Abstract
Activation of receptors for NMDA has been shown to be associated with seizures and ischemic damage in brain. Neuromodulation of NMDA-mediated activity can occur at several sites including strychnine-insensitive glycine receptors (SIGR). Autoradiography reveals that felbamate is capable of interacting with SIGR in human brain. This property is not shared by the other anticonvulsant compounds including carbamazepine, phenytoin, valproic acid and phenobarbital even when present at relatively high concentrations. The results show that felbamate decreases antagonist ([3H]5,7 dichlorokynurenic acid) binding, but increases agonist ([3H]glycine) binding at SIGR. Felbamate is acting as a functional antagonist at subtypes of SIGR, or at an allosterically coupled site on the protein, to modulate NMDA associated channel opening in human brain. This property is related to the effectiveness of the compound as a unique anticonvulsant and neuroprotectant.
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Wamsley, J., Sofia, D. & McCabe, T. Binding Of Felbamate To Glycine Receptors In Human Postmortem Brain: Role In Mediating Anticonvulsant And Neuroprotectant Effects. Neuropsychopharmacol 11, 289 (1994). https://doi.org/10.1038/sj.npp.1380229
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DOI: https://doi.org/10.1038/sj.npp.1380229