Felbamate block of recombinant N-methyl-D-aspartate receptors: Selectivity for the NR2B subunit

  • Harty T
  • Rogawski M
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The anticonvulsant felbamate blocks N-methyl-D-asparate (NMDA) receptors but fails to exhibit the neurobehavioral toxicity characteristic of other NMDA receptor antagonists. To investigate the possibility that felbamate's favorable toxicity profile could be related to NMDA receptor subtype selectivity, we examined the specificity of felbamate block of recombinant NMDA receptors composed of the NR1a subunit and various NR2 subunits. Felbamate produced a rapid, concentration-dependent block of currents evoked by 50 μM NMDA and 10 μM glycine in human embryonic kidney 293 cells expressing the rat NR1a subunit, and either the NR2A, NR2B or NR2C subunits; the IC50values for block were 2.6, 0.52 and 2.4 mM, respectively (holding potential, -60 mV). The Hill coefficient values were

Author-supplied keywords

  • Felbamate
  • NMDA receptor
  • NR2 subunit
  • Voltage-clamp recording

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  • T. Patrick Harty

  • Michael A. Rogawski

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