The compound BHT-920 has been shown to be therapeutically effective in the treatment of schizophrenic symptoms. The present studies showed that BHT-920 selectively modified dopaminergic transmission in corpus striatum by reducing tyrosine hydroxylase activity. This effect was not demonstrable in other brain areas or in peripheral nervous tissue. The decrease in enzyme activity elicited by BHT-920 was attenuated by haloperidol. BHT-920 reduced the specific binding of 3H- Haloperidol but not of 3H-N-propylnorapomorphine, suggesting an interaction of this compound at the D2-dopamine receptor sites.