in our laboratory first identified the N -Methyl-D-aspartate (NMDA) subtype of glutamate receptor as a molecular target for xenon, 9 , 10 and we subsequently showed that xenon inhibits NMDA receptors by competing with the coagonist glycine at the glycine-binding site on the GluN1 subunit. (asahq.org)
  • 11 The finding that xenon is an NMDA receptor antagonist led to the idea that xenon could be used as a neuroprotectant, as overactivation of NMDA receptors plays a role in various pathologic conditions, such as ischemia, stroke, and traumatic brain injury. (asahq.org)
  • 15 - 26 We have recently shown that xenon neuroprotection against hypoxic/ischemic injury in vitro is mediated by xenon inhibition at the glycine site of the NMDA receptor. (asahq.org)
  • It also acts as an NMDA receptor antagonist, inhibits nACh and voltage-gated sodium channels, and activates 5-HT3 and twin-pore K+ channels. (wikipedia.org)
  • The drug is a rapid-acting and long-lasting antidepressant as well as robust cognitive enhancer by virtue of its ability to both inhibit and enhance NMDA receptor-mediated signal transduction. (wikipedia.org)
  • Rapastinel belongs to a group of compounds, referred to as glyxins (hence the original developmental code name of rapastinel, GLYX-13), that were derived via structural modification of B6B21, a monoclonal antibody that similarly binds to and modulates the NMDA receptor. (wikipedia.org)
  • Glyxins and B6B21 do not bind to the glycine site of the NMDA receptor but rather to a different regulatory site on the NMDA receptor complex that serves to allosterically modulate the glycine site. (wikipedia.org)
  • As such, rapastinel is technically an allosteric modulator of the glycine site of the NMDA receptor, and hence is more accurately described as a functional glycine site weak partial agonist. (wikipedia.org)
  • In concert with a learning task, rapastinel has also been shown to elevate gene expression of hippocampal NR1, a subunit of the NMDA receptor, in three-month-old rats. (wikipedia.org)
  • Additionally, rapastinel has demonstrated antinociceptive activity, which is of particular interest, as both competitive and noncompetitive NMDA receptor antagonists are ataxic at analgesic doses, while rapastinel and other glycine subunit ligands are able to elicit analgesia at non-ataxic doses. (wikipedia.org)
  • It inhibits receptor activity in the NMDA glutamate receptor subtypes. (wikipedia.org)
  • distribution of glycine
  • Immunocytochemistry at the light microscope level with immunofluorescence and silver-intensified colloidal gold revealed a wide distribution of glycine-like immunoreactivity throughout all laminae of the rat spinal cord and in all segments studied from the cervical, thoracic, lumbar, and sacral cord. (jneurosci.org)
  • The concentration and relative distribution of glycine receptors were determined for gerbil brain stem auditory nuclei using 3H-strychnine and quantitative autoradiographic techniques. (jneurosci.org)
  • Mutations
  • showed that mutations M287L in the transmembrane 3 region and Q266I in the transmembrane 2 region of the α1 subunit lead to a reduction in ethanol potentiation of glycine-induced current. (aspetjournals.org)
  • modulation
  • Low-nanomolar concentrations of contaminating zinc in electrophysiological buffers are capable of synergistically enhancing receptor modulation by other compounds, such as ethanol. (aspetjournals.org)
  • This suggests that, unless accounted for, previous studies of glycine receptor modulation were measuring the effects of modulator plus comodulation by zinc on receptor function. (aspetjournals.org)
  • Since zinc is present in vivo at a variety of concentrations, it will influence glycine receptor modulation by other pharmacologic agents. (aspetjournals.org)
  • alpha1
  • the TM3-4 loop length is critical for glycine receptor alpha1 desensitization and a direct neighborhood of both basic stretches changes receptor properties from non-desensitizing to desensitizing. (nih.gov)