N1-dansyl-spermine:: a potent polyamine antagonist

(T)he potential polyamine antagonist action of N-1-dansyl-spermine (a potent NMDA antagonist) was assessed in two in vivo mouse models of polyamine action. Co-administration of N-1-dansyl-spermine (2-10 mug, i.c.v.) with spermine (100 mug, i.c.v.) resulted in a dose-dependent antagonism of the spermine-induced CNS excitation (body tremor and fatal tonic convulsions). In addition, the same dose of N-1-dansylspermine antagonised spermine's enhancement of NMDA-induced convulsions. These results suggest that N-1-dansyl-spermine is in vivo a potent antagonist of the CNS effects of spermine and of its action at the positive polyamine modulatory site on the NMDA receptor. (C) 2004 Elsevier B.V. All rights reserved.