INHIBITORY EFFECTS OF PENTAMIDINE ANALOGS ON SPERMINE STIMULATED LIGAND-BINDING TO THE NMDA RECEPTOR COMPLEX

SAR studies of butamidine derivatives with the NMDA receptor complex r evealed that hydrophobic rather than hydrophilic linkers between the a midinophenyl groups promote NMDA antagonism. Conformation of the linke r did not influence binding in the absence of bis-methoxy substituents ortho to the linker. Like pentamidine, the compounds are noncompetiti ve NMDA receptor antagonists. (C) 1997 Elsevier Science Ltd.