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  • 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)
  • 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)
  • 1995
  • Kneussel et al , 1999b ), whereas it only functionally associates with individual GABA A receptor subtypes ( Meyer et al , 1995 ). (embopress.org)
  • subunits
  • Adult glycine receptors are heterodimers composed of two subunits of 48 kDa and 58 kDa, denoted as a1 and b subunits. (novusbio.com)
  • Fetal glycine receptors are homomers composed of a2 subunits. (novusbio.com)
  • Receptors of this family are arranged as five subunits surrounding a central pore, with each subunit composed of four α helical transmembrane segments. (wikipedia.org)
  • The α-subunits are also able to form functional homo-pentameric receptors in heterologous expression systems in African clawed frog's oocytes or mammalian cell lines, and the α1 homomeric receptor is essential for studies of channel pharmacokinetics and pharmacodynamics. (wikipedia.org)
  • these receptors are formed by five subunits arranged in a pseudosymmetric ring around the central pore. (jneurosci.org)
  • It is a pentameric receptor composed of alpha and beta subunits. (wikipedia.org)
  • In other receptors, this mutation shifts agonist sensitivity in proportion to the number of mutated subunits. (ucl.ac.uk)
  • extracellular
  • In each subunit, the extracellular glycine-binding domains form a juxtamembrane interface with the membrane helices and the conserved M2-M3 loop, through which conformational changes induced by agonist binding propagate to the channel gate. (jneurosci.org)
  • Glycine release was independent of neuronal activity or extracellular Ca 2+ . (jneurosci.org)
  • modulators
  • This is the talk page for discussing improvements to the Glycine receptor modulators template. (wikipedia.org)
  • We investigated the utility of previously described "zinc-enhancement-insensitive" α 1 glycine receptor mutants D80A, D80G, and W170S to probe for interactions between zinc and other allosteric modulators at the glycine receptor. (aspetjournals.org)
  • Additionally, we determined that this interaction is abolished at higher zinc concentrations when receptor-enhancing binding sites are saturated, suggesting a mechanism by which modulators such as ethanol and inhalants are capable of increasing receptor affinity for zinc, in addition to enhancing channel function on their own. (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)