The effects of the anxiolytic drug buspirone and its metabolite 1-PP on the dopaminergic system were investigated. A single buspirone administration was found to decrease DA levels and increase its metabolite DOPAC in striatal samples. The levels of the other DA metabolite, 3MT, were unaffected; however its formation rate after inhibition of its metabolism, was found to be increased by buspirone. 1-PP did not affect either DOPAC or 3MT levels and formation. Striatal microdialysis showed that buspirone enhances DA release. In vivo voltammetry indicates that the increase of DA metabolism is identical in the two sampled dopaminergic areas, striatum and nucleus accumbens. On the basis of the results obtained ex vivo and in vivo the multiple effect of buspirone on dopaminergic system is discussed.