CGP 37849 is a competitive orally active N-methyl-D-aspartate (NMDA) receptor antagonist ((Ki = 35 nM)) with potency.CGP 37849 is an anticonvulsant in rodents and also has antidepressant and anxiolytic properties.

[3H]-(±)-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonate (CPP):35 nM(Ki), l-[3H]-glutamate:220 nM(Ki), Seizures:21 mg/kg(ED50)

Within the hippocampal slice in vitro, CGP 37849 demonstrates reversible and selective antagonism against NMDA-induced increases in the firing rate of CA1 pyramidal cells. In the presence of a low Mg2+ level medium, concentrations of CGP 37849 up to 10 μM effectively inhibit burst firing evoked in CA1 neurons by stimulating Schaffer collateral-commissural fibers, while leaving the magnitude of the initial population spike unaffected.[1]

In vivo, oral administration to rats of CGP 37849 selectively blocks firing in hippocampal neurons 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]