127910-31-0

CGP 37849 potently (K_i of 220 nM) and competitively inhibits NMDA-sensitive l-[³H]-glutamate binding to postsynaptic density (PSD) fractins from rat brain. CGP 37849 inhibits the binding of the selective NMDA receptor antagonist, [³H]-(±)-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonate (CPP), with a K_i of 35 nM^[1].
In vivo, oral administration to rats of CGP 37849 selectively blocks firing in hippocampal neurones induced by ionophoretically-applied NMDA, without affecting the responses to quisqualate or kainate^[1].
Oral administration to mice of CGP 37849 suppresses maximal electroshock-induced seizures in mice with an ED₅₀ of 21 mg/kg^[1].