MK-801 (dizocilpine maleate), a non-competitive, N-methyl-D-aspartate receptor antagonist which induces a characteristic phencyclidine-like motor syndrome in rodents, was administered to rats after handling habituation to examine the effects of this drug on concentrations of monoamines and their metabolites in 14 brain regions. MK-801 increased dopamine and serotonin metabolism in several regions, the most marked effects being determined in frontal and piriform cortex, nucleus accumbens and striatum. The data indicate that not only effects on dopaminergic transmission but also on serotonergic transmission may be involved in the pharmacological actions of MK-801.