Glutamate Antagonists

Multiple glutamate receptor antagonists were taken into phase II and III trials, including: the competitive NMDA receptor antagonists selfotel (CGS 19755) and aptiganel (CNS 1102), which block the binding of glutamate to its receptor complex recognition site; eliprodil, which blocks the polyamine site; and CP-101,606, which blocks the NR2B subunit on the NMDA receptor complex. None of these produced a statistically significant improvement in neurological recovery in TBI or ischemic stroke trials.15,16

An alternative mechanism for countering glutamate excitotoxicity is to increase g-amino-butyric acid (GABA) mediated inhibitory transmission with the administration of GABA receptor agonists. This approach resulted in the clinical evaluation of the GABA partial agonist new compound entity chlomethiazole in a phase III stroke trial. However, no significant beneficial effect was demonstrated.15'16

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