CGP 37849 potently (Ki 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 Ki 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].
