Noncompetitive Inhibition of N‐Methyl‐D‐Aspartate by Conantokin‐G: Evidence for an Allosteric Interaction at Polyamine Sites

@article{Skolnick1992NoncompetitiveIO,
  title={Noncompetitive Inhibition of N‐Methyl‐D‐Aspartate by Conantokin‐G: Evidence for an Allosteric Interaction at Polyamine Sites},
  author={P. Skolnick and K. Boje and R. Miller and M. Pennington and M. Maccecchini},
  journal={Journal of Neurochemistry},
  year={1992},
  volume={59}
}
Abstract: Conantokins T and G are polypeptide toxins present in snails of the genus Conus. These substances were recently reported to act as N‐methyl‐D‐aspartate (NMDA) antagonists. In the present study, we examined the possible mechanisms producing this antagonism. Conantokin‐G inhibited spermine‐ and spermidine‐stimulated [3H]MK‐801 binding to extensively washed rat forebrain membranes in a noncompetitive manner with IC50 values of ∼507 and ∼946 nM, respectively. In contrast, glutamate… Expand
Synthetic Analogues of Conantokin‐G: NMDA Antagonists Acting Through a Novel Polyamine‐Coupled Site
NMDA receptor subunit‐dependent modulation by conantokin‐G and Ala(7)‐conantokin‐G
Amino acid determinants for NMDA receptor inhibition by conantokin‐T
Conantokin G is an NR2B-selective competitive antagonist of N-methyl-D-aspartate receptors.
Direct binding properties of conantokins to native N-methyl-d-aspartate receptors.
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