Endogenous indoles as novel polyamine site ligands at the N-methyl-D-aspartate receptor complex

High-throughput ligand displacement screens of a series of endogenous indol es revealed that tryptamine, serotonin and 5-methoxytryptamine readily disp lace [H-3]spermidine and [H-3]MK-801 from their respective binding sites in rat brain homogenate. These data, coupled with their potent inhibition of spermidine-potentiated [H-3]MK-801 binding, suggest that certain endogenous indoles may act as Ligands to one or more polyamine binding sites in the b rain, including those on the N-methyl-D-aspartate receptor complex. (C) 200 1 Elsevier Science B.V. All rights reserved.