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={Phil Skolnick and Kathleen M. K. Boje and Ruthellen Miller and Michael Pennington and Maria L. Maccecchini},
  journal={Journal of neurochemistry},
  year={1992},
  volume={59 4},
  pages={1516-21}
}
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 approximately 507 and approximately 946 nM, respectively. In contrast… CONTINUE READING

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