Benzyl-polyamines: novel, potent N-methyl-D-aspartate receptor antagonists.

  title={Benzyl-polyamines: novel, potent N-methyl-D-aspartate receptor antagonists.},
  author={Kazuei Igarashi and Akira Shirahata and A J Pahk and Keiko Kashiwagi and Keith W Williams},
  journal={The Journal of pharmacology and experimental therapeutics},
  volume={283 2},
The effects of benzyl-polyamines were studied at recombinant N-methyl-D-aspartate (NMDA) receptors expressed in Xenopus laevis oocytes. A number of mono-, di- and tri-benzyl polyamines, having benzyl substitutions on the terminal or central amino groups, inhibited responses of NR1/NR2 receptors in oocytes voltage-clamped at -70 mV. Among the most potent compounds was N1,N4, N8-tri-benzyl-spermidine (TB-3-4), which had an IC50 value of 0.2 microM. TB-3-4 was approximately 40-fold more potent at… CONTINUE READING
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Differential contribution of the NR 1 - and NR 2 A - subunits to the selectivity filter of recombinant NMDA receptor channels

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